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Available online at www.icjpir.com ISSN: 2349-5448
Intercontinental journal of pharmaceutical
Investigations and Research
ICJPIR |Volume 4 | Issue 1 | Jan – Mar- 2017 Research Article
Formulation and evaluation of Rosiglitazone nanosuspension
K.Hemalatha, S.Rajashekar
CMR of Pharmacy, Kandlakoya Hyderabad, Telangana
Corresponding Author: K.Hemalatha
Email: hemasweety.latha903@gmail.com
ABSTRACT
The main aim of this study is to formulate and evaluate Rosiglitazone Nano suspension. Nano suspensions are
colloidal dispersion of Nano sized drug particles stabilized by surfactants. They can also be defined as a biphasic
system consisting of pure drug particles dispersed in an aqueous vehicle in which the diameter of the suspended
particle is less than 1micro meter in size. Rosiglitazone is an oral rapid and short –acting anti-diabetic drug from the
sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enter hepatic
circulation. Rosiglitazone Nano suspension was prepared by precipitation technique. After preparation of Nano
suspension various characterization studies were done such as drug content, %yield, FTIR, DSC, TEM, and Invitro
drug release.PVPK30,polaxomer are used as stabilizers. From the dissolution study F4 formulation which containts
PVPK30 as stabilizer was considered as optimized formulation. It showed maximum drug release at 30min.FTIR and
DSC studies revealed that good stability in dispersion.
INTRODUCTION
Oral drug delivery system
Oral dosage form is the physical form of a dose
of a chemical compound used as a drug or
medication intended for administration or
consumption by oral route. Oral drug delivery is
the most desirable and preferred method of
administering therapeutic agents for their systemic
effects. In addition, the oral medication is generally
considered as the first avenue investigated in the
discovery and development of new drug entities,
pharmaceutical formulations, mainly because of
patient acceptance and convenience in
administration. Of drugs that are administered
orally, solid dosage forms represent the preferred
class of product.
Advantages
 Oral route of drug administration have wide
acceptance up to 50-60% of total dosage forms
 Ease of administration
 Solid dosage forms represent unit dosage forms
in which one usual dose of the drug has been
accurately placed
 Self-medication
 Avoidance of pain
 Patient compliance
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Disadvantages:
 Action of drugs is slower
 Unpalatable drugs are difficult
 May cause nausea and vomiting
Importance of drug solubility
Solubility is one of the important parameter in
Biopharmaceutical classification system (BCS),
and dissolution rate is the most essential factor
controlling the bioavailability of drugs. Poorly
water soluble drugs often require high doses in
order to reach therapeutic plasma concentrations
after oral administration. Low aqueous solubility is
the major problem encountered with formulation
development of new chemical entities as well as
generic development. A compound with solubility
of less than 1 part per 10,000 part of water is
categorized as poorly water soluble drug (sanjeev
K, et al. 2009) [1].
Approaches for enhancement of solubility and
dissolution rate
Solubility behavior of a drug is one of the key
determinants of its oral bioavailability. Noyes-
Whitney equation provides some hints as to how
the dissolution rate of even very poorly soluble
compounds might be improved to minimize the
limitations to oral availability.
dc/dt = AD ( Cs-C )/h
Where, dC/dt = rate of dissolution
A = surface area available for dissolution
D =diffusion coefficient of the compound
Cs= solubility of the compound in the dissolution
medium
C =concentration of drug in the medium at time t
h =thickness of the diffusion boundary layer adjacent
to the surface of the dissolving compound.
To increase the dissolution rate from equation the
following approaches are available.
1. To increases the surface area available for
dissolution by
 Decreasing the particle size of drug.
 Optimizing the wetting characteristics of
compound surface.
2. To decrease the boundary layer thickness.
3. Ensure sink condition for dissolution.
4. Improving apparent solubility of drug under
physiologically relevant conditions.
Methods for enhancement of bioavailability:
(Pinnamaneni S, et al. 2002) [2]
There are numerous techniques to enhance
bioavailability, which involves:
Physical modification
Physical modification often aims to increase the
surface area, solubility and wet ability of the
powder particles and is therefore focused on
particle size reduction or generation of amorphous
states. The various approaches under this method
are:
i. Particle size reduction:
 Micronization
 Nanosuspension
ii. Modifications of the crystal habit:
 Polymorphs.
 Pseudo polymorphs (including solvates)
iii. Complexation / solubilization:
 Use of cyclodextrines
 Use of surfactants
iv. Drug dispersion in carriers:
 Solid dispersions
 Eutectic mixtures
 Solid solutions
Chemical modification
Chemical modification aim at altering the drug
chemically by various methods in order to produce
a water soluble compound. The widely used
approaches under this category are:
 Formation of soluble prodrugs
 Formation of salts of the compound
 Preparation of covalent polymer drug conjugates.
Nanosuspension
Nanosuspension is favoured for compounds that
are insoluble in water (but are soluble in oil) with
high log P value, high melting point and high
doses. Nanosuspension technology can also be used
for drugs which are insoluble in both water and
organic solvents. Hydrophobic drugs such as
Atorvastatin, 13 Famotidine, 14 Simvastatin, 15
Revaprazan, 16 Aceclofenac, 17 are formulated as
Nanosuspension. Nanosuspensions are colloidal
dispersions of nanosized drug particles stabilized
by surfactants. They can also be defined as a
biphasic system consisting of pure drug particles
dispersed in an aqueous vehicle in which the
diameter of the suspended particle is less than 1µm
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in size. The Nanosuspensions can also be
lyophilized or spray dried and the nanoparticles of
a Nanosuspension can also be incorporated in a
solid matrix.( Banavath H, et al. 2010) [3]
Nano is a Greek word, which means „dwarf‟.
Nano means it is the factor of 10-9
or one billionth.
Some comparisons of nanoscale are given below,
0.1 nm = Diameter of one Hydrogen atom.
2.5 nm = Width of a DNA molecule
1micron = 1000 nm.
1 nm = 10-9
m = 10-7
cm = 10-6
mm.
Micron = 10-6
m= 10-4
cm = 10-3
mm 4.
For a long duration of time micronization of
poorly soluble drugs by colloid mills or jet mills
was preferred. The overall particle size distribution
ranges from 0.1µm to approximately 25µm, only
negligible amount being below 1µm in the
nanometer range.
Rationale for nanosuspension
 Preparing nano suspensions is preferred for the
compounds that are insoluble in water (but are
soluble in oil) with high log P value.
 Conventionally the drugs that are insoluble in
water but soluble in oil phase system are
formulated in liposome, emulsion systems but
these lipidic
 Formulation approaches are not applicable to all
drugs. In these cases nano suspensions are
preferred.
 In case of drugs that are insoluble in both water
and in organic media instead of using lipidic
systems Nano suspensions are used as a
formulation approach.
 Nano suspension formulation approach is most
suitable for the compounds with high log P value,
high melting point and high dose.(Mohanty S, et
al.2010) [4]
Benefits of nanosuspension technology for
poorly soluble drugs
 Reduced particle size, increased drug dissolution
rate, increased rate and extent of absorption,
increased bioavailability of drug, area under
plasma versus time curve, onset time, peak drug
level, reduced variability, reduced fed/fasted
effects.
 Nanosuspensions can be used for compounds that
are water insoluble but which are soluble in oil.
On the other hand, Nanosuspensions can be used
in contrast with lipidic systems, successfully
formulate compounds that are insoluble in both
water and oils.
 Nanoparticles can adhere to the gastrointestinal
mucosa, prolonging the contact time of the drug
and thereby enhancing its absorption.
 A pronounced advantage of Nanosuspension is
that there are many administration routes for
Nanosuspensions, such as oral, parenteral,
pulmonary, dermal and ocular.
 Nanosuspension of nanoparticles (NPs) offers
various advantages over conventional ocular
dosage forms, including reduction in the amount
of dose, maintenance of drug release over a
prolonged period of time, reduction in systemic
toxicity of drug, enhanced drug absorption due to
longer residence time of nanoparticles on the
corneal surface, higher drug concentrations in the
infected tissue, suitability for poorly water-
soluble drugs and smaller particles are better
tolerated by patients than larger particles,
therefore nanoparticles may represent auspicious
drug carriers for ophthalmic applications.
 Nanosuspension has low incidence of side effects
by the excipients.
 Nanosuspensions overcome delivery issues for
the compounds by obviating the need to dissolve
them, and by maintaining the drug in a preferred
crystalline state of size sufficiently small for
pharmaceutical acceptability.
 Increased resistance to hydrolysis and oxidation,
increased physical stability to settling.
 Reduced administration volumes; essential for
intramuscular, subcutaneous, ophthalmic use.
 Finally, Nanosuspensions can provide the passive
targeting (.Nagare SK,et al.2012) [5]
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PREPARATION OF NANO SUSPENSION
Figure no 1: Approaches for Preparation of Nano suspension
Precipitation method
Precipitation method is a general method used
to prepare submicron particles of poorly soluble
drugs. [Matteucci ME, et al.2007] [7] In this
method, drug is dissolved in solvent and then
solution is mixed with solvent to which drug is
insoluble in the presence of surfactant. Rapid
addition of solution to such solvent (generally
water) leads to rapid supersaturation of drug in the
solution, and formation of ultrafine amorphous or
crystalline drug. This method involves nuclei
formation and crystal growth which are mainly
dependent on temperature. High nucleation rate and
low crystal growth rate are primary requirements
for preparing a stable suspension with minimum
particle size. [Bodmeier R, et al.1998] [6]
High-pressure homogenization
This technique involve the following three
steps: First, drug powders are dispersed in a
stabilizer solution to form pre suspension; after
that, pre suspension is homogenized by high
pressure homogenizer at a low pressure sometimes
for pre milling; and finally homogenized at a high
pressure for 10 to 25 cycles until the nano
suspension
Figure no 2: High pressure homogenization
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MATERIALS AND METHODS
Materials
The following materials available were used as
supplied by the manufacturer without further
purification or investigation
Table no 2: list of materials used in formulation
S.NO INGREDIENTS SPECIFICATION RATIONALE SOURCE
1 Rosiglitazone USP API CHANDRA LABS
2 PVP USP polymer STANDARD REAGENTS PVT
LTD
3 UREA USP polymer STANDARD REAGENTS PVT
LTD
4 Polaxomer USP polymer STANDARD REAGENTS PVT
LTD
5 Potassium dihydrogen
phosphate
USP Buffer STANDARD REAGENTS PVT
LTD
6 HCL USP STANDARD REAGENTS PVT
LTD
7 Sodium hydroxide pellets USP STANDARD REAGENTS PVT
LTD
Formulation development
Preparation of Nano suspension by
Microprecipitation
Nanoedge is a combination of
microprecipitation techniques. The drug dissolved
in suitable solvent. In another one beaker stabilizer
and solvent which drug is insoluble. Drug and
stabilizer different ratios were taken as shown in
Table 6.
 Drug was dissolved in methanol
 Stabilizer dissolved in water
Table 3: Drug and Excipients ratio for Nanosuspesion
INGREDIENTS F1 F2 F3 F4 F5 F6 F7 F8 F9
Drug (mg) 500 500 500 500 500 500 500 500 500
PVP K 30 (mg) 250 500 750 - - - - - -
Polaxomer 188 (mg) - - - 250 500 750 - - -
Urea(mg) - - - - - - 250 500 750
Methanol(ml) 10 10 10 10 10 10 10 10 10
Water(ml) q.s q.s q.s q.s q.s q.s q.s q.s q.s
Characterisation of Nanosuspension
Drug content
Accurately weighed amount of each preparation
dissolved in required amount of methanol and
diluted suitably in pH 6.8 phosphate buffers. The
drug content was determined
spectrophotometrically at required wavelength.
Calculation was done using following formula:
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Determination of Nanosuspension particle
yield
The nanosuspension production yield was
calculated by gravimetry. Fixed volumes of
nanoparticles suspension were centrifuged
(15,000×g, 30 min, 15ºC) and sediments were
dried. The percentage yield was calculated as follows:
Micromeritic properties of
Nanosuspension
Bulk Density (Db)
It is the ratio of total mass of powder to the bulk
volume of powder. It was measured by pouring the
weight powder (passed through standard sieve #
20) into a measuring cylinder and initial weight
was noted. This initial volume is called the bulk
volume. From this the bulk density is calculated
according to the formula mentioned below. It is
expressed in g/ml and is given by,
Db = M/ Vb
Where, M is the mass of powder
Vb is the bulk volume of the powder.
Tapped Density (Dt)
It is the ratio of total mass of the powder to the
tapped volume of the powder. Volume was
measured by tapping the powder for 750 times and
the tapped volume was noted if the difference
between these two volumes is less than 2%. If it is
more than 2%, tapping is continued for 1250 times
and tapped volume was noted. Tapping was
continued until the difference between successive
volumes is less than 2 % (in a bulk density
apparatus). It is expressed in g/ml and is given by,
Dt = M / Vt
Where,
M is the mass of powder
Vt is the tapped volume of the powder.
Angle of Repose (Ө)
The friction forces in a loose powder can be
measured by the angle of repose (q). It is an
indicative of the flow properties of the powder. It is
defined as maximum angle possible between the
surface of the pile of powder and the horizontal
plane
Ө= tan-1
(h / r)
Where,
Ө is the angle of repose.
h is the height in cm
r is the radius in cm
The powder mixture was allowed to flow
through the funnel fixed to a stand at definite
height (h). The angle of repose was then calculated
by measuring the height and radius of the heap of
powder formed. Care was taken to see that the
powder particles slip and roll over each other
through the sides of the funnel. Relationship
between angle of repose and powder flow property.
Table 4: Angle of Repose as an Indication of Powder Flow Properties
Sr. No. Angle of Repose(0
) Type of Flow
1 <20 Excellent
2 20-30 Good
3 30-34 Passable
4 >34 Very Poor
Carr’s index (or) % compressibility
It indicates powder flow properties. It is expressed in percentage and is give by,
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Where,
Dt is the tapped density of the powder and
Db is the bulk density of the powder
Table 5: Relationship between % compressibility and flow ability
s no. % Compressibility Flow ability
1 5-12 Excellent
2 12-16 Good
3 18-21 Fair Passable
4 23-35 Poor
5 33-38 Very Poor
6 <40 Very Very Poor
Hausners ratio
Hausner ratio is an indirect index of ease of powder flow. It is calculated by the following formula.
Where, Dt is the tapped density, Db is the bulk
density.
Lower Hausners ratio (<1.25) indicates better flow
properties than higher ones (>1.25).
Invitro drug release studies
Dissolution test was carried out in USP rotating
basket dissolution apparatus. Employing the stirrer
speed at 100 rpm and Phosphate buffer pH 6.8 as
dissolution medium (900ml), at fixed time intervals
5 ml of the aliquot was withdrawn and same
quantity was replaced by fresh buffer. The
withdrawn samples were spectrophotometrically
analyzed at respective wavelength on Lab India
UV3000+.
The results of invitro release pro files obtained
for the BDDS formulations were fitted into four
models of data treatment as follows:
1. Cumulative percent drug released versus time
(zero order kinetic model).
2. Log cumulative percent drug remaining versus
time (first- order kinetic model).
Fourier transform Infrared spectroscopy
(FTIR)
Fourier transform infrared (FTIR) spectroscopy
was employed to characterize further the possible
interactions between the drug and the carrier in the
solid state on a FTIR spectrophotometer by the
ATR (attenuated total reflectance) technique. For
this technique ZnSe crystal was used to know the
wavelength of those drug and carriers. The spectra
were scanned over a frequency range 4000-550 cm-
1.
H) Differential Scanning Calorimetry (DSC)
The possibility of any interaction between the
drug and the carriers during preparation of solid
dispersion was assessed by carrying out thermal
analysis of drug and polymer alone as well as
physical mixture and solid dispersion using DSC.
DSC analysis was performed using Hitachi DSC
7020, on 5 to 15 mg samples. Samples were heated
in sealed aluminum pan at a rate of 10°C/min
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conducted over a temperature range of 30 to 350°C
under a nitrogen flow of 50 mL/min.
Scanning Electron Microscopy (SEM)
The surface morphology of the raw materials
and of the ternary systems was examined by means
of JSM‐6400 (Jeol, Japan) scanning electron
microscope. The samples were previously fixed
on a brass stub using double‐sided adhesive
tape and were then made electrically conductive
by coating with a thin layer of gold and palladium
alloy (180‐200 Å) using a fine coat ion sputter
(JEOL, fine coat ion sputter JFC‐1100). The
pictures were taken at an excitation voltage of
20 kV and magnification in the range of 118 to
245X.
Zeta potential
The stability of dispersion of Nanosuspension
was examined by using HORIBA SZ 100 Nano
partical series. The samples were taken by
Electrode cell (Carbon, 6mm) and measured at
25.1o
C. The picture was taken at electrode voltage
3.9V and conductivity 0.092 mS/cm.
Table no 7 : Stability behaviour by zeta potential
Zeta potential [mV] Stability behavior of the colloid
From 0 to ±5, Rapid coagulation or flocculation
From ±10 to ±30 Incipient instability
From ±30 to ±40 Moderate stability
From ±40 to ±60 Good stability
More than ±61 Excellent stability
Particle Size analysis
The Particle size of Nanosuspension was
examined by using HORIBA SZ 100 Nano partica
series.
Spray drying of Nanosuspension
Spray drying was carried out to get the dry nano
size powder. An optimized batch of aqueous
nanosuspension was transferred into nano size
powder by a lab spray dryer LU-222 lab ultima.
Spray dried powder was directly collected after the
process. In this process, the spray dryer was set to
the conditions given in following table.
Table no 8 : Spray dryer Parameter
Inlet Temperature 105-110o
C
Outlet Temperature 100o
C
Cool Temperature 40o
C
Aspirator flow rate 45 nm3
/hr
Feed pump flow rate 3 ml/min
Cycle time 70 min
RESULTS AND DISCUSSIONS
Melting point
Drug: Rosiglitazone
Limit: 153 - 1550
C
Observed: 1540
C
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Characterization of Nanosuspension
Table no 11: Drug content and % Yield of Nanosuspension
Formulation Code Drug content % Yield Solubility (mg/ml)
F1 91.75±0.46 86.62±0.48 0.78
F2 91.02±1.20 90.80±0.88 0.84
F3 93.51±0.66 93.68±0.90 0.94
F4 94.80±0.65 98.05±1.05 1.20
F5 95.83±0.82 98.67±1.17 1.26
F6 88.58±1.50 90.80±0.72 1.24
F7 89.33±1.17 89.24±1.45 0.68
F8 92.33±0.86 93.75±1.40 0.72
F9 91.16±1.32 92.46±0.70 0.85
Drug content
From the table 7.2, it was noted that increase
the concentration of stabilizer obtaining more drug
content. All the formulations drug content was
found to be in the range of 88.50±1.50 to
95.83±0.82.
Percentage Yield
From the table 7.2, it was noted that increase
the concentration of stabilizer obtaining more yield.
The entire formulations percentage yield was found
to be in the range of 86.62±0.48 to 98.67±1.17.
Solubility studies
From the table 7.2, it was noted that, all the
formulations solubility was found to be in the range
of 0.68 to 1.26 mg/ml.
Drug – Excipient compatibility studies
Fourier transform-infrared spectroscopy
Fig No: 12 FT-IR Spectrum of Rosiglitazone pure drug.
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Figure no 13: FT-IR Spectrum of Optimised
DSC studies
Figure no 14: DSC Spectrum of Rosiglitazone pure drug.
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Figure no 15: DSC Spectrum of Optimised
Particle size analysis
Transmission electron microscopy
The nanosuspension appeared dark and with
bright surroundings and a positive image (Fig. 2).
The droplet size ranged between 30 and 50nm and
was in agreement with the droplet size distribution
measured using photon correlation spectroscopy.
Fig 16: TEM image of Optimized formulation (F5)
Zeta sizer
The Size of the nanosuspension droplet size was found to be 32.1nm in diameter with the help of zeta sizer
with a zeta potential of -13.
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Resultssize(d.nm): %Intensity Width(d.nm)
Z- AVERAGE (D.NM): 32.1Peak1: 38.4 100 106.8
PdI: 0.168 Peak2:-- -- --
Intercept: 0.96 Peak3:-- -- --
Result quality:good
Resultssize(d.nm): %Intensity Width(d.nm)
Zeta Potential (mV): -13.61 Peak1: -13.1 98.5 16.4
Conductivity (mS/cm): 1.24 Peak2:-- -- --
Result quality: good Peak3:-- -- --
Accelerated stability studies
All the selected formulations were subjected to
a stability testing for three months as perICH norms
at a temperature of 40º ± 2º. All selected
formulations were analysed for the change in
appearance, pH or drug content by procedure stated
earlier.
Sr.no. Batches Months Appearance pH Drug content (%) Dissolution at 30mins
01 F5 0 Clear 6.8 99.95 98.52
1 Clear 6.8 98.60 98.20
2 Clear 6.7 97.00 98.20
3 Clear 6.6 96.20 97.62
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Invitro drug release studies
Table no 12: Dissolution data of NanosuspensionTime
(Min) F1 F2 F3 F4 F5 F6 F7 F8 F9 Pure
Drug
0 0 0 0 0 0 0 0 0 0 0
5 12.24 13.16 8.24 15.21 20.87 10.15 10.25 12.50 12.2 2.56
10 30.72 25.52 20.79 23.33 36.8 21.87 24.23 25.23 24.11 8.95
15 57.18 49.47 35.93 45.92 51.23 45.23 48.21 48.23 37.31 18.58
20 79.68 64.16 52.29 67.29 78.23 61.23 69.23 66.23 50.33 36.54
30 84.89 73.02 72.29 79.02 98.23 71.34 76.77 78.12 63.29 48.52
45 94.68 82.70 75.41 99.11 80.23 82.28 86.32 77.60 62.35
60 97.5 93.12 85.52 99.23 89.23 92.16 94.99 78.84
Figure no 17: invitro drug release studies for F1-F9
Figure no 18: Comparison of in vitro drug release studies with pure drug
0
20
40
60
80
100
120
0 20 40 60 80
%CDR
Time in mins
Dissolution profile F1
F2
F3
F4
F5
F6
F7
F8
F9
Pure Drug
0
20
40
60
80
100
120
0 20 40 60 80
%CDR
Time in mins
F5 Vs Pure drug
F5
Pure Drug
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From the dissolution studies, it was evident that
the formulations prepared with PVP K30 were
shown good drug release at 60min in concentration
of 250mg. Increase the concentration of stabilizer
above 250mg retarded the release of drug [8].
Formulations prepared with Polaxomer
188 were shown good drug release at 30 min in the
concentration of 500 mg of stabilizer. Among all
formulations F5 formulation was considered as
optimized formulation which was shown maximum
drug release at 30 min [9]
CONCLUSION
Finally, it can be concluded from the results of
present study that Nanosuspension improve the
solubility, and improve the site specificity of the
drug Rosiglitazone. Nanosuspension creates a new
opportunity for the low soluble drugs [10-11]. The
obtained nanosuspension was carried out for the
following characterization:
Drug content
From the table 7 it was noted that increase the
concentration of stabilizer obtaining more drug
content.All formulations drug content was found to
be in the range of 88.50+1.50to 95.83
Solubilitiy studies
From the table 7 it was noted that, All
formulations solubility was found to be in the range
of 0.68 to 1.28mg/ml.
Percentage Yield
From the table 7 it was noted that increase the
concentration of stabilizer obtaining more yield.
The entire formulations percentage yield was found
to be in the range of 86.62+98.67.
Dissolution studies
The formulations prepared with PVPK30 were
shown good drug release at 30min in concentration
of 1000mg.Increase the concentration of stabilizer
above 1000mg retards the release of drug.
Drug and Excipient Compatibility Studies
These studies were carried out using FTIR.
There is good computability were found between
drug and excipients.
TEM Studies
Optimized formulation has taken for TEM
studies. It has shown that nano suspension particle
size was ranged between 30 to 50 nm [12].
Zeta potential
Zeta potential studies were revealed that good
stability in dispersion of optimized nano suspension
[13].
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[13]. N.A.M. Deecaraman, C.Rani, Mohanraj KP, Kumar KV, preparation and solid state characterization of
atorvastatin nanosuspensions for enhanced solubility and dissolution, International Journal of PharmTech
Research, 1, 2009,1725-1730.Patel DJ, Patelj K.

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Formulation and evaluation of rosiglitazone nanosuspension

  • 1. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~29~ Available online at www.icjpir.com ISSN: 2349-5448 Intercontinental journal of pharmaceutical Investigations and Research ICJPIR |Volume 4 | Issue 1 | Jan – Mar- 2017 Research Article Formulation and evaluation of Rosiglitazone nanosuspension K.Hemalatha, S.Rajashekar CMR of Pharmacy, Kandlakoya Hyderabad, Telangana Corresponding Author: K.Hemalatha Email: hemasweety.latha903@gmail.com ABSTRACT The main aim of this study is to formulate and evaluate Rosiglitazone Nano suspension. Nano suspensions are colloidal dispersion of Nano sized drug particles stabilized by surfactants. They can also be defined as a biphasic system consisting of pure drug particles dispersed in an aqueous vehicle in which the diameter of the suspended particle is less than 1micro meter in size. Rosiglitazone is an oral rapid and short –acting anti-diabetic drug from the sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enter hepatic circulation. Rosiglitazone Nano suspension was prepared by precipitation technique. After preparation of Nano suspension various characterization studies were done such as drug content, %yield, FTIR, DSC, TEM, and Invitro drug release.PVPK30,polaxomer are used as stabilizers. From the dissolution study F4 formulation which containts PVPK30 as stabilizer was considered as optimized formulation. It showed maximum drug release at 30min.FTIR and DSC studies revealed that good stability in dispersion. INTRODUCTION Oral drug delivery system Oral dosage form is the physical form of a dose of a chemical compound used as a drug or medication intended for administration or consumption by oral route. Oral drug delivery is the most desirable and preferred method of administering therapeutic agents for their systemic effects. In addition, the oral medication is generally considered as the first avenue investigated in the discovery and development of new drug entities, pharmaceutical formulations, mainly because of patient acceptance and convenience in administration. Of drugs that are administered orally, solid dosage forms represent the preferred class of product. Advantages  Oral route of drug administration have wide acceptance up to 50-60% of total dosage forms  Ease of administration  Solid dosage forms represent unit dosage forms in which one usual dose of the drug has been accurately placed  Self-medication  Avoidance of pain  Patient compliance
  • 2. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~30~ Disadvantages:  Action of drugs is slower  Unpalatable drugs are difficult  May cause nausea and vomiting Importance of drug solubility Solubility is one of the important parameter in Biopharmaceutical classification system (BCS), and dissolution rate is the most essential factor controlling the bioavailability of drugs. Poorly water soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as generic development. A compound with solubility of less than 1 part per 10,000 part of water is categorized as poorly water soluble drug (sanjeev K, et al. 2009) [1]. Approaches for enhancement of solubility and dissolution rate Solubility behavior of a drug is one of the key determinants of its oral bioavailability. Noyes- Whitney equation provides some hints as to how the dissolution rate of even very poorly soluble compounds might be improved to minimize the limitations to oral availability. dc/dt = AD ( Cs-C )/h Where, dC/dt = rate of dissolution A = surface area available for dissolution D =diffusion coefficient of the compound Cs= solubility of the compound in the dissolution medium C =concentration of drug in the medium at time t h =thickness of the diffusion boundary layer adjacent to the surface of the dissolving compound. To increase the dissolution rate from equation the following approaches are available. 1. To increases the surface area available for dissolution by  Decreasing the particle size of drug.  Optimizing the wetting characteristics of compound surface. 2. To decrease the boundary layer thickness. 3. Ensure sink condition for dissolution. 4. Improving apparent solubility of drug under physiologically relevant conditions. Methods for enhancement of bioavailability: (Pinnamaneni S, et al. 2002) [2] There are numerous techniques to enhance bioavailability, which involves: Physical modification Physical modification often aims to increase the surface area, solubility and wet ability of the powder particles and is therefore focused on particle size reduction or generation of amorphous states. The various approaches under this method are: i. Particle size reduction:  Micronization  Nanosuspension ii. Modifications of the crystal habit:  Polymorphs.  Pseudo polymorphs (including solvates) iii. Complexation / solubilization:  Use of cyclodextrines  Use of surfactants iv. Drug dispersion in carriers:  Solid dispersions  Eutectic mixtures  Solid solutions Chemical modification Chemical modification aim at altering the drug chemically by various methods in order to produce a water soluble compound. The widely used approaches under this category are:  Formation of soluble prodrugs  Formation of salts of the compound  Preparation of covalent polymer drug conjugates. Nanosuspension Nanosuspension is favoured for compounds that are insoluble in water (but are soluble in oil) with high log P value, high melting point and high doses. Nanosuspension technology can also be used for drugs which are insoluble in both water and organic solvents. Hydrophobic drugs such as Atorvastatin, 13 Famotidine, 14 Simvastatin, 15 Revaprazan, 16 Aceclofenac, 17 are formulated as Nanosuspension. Nanosuspensions are colloidal dispersions of nanosized drug particles stabilized by surfactants. They can also be defined as a biphasic system consisting of pure drug particles dispersed in an aqueous vehicle in which the diameter of the suspended particle is less than 1µm
  • 3. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~31~ in size. The Nanosuspensions can also be lyophilized or spray dried and the nanoparticles of a Nanosuspension can also be incorporated in a solid matrix.( Banavath H, et al. 2010) [3] Nano is a Greek word, which means „dwarf‟. Nano means it is the factor of 10-9 or one billionth. Some comparisons of nanoscale are given below, 0.1 nm = Diameter of one Hydrogen atom. 2.5 nm = Width of a DNA molecule 1micron = 1000 nm. 1 nm = 10-9 m = 10-7 cm = 10-6 mm. Micron = 10-6 m= 10-4 cm = 10-3 mm 4. For a long duration of time micronization of poorly soluble drugs by colloid mills or jet mills was preferred. The overall particle size distribution ranges from 0.1µm to approximately 25µm, only negligible amount being below 1µm in the nanometer range. Rationale for nanosuspension  Preparing nano suspensions is preferred for the compounds that are insoluble in water (but are soluble in oil) with high log P value.  Conventionally the drugs that are insoluble in water but soluble in oil phase system are formulated in liposome, emulsion systems but these lipidic  Formulation approaches are not applicable to all drugs. In these cases nano suspensions are preferred.  In case of drugs that are insoluble in both water and in organic media instead of using lipidic systems Nano suspensions are used as a formulation approach.  Nano suspension formulation approach is most suitable for the compounds with high log P value, high melting point and high dose.(Mohanty S, et al.2010) [4] Benefits of nanosuspension technology for poorly soluble drugs  Reduced particle size, increased drug dissolution rate, increased rate and extent of absorption, increased bioavailability of drug, area under plasma versus time curve, onset time, peak drug level, reduced variability, reduced fed/fasted effects.  Nanosuspensions can be used for compounds that are water insoluble but which are soluble in oil. On the other hand, Nanosuspensions can be used in contrast with lipidic systems, successfully formulate compounds that are insoluble in both water and oils.  Nanoparticles can adhere to the gastrointestinal mucosa, prolonging the contact time of the drug and thereby enhancing its absorption.  A pronounced advantage of Nanosuspension is that there are many administration routes for Nanosuspensions, such as oral, parenteral, pulmonary, dermal and ocular.  Nanosuspension of nanoparticles (NPs) offers various advantages over conventional ocular dosage forms, including reduction in the amount of dose, maintenance of drug release over a prolonged period of time, reduction in systemic toxicity of drug, enhanced drug absorption due to longer residence time of nanoparticles on the corneal surface, higher drug concentrations in the infected tissue, suitability for poorly water- soluble drugs and smaller particles are better tolerated by patients than larger particles, therefore nanoparticles may represent auspicious drug carriers for ophthalmic applications.  Nanosuspension has low incidence of side effects by the excipients.  Nanosuspensions overcome delivery issues for the compounds by obviating the need to dissolve them, and by maintaining the drug in a preferred crystalline state of size sufficiently small for pharmaceutical acceptability.  Increased resistance to hydrolysis and oxidation, increased physical stability to settling.  Reduced administration volumes; essential for intramuscular, subcutaneous, ophthalmic use.  Finally, Nanosuspensions can provide the passive targeting (.Nagare SK,et al.2012) [5]
  • 4. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~32~ PREPARATION OF NANO SUSPENSION Figure no 1: Approaches for Preparation of Nano suspension Precipitation method Precipitation method is a general method used to prepare submicron particles of poorly soluble drugs. [Matteucci ME, et al.2007] [7] In this method, drug is dissolved in solvent and then solution is mixed with solvent to which drug is insoluble in the presence of surfactant. Rapid addition of solution to such solvent (generally water) leads to rapid supersaturation of drug in the solution, and formation of ultrafine amorphous or crystalline drug. This method involves nuclei formation and crystal growth which are mainly dependent on temperature. High nucleation rate and low crystal growth rate are primary requirements for preparing a stable suspension with minimum particle size. [Bodmeier R, et al.1998] [6] High-pressure homogenization This technique involve the following three steps: First, drug powders are dispersed in a stabilizer solution to form pre suspension; after that, pre suspension is homogenized by high pressure homogenizer at a low pressure sometimes for pre milling; and finally homogenized at a high pressure for 10 to 25 cycles until the nano suspension Figure no 2: High pressure homogenization
  • 5. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~33~ MATERIALS AND METHODS Materials The following materials available were used as supplied by the manufacturer without further purification or investigation Table no 2: list of materials used in formulation S.NO INGREDIENTS SPECIFICATION RATIONALE SOURCE 1 Rosiglitazone USP API CHANDRA LABS 2 PVP USP polymer STANDARD REAGENTS PVT LTD 3 UREA USP polymer STANDARD REAGENTS PVT LTD 4 Polaxomer USP polymer STANDARD REAGENTS PVT LTD 5 Potassium dihydrogen phosphate USP Buffer STANDARD REAGENTS PVT LTD 6 HCL USP STANDARD REAGENTS PVT LTD 7 Sodium hydroxide pellets USP STANDARD REAGENTS PVT LTD Formulation development Preparation of Nano suspension by Microprecipitation Nanoedge is a combination of microprecipitation techniques. The drug dissolved in suitable solvent. In another one beaker stabilizer and solvent which drug is insoluble. Drug and stabilizer different ratios were taken as shown in Table 6.  Drug was dissolved in methanol  Stabilizer dissolved in water Table 3: Drug and Excipients ratio for Nanosuspesion INGREDIENTS F1 F2 F3 F4 F5 F6 F7 F8 F9 Drug (mg) 500 500 500 500 500 500 500 500 500 PVP K 30 (mg) 250 500 750 - - - - - - Polaxomer 188 (mg) - - - 250 500 750 - - - Urea(mg) - - - - - - 250 500 750 Methanol(ml) 10 10 10 10 10 10 10 10 10 Water(ml) q.s q.s q.s q.s q.s q.s q.s q.s q.s Characterisation of Nanosuspension Drug content Accurately weighed amount of each preparation dissolved in required amount of methanol and diluted suitably in pH 6.8 phosphate buffers. The drug content was determined spectrophotometrically at required wavelength. Calculation was done using following formula:
  • 6. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~34~ Determination of Nanosuspension particle yield The nanosuspension production yield was calculated by gravimetry. Fixed volumes of nanoparticles suspension were centrifuged (15,000×g, 30 min, 15ºC) and sediments were dried. The percentage yield was calculated as follows: Micromeritic properties of Nanosuspension Bulk Density (Db) It is the ratio of total mass of powder to the bulk volume of powder. It was measured by pouring the weight powder (passed through standard sieve # 20) into a measuring cylinder and initial weight was noted. This initial volume is called the bulk volume. From this the bulk density is calculated according to the formula mentioned below. It is expressed in g/ml and is given by, Db = M/ Vb Where, M is the mass of powder Vb is the bulk volume of the powder. Tapped Density (Dt) It is the ratio of total mass of the powder to the tapped volume of the powder. Volume was measured by tapping the powder for 750 times and the tapped volume was noted if the difference between these two volumes is less than 2%. If it is more than 2%, tapping is continued for 1250 times and tapped volume was noted. Tapping was continued until the difference between successive volumes is less than 2 % (in a bulk density apparatus). It is expressed in g/ml and is given by, Dt = M / Vt Where, M is the mass of powder Vt is the tapped volume of the powder. Angle of Repose (Ө) The friction forces in a loose powder can be measured by the angle of repose (q). It is an indicative of the flow properties of the powder. It is defined as maximum angle possible between the surface of the pile of powder and the horizontal plane Ө= tan-1 (h / r) Where, Ө is the angle of repose. h is the height in cm r is the radius in cm The powder mixture was allowed to flow through the funnel fixed to a stand at definite height (h). The angle of repose was then calculated by measuring the height and radius of the heap of powder formed. Care was taken to see that the powder particles slip and roll over each other through the sides of the funnel. Relationship between angle of repose and powder flow property. Table 4: Angle of Repose as an Indication of Powder Flow Properties Sr. No. Angle of Repose(0 ) Type of Flow 1 <20 Excellent 2 20-30 Good 3 30-34 Passable 4 >34 Very Poor Carr’s index (or) % compressibility It indicates powder flow properties. It is expressed in percentage and is give by,
  • 7. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~35~ Where, Dt is the tapped density of the powder and Db is the bulk density of the powder Table 5: Relationship between % compressibility and flow ability s no. % Compressibility Flow ability 1 5-12 Excellent 2 12-16 Good 3 18-21 Fair Passable 4 23-35 Poor 5 33-38 Very Poor 6 <40 Very Very Poor Hausners ratio Hausner ratio is an indirect index of ease of powder flow. It is calculated by the following formula. Where, Dt is the tapped density, Db is the bulk density. Lower Hausners ratio (<1.25) indicates better flow properties than higher ones (>1.25). Invitro drug release studies Dissolution test was carried out in USP rotating basket dissolution apparatus. Employing the stirrer speed at 100 rpm and Phosphate buffer pH 6.8 as dissolution medium (900ml), at fixed time intervals 5 ml of the aliquot was withdrawn and same quantity was replaced by fresh buffer. The withdrawn samples were spectrophotometrically analyzed at respective wavelength on Lab India UV3000+. The results of invitro release pro files obtained for the BDDS formulations were fitted into four models of data treatment as follows: 1. Cumulative percent drug released versus time (zero order kinetic model). 2. Log cumulative percent drug remaining versus time (first- order kinetic model). Fourier transform Infrared spectroscopy (FTIR) Fourier transform infrared (FTIR) spectroscopy was employed to characterize further the possible interactions between the drug and the carrier in the solid state on a FTIR spectrophotometer by the ATR (attenuated total reflectance) technique. For this technique ZnSe crystal was used to know the wavelength of those drug and carriers. The spectra were scanned over a frequency range 4000-550 cm- 1. H) Differential Scanning Calorimetry (DSC) The possibility of any interaction between the drug and the carriers during preparation of solid dispersion was assessed by carrying out thermal analysis of drug and polymer alone as well as physical mixture and solid dispersion using DSC. DSC analysis was performed using Hitachi DSC 7020, on 5 to 15 mg samples. Samples were heated in sealed aluminum pan at a rate of 10°C/min
  • 8. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~36~ conducted over a temperature range of 30 to 350°C under a nitrogen flow of 50 mL/min. Scanning Electron Microscopy (SEM) The surface morphology of the raw materials and of the ternary systems was examined by means of JSM‐6400 (Jeol, Japan) scanning electron microscope. The samples were previously fixed on a brass stub using double‐sided adhesive tape and were then made electrically conductive by coating with a thin layer of gold and palladium alloy (180‐200 Å) using a fine coat ion sputter (JEOL, fine coat ion sputter JFC‐1100). The pictures were taken at an excitation voltage of 20 kV and magnification in the range of 118 to 245X. Zeta potential The stability of dispersion of Nanosuspension was examined by using HORIBA SZ 100 Nano partical series. The samples were taken by Electrode cell (Carbon, 6mm) and measured at 25.1o C. The picture was taken at electrode voltage 3.9V and conductivity 0.092 mS/cm. Table no 7 : Stability behaviour by zeta potential Zeta potential [mV] Stability behavior of the colloid From 0 to ±5, Rapid coagulation or flocculation From ±10 to ±30 Incipient instability From ±30 to ±40 Moderate stability From ±40 to ±60 Good stability More than ±61 Excellent stability Particle Size analysis The Particle size of Nanosuspension was examined by using HORIBA SZ 100 Nano partica series. Spray drying of Nanosuspension Spray drying was carried out to get the dry nano size powder. An optimized batch of aqueous nanosuspension was transferred into nano size powder by a lab spray dryer LU-222 lab ultima. Spray dried powder was directly collected after the process. In this process, the spray dryer was set to the conditions given in following table. Table no 8 : Spray dryer Parameter Inlet Temperature 105-110o C Outlet Temperature 100o C Cool Temperature 40o C Aspirator flow rate 45 nm3 /hr Feed pump flow rate 3 ml/min Cycle time 70 min RESULTS AND DISCUSSIONS Melting point Drug: Rosiglitazone Limit: 153 - 1550 C Observed: 1540 C
  • 9. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~37~ Characterization of Nanosuspension Table no 11: Drug content and % Yield of Nanosuspension Formulation Code Drug content % Yield Solubility (mg/ml) F1 91.75±0.46 86.62±0.48 0.78 F2 91.02±1.20 90.80±0.88 0.84 F3 93.51±0.66 93.68±0.90 0.94 F4 94.80±0.65 98.05±1.05 1.20 F5 95.83±0.82 98.67±1.17 1.26 F6 88.58±1.50 90.80±0.72 1.24 F7 89.33±1.17 89.24±1.45 0.68 F8 92.33±0.86 93.75±1.40 0.72 F9 91.16±1.32 92.46±0.70 0.85 Drug content From the table 7.2, it was noted that increase the concentration of stabilizer obtaining more drug content. All the formulations drug content was found to be in the range of 88.50±1.50 to 95.83±0.82. Percentage Yield From the table 7.2, it was noted that increase the concentration of stabilizer obtaining more yield. The entire formulations percentage yield was found to be in the range of 86.62±0.48 to 98.67±1.17. Solubility studies From the table 7.2, it was noted that, all the formulations solubility was found to be in the range of 0.68 to 1.26 mg/ml. Drug – Excipient compatibility studies Fourier transform-infrared spectroscopy Fig No: 12 FT-IR Spectrum of Rosiglitazone pure drug.
  • 10. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~38~ Figure no 13: FT-IR Spectrum of Optimised DSC studies Figure no 14: DSC Spectrum of Rosiglitazone pure drug.
  • 11. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~39~ Figure no 15: DSC Spectrum of Optimised Particle size analysis Transmission electron microscopy The nanosuspension appeared dark and with bright surroundings and a positive image (Fig. 2). The droplet size ranged between 30 and 50nm and was in agreement with the droplet size distribution measured using photon correlation spectroscopy. Fig 16: TEM image of Optimized formulation (F5) Zeta sizer The Size of the nanosuspension droplet size was found to be 32.1nm in diameter with the help of zeta sizer with a zeta potential of -13.
  • 12. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~40~ Resultssize(d.nm): %Intensity Width(d.nm) Z- AVERAGE (D.NM): 32.1Peak1: 38.4 100 106.8 PdI: 0.168 Peak2:-- -- -- Intercept: 0.96 Peak3:-- -- -- Result quality:good Resultssize(d.nm): %Intensity Width(d.nm) Zeta Potential (mV): -13.61 Peak1: -13.1 98.5 16.4 Conductivity (mS/cm): 1.24 Peak2:-- -- -- Result quality: good Peak3:-- -- -- Accelerated stability studies All the selected formulations were subjected to a stability testing for three months as perICH norms at a temperature of 40º ± 2º. All selected formulations were analysed for the change in appearance, pH or drug content by procedure stated earlier. Sr.no. Batches Months Appearance pH Drug content (%) Dissolution at 30mins 01 F5 0 Clear 6.8 99.95 98.52 1 Clear 6.8 98.60 98.20 2 Clear 6.7 97.00 98.20 3 Clear 6.6 96.20 97.62
  • 13. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~41~ Invitro drug release studies Table no 12: Dissolution data of NanosuspensionTime (Min) F1 F2 F3 F4 F5 F6 F7 F8 F9 Pure Drug 0 0 0 0 0 0 0 0 0 0 0 5 12.24 13.16 8.24 15.21 20.87 10.15 10.25 12.50 12.2 2.56 10 30.72 25.52 20.79 23.33 36.8 21.87 24.23 25.23 24.11 8.95 15 57.18 49.47 35.93 45.92 51.23 45.23 48.21 48.23 37.31 18.58 20 79.68 64.16 52.29 67.29 78.23 61.23 69.23 66.23 50.33 36.54 30 84.89 73.02 72.29 79.02 98.23 71.34 76.77 78.12 63.29 48.52 45 94.68 82.70 75.41 99.11 80.23 82.28 86.32 77.60 62.35 60 97.5 93.12 85.52 99.23 89.23 92.16 94.99 78.84 Figure no 17: invitro drug release studies for F1-F9 Figure no 18: Comparison of in vitro drug release studies with pure drug 0 20 40 60 80 100 120 0 20 40 60 80 %CDR Time in mins Dissolution profile F1 F2 F3 F4 F5 F6 F7 F8 F9 Pure Drug 0 20 40 60 80 100 120 0 20 40 60 80 %CDR Time in mins F5 Vs Pure drug F5 Pure Drug
  • 14. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~42~ From the dissolution studies, it was evident that the formulations prepared with PVP K30 were shown good drug release at 60min in concentration of 250mg. Increase the concentration of stabilizer above 250mg retarded the release of drug [8]. Formulations prepared with Polaxomer 188 were shown good drug release at 30 min in the concentration of 500 mg of stabilizer. Among all formulations F5 formulation was considered as optimized formulation which was shown maximum drug release at 30 min [9] CONCLUSION Finally, it can be concluded from the results of present study that Nanosuspension improve the solubility, and improve the site specificity of the drug Rosiglitazone. Nanosuspension creates a new opportunity for the low soluble drugs [10-11]. The obtained nanosuspension was carried out for the following characterization: Drug content From the table 7 it was noted that increase the concentration of stabilizer obtaining more drug content.All formulations drug content was found to be in the range of 88.50+1.50to 95.83 Solubilitiy studies From the table 7 it was noted that, All formulations solubility was found to be in the range of 0.68 to 1.28mg/ml. Percentage Yield From the table 7 it was noted that increase the concentration of stabilizer obtaining more yield. The entire formulations percentage yield was found to be in the range of 86.62+98.67. Dissolution studies The formulations prepared with PVPK30 were shown good drug release at 30min in concentration of 1000mg.Increase the concentration of stabilizer above 1000mg retards the release of drug. Drug and Excipient Compatibility Studies These studies were carried out using FTIR. There is good computability were found between drug and excipients. TEM Studies Optimized formulation has taken for TEM studies. It has shown that nano suspension particle size was ranged between 30 to 50 nm [12]. Zeta potential Zeta potential studies were revealed that good stability in dispersion of optimized nano suspension [13]. REFERENCES [1]. Katteboinaa S, Drug nanocrystals: A novel formulation approach for poorly Soluble drugs, International journal of pharmtech research, 1(3), 2009, 682-694. [2]. Dineshkumar B, Nanosuspension Technology in DrugDelivery System, Nanoscience and Nanotechnology: An International Journal, 3(1), 2013, 1-3. [3]. Patel AP, A review on drug nanocrystal a carrier free drug delivery, IJRAP, 2(2), 2011, 448-458. [4]. Dhiman S, Nanosuspension: a recent approach for nano drug delivery system, International journal of current pharmaceutical research, 3, 2011, 96-101. [5]. Maravajhala V, Papishetty S, Bandlapalli S, Nanotechnology in development of drug delivery system. International Journal of Pharmaceutical Science and Research, 3(1), 2012, 84-96. [6]. Patel BP, A Review On Techniques Which Are Useful For Solubility Enhancement Of Poorly Water Soluble Drugs, International Journal For Research In Management And Pharmacy, 1, 2012, 56-70. [7]. Shukla M Enhanced Solubility Study Of Rosiglitazone Using Different Solubilization Techniques, International Journal Of Pharmacy and Pharmaceutical Sciences, 2, 2010, 46-48. [8]. Chaudhary A, Enhancement of solubilization and bioavailability of poorly soluble drugs by physical and chemical modifications: A recent review, Journal of Advanced Pharmacy Education & Research, 2 (1), 2012, 32-67.
  • 15. Hemalatha K et al, ICJPIR 2017, 4(1), 29-43 www.icjpir.com ~43~ [9]. Kapadiya N, Hydrotropy: A Promising Tool for Solubility Enhancement: A Review. International Journal of Drug Development & Research, 3, 2011, 26-33. [10]. Thorat YS, Solubility Enhancement Techniques: A Review On Conventional And Novel Approaches, IJPSR, 2(10), 2011, 2501-2513. [11]. Sharma D, Solubility Enhancement – Eminent Role in Poorly Soluble Drugs, “Research J. Pharm. and Tech”, 2(2), 2009, 220-224. [12]. Jain S, Solubility Enhancement by Solvent Deposition Technique: An Overview, Asian Journal Of Pharmaceutical And Clinical Research, 5(4), 2012, 15-19. [13]. N.A.M. Deecaraman, C.Rani, Mohanraj KP, Kumar KV, preparation and solid state characterization of atorvastatin nanosuspensions for enhanced solubility and dissolution, International Journal of PharmTech Research, 1, 2009,1725-1730.Patel DJ, Patelj K.