Cardiac Output, Venous Return, and Their Regulation
PPT 10.pptx
1. DEVELOPMENTAND IN-VITRO EVALUATION OF FUSIDIC ACID
CONTAINING NIOSOMAL GEL FOR WOUND TREATMENT
A Thesis Submitted
in Partial Fulfillment of the Requirements for the Degree of
MASTER OF PHARMACY
in
PHARMACEUTICS
by
BHARTENDU KUMAR SHUKLA
(Enrollment No.: 062175047166)
Under the Supervision of
Dr. VIVEK (Associate Professor)
IIMT College of Pharmacy
to the
FACULTY OF PHARMACY
DR. APJ ABDUL KALAM TECHNICAL UNIVERSITY
LUCKNOW
(Formerly Uttar Pradesh Technical University) LUCKNOW
July’2021
2. Introduction
Drug Profile
Aim and Objective
Plan of work
Experimental Work
Results and Conclusion
Contents
Contents
3. Niosomes are nano-sized vesicles produced by the absorption of
artificial surfactants (Non-ionic) by medium in the form or
absence of cholesterol and active vectors both to amphiphilic
and lipophilic drugs
The sizes vary from 10 to 1000 nm
Various modes of administration of niosomal formulations, such
as peroral, intravenous, transdermal, intramuscular, are
available.
It is very cost effective and chemically most stable to
phospholipid
Introduction
5. Noisome as a brain targeted vasoactive intestinal peptide (VIP) delivery
system
Niosomes as a Drug Carriers
Niosomal immunological activity
Transdermal-delivery of niosomal drugs
Delivery of peptide drugs
Targeting of bioactive agents
Ophthalmic drug delivery
Diagnostic imaging with niosomes
Application of Niosomes
6. Drug Profile
Fusidic Acid :
Fusidic acid obtained from the broth fermented fungus Fusidiumcoccineum,
demonstrated antifungal activity by inhibiting protein synthesis of fungus, an EC
inhibitor (pantothenate kinase) and a metabolite of E. coli.
Appearance: Solid with white Colour powder.
Solubility: DMSO, Ethanolic methyl formamide
Molecular weight: 516.7g/mol
Melting point: 191.5 0c
Pka: 5.34
7. Gel formulations offer quick release of drugs relative to creams and lotions.
Fusidic acid is usually administered in viscous formulations such as
creams.
Niosomes is chosen as a vesicular system to overcome the unwanted
effects and to optimize its beneficial attributes
Niosomes are expected to offer achieve better penetration of drug with
minimum undesired side effects when implemented in topical formulation
To improve permeation of drug.
Targeted & Controlled drug delivery.
To improve the targeting and bioavailability of drugs.
Increase of drug residence time.
Aim and Objective:
8. Literature review
Selection of drug and Excipients:
Drug: Fusidic Acid
Excipients: Cholesterol , SPAN-80
Pre-formulation studies:
Organoleptic properties
Melting point determination
High performance liquid chromatography (HPLC) analysis
Solubility study in different solvents
Plan of Work
9. Plan of Work
Preparations of Niosomes of Fusidic Acid
Niosomal gel of Fusidic Acid: Niosomal Gel Evaluation
Optical Microscopy
Surface morphology, size of particle and Zeta potential
Efficiency of entrapment
• Physical-appearance
• PH
• Uniformity of drug-content
• Activation of in-vitro drug
• The kinetics of product release
10. Preparation of Niosomes of fusidic acid :
Niosomes have been formulated using the systemology of hydration by thin film. The non-
ionic-surfactant & cholesterol at different specified molar-ratios (1:1, 2:1, 3:1; Surfactant:
Cholesterol M.R) were dispersed in the solvent mixture of methanol & chloroform (1:2v /
v) together with the addition of Fusidic acid weighed as a dose.
Formulation Code Molar Ratio (Chl:
Span 80)
Drug (mg) Cholesterol
(mg)
Span 80 (mg)
F1 1:1 250 38.6 42.8
F2 1:2 250 38.6 85.7
F3 1:3 250 38.6 128.5
F4 1:4 250 38.6 171.2
F5 1:5 250 38.6 214
F6 1:8 250 38.6 342.4
F7 1:10 250 38.6 428
Experimental work :
11. 1. Organoleptic-properties
The organoleptic-properties of Fusidic Acid was found to be as per I.P.
monograph. The Organoleptic properties of Fusidic Acid were found is given in
table
Sr. No. Properties Inferences
1. Colour White
2. Odour Odourless
3. Form Crystalline
4. Taste Bitter
Melting point of Fusidic Acid was determined using the capillary tube system and was
found to be quite similar to the reported melting point as shown in table
Drug Reference M.P. Observed M.P.
Fusidic Acid 191-194°C 192.25±0.0150C
Result and discussion
2. Melting point
12. Result and discussion
3. Solubility of fusidic acid in different solvents
Drug solubility in various solvents was performed to screen the components to be used
for the development of formulations. Solubility is mentioned as follow in table
Sr.no Solvent system Solubility of drug (mg/ml)
01. Water 0.081 ± 0.001
02. Buffer pH 7.4 1.517 ± 0.000
03. Chloroform 2.173 ± 0.010
04. Acetone 6.677 ± 0.009
05. Methanol 9.627 ± 0.007
06. Ethanol 9.740 ± 0.005
07. DMF 14.073 ± 0.004
08. DMSO 14.329 ± 0.006
Discussion: From the above data, it is clearly seen that Fusidic Acid is highly soluble in
ethanol, methanol, water followed by acetone
13. Partition coefficient is used to determine the lipophilicity of drug substances. It is
determined using water and n-octanol. Log p value indicates the lipophilicity or
hydrophilicity nature of the compounds. Log p value greater than one indicates the
lipophilic nature of drug while the Log p value less then one indicates the hydrophilic
nature of the drugs.
Discussion: The partition coefficient of Fusidic Acid in n-octanol: water was found to
be 5.344 ± 0.004; this indicates that the drug is lipophilic in nature (table 7.7) which is
similar to the literature
Partition coefficient of drug Solvent system Log P Values Reference
Fusidic Acid n-octanol: water 5.209 ± 0.004 5.35
Result and discussion
4. Partition-coefficient determination of drug
14. S.No. Formulation Code pH Appearance of Gel
1 N1 - Gel not formed
2 N2 7.23±0.025 Sticky Gel Formed
3 N3 7.34±0.02 Uniform Gel Formed
Discussion: The pH values of formulations N2 & N3 were to be 7.236±0.025 and
7.34±0.02 respectively as shown in above table
S.No. Formulation Code % Drug Content
1 N2 76.21±0.065
2 N3 87.84±0.051
Discussion: The drug content of niosomal gels was found to be 87.84±0.051 &
97.45±0.065 respectively. The percentage drug content of all formulations was found to
be satisfactory. Hence, the system adopted for gel formulations was found to be suitable.
Formulation N3 is selected for further release study.
Result and discussion
5. pH of FA Niosomal Gel
6. %Drug content of niosomal gel
15. Percentage Drug Entrapment of all formulation was given in a table
S.No. Formulation Code Percentage drug entrapment
01. F3 13.16±0.065
02. F4 27.01±0.051
03. F5 48.07±0.106
04. F6 59.28±0.013
05. F7 67.33±0.014
06. F8 78.84±0.022
07. F9 68.29±0.026
Result and discussion
7. Entrapment Efficiency percentage
8. In vitro release kinetic :
Formulation Name Zero-order First-order Higuchi Peppas
R2 K0 R2 K0 R2 K0 R2 K0
F9 0.736 3.103 0.840 -0.025 0.916 18.811 0.918 0.805
16. The in-vitro drug release of Formulation N3 and Pure drug was given in a table
Time (hr) % Drug release of pure drug
Suspension
% Drug release of N3 formulation
0 0 0
15 mins 22.45±0.830 3.09±0.271
30 mins 55.81±0.543 7.62±0.271
1 hr 68.08±2.057 10.10±0.270
2 hr 81.44±0.543 22.26±0.269
3 hr 88.20±0.543 30.19±0.156
4 hr 91.33±0.741 39.72±0.156
5 hr 91.85±0.258 48.01±0.271
6 hr 93.21±0.264 55.11±0.156
Result and discussion
9. In vitro release study :
17. 10. HPLC analysis of fusidic acid
Result and discussion
Calibration curve of Fusidic Acid
Sr-
No.
Concn.
(µg/ml)
Area under Curve
01. 10 49391.67 ± 12.096
02. 20 104428 ± 11.357
03. 30 141912 ± 12.124
04. 40 188793.3 ± 16.802
05. 50 240351.7 ± 11.590
06. 60 288107.7 ± 12.220
y = 4709.2x + 4007.6
R² = 0.9982
0
50000
100000
150000
200000
250000
300000
350000
0 10 20 30 40 50 60 70
Area
under
curve
Cocentration(mg/ml)
Absorption maxima (λ max) of Fusidic Acid in Methanol.
Name of drug Absorption maxima (λ max)
Observed Reference
Fusidic Acid 235 235
19. Statistical parameters Results
λmax 235 nm
Flow-Rate 2 ml per min
Retention-Time 11.44
Regression equation (y = mx + c) y = 4709.2x + 4007.5
Slope (b) 4709.2
Intercept (C) 4007.5
Correlation coefficient (r2) 0.998
Discussion: - From the above data it was revealed that Fusidic acid displayed strong
linearity with R2 = 0.998 and equation y = 4709.2x + 4007.5.
Result and discussion
Result of regression analysis of UV system
20. FTIR Studies:
Result and discussion
Reported
(cm-1)
Observed(
cm-1)
Characteristics Peaks
3346 3342.08 O – H stretching
1686 1686.01 C = O symmetrical stretching
970 975.15 C = C – H Double bond planar
deformation
850 854.25 C = C – C Double bond planar
deformation
607 607.04 C = C – O Double bond planar
deformation
FTIR interpretation
Discussion: The Fusidic Acid FTIR spectra are shown in above Figure and Table. The major Infra-
red absorption peaks of Fusidic Acid were found at 3342.08 cm-1 (O – H stretching), 1686.01 cm-
1 (symmetrical stretching of the functional group C = O), 975.15 cm-1 (planar deformation of dual
bond C = C – H), 854.25 cm-1 (planar deformation of dual bond C = C – C), 607.04 cm-1 (planar
deformation of dual bond C = C – O) were all observed in the Fusidic Acid spectra. Such observed
principal peaks confirmed the Fusidic Acid 's purity and authenticity.
11. FTIR analysis of fusidic acid
21. Result and discussion
12. FTIR analysis of formulation of fusidic acid Niosomal gel
FTIR of formulation (N3)
As shown in the spectrum of
formulation , peaks were obtained at
2917.30 cm–1 (aliphatic C–H
vibrations), 1738.33 cm–1 (N–H
stretching), 1172.36 cm–1 (C=S
stretching) and 1098.33 cm–1 (C–O
stretch of alcohols secondary).
Discussion: The FTIR spectrum of final formulation (N3) indicate that characteristic peak
of Fusidic acid was not visible in the niosomes gel spectra which indicates that drug was
completely encapsulate in the niosomal gel.
22. The melting point of Fusidic acid was found to be 192.25±0.0150C after
physicochemical examination.
Maximum absorption in methanol on HPLC analysis was found to be 235 nm
Fusidic acid partition coefficient in n-octanol: water was found to be 5.209±0.004, this
suggests lipophilic existence of the substance.
Particle size of prepared niosomes was found to be Percentage efficiency of trapping
was found in the range from 13.16±0.065 to 78.84±0.022
The pH of niosomal gel prepared was found to be 7.23±0.025 7.34±0.02.
Summary And Conclusion
23. Summary And Conclusion
In all formulations with gel formation, a percentage of the drug content was obtained
from 76.21±0.065 to 87.84±0.051
In vitro data showed that pure drug release within 6 hours showed 93 %
In 24 hours, the drug release from the niosomal gel prepared in Formulation F8
exceeded 72.95±0.271 percent
Span 80 can be regarded as an important carrier for developing a framework for
transdermal drug delivery