Nanoparticle method and evaluation test

1. Sachin Suryawanshi
M.Pharmacy (Pharmaceutics)
Roll No. 112
1
NANOPARTICLES

2. Contents:
2
 Introduction
 Application
 Advantages and Disadvantages
 Ideal characteristics
 Methods of Preparation
 Characterization
 Evaluation
 Recent Advances
 Commercial product of Nanoparticle
 Applications

3. INTRODUCTION
3
 Nanoparticles are sub-nanosized colloidal structures
composed of synthetic or semi-synthetic polymers.
 Its size ranges from 1-100nm.
 Types of Nanoparticles
1.Nanospheres
2.Nanocapsule

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 Nanospheres - Matrix systems.
 Nanocapsules - which are Reservoir systems
composed of a polymer membrane surrounding an oily
or aqueous core.

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Advantages
Site specific
targetting
More uniform
effect of the drug
Reduction in the
frequency of the
dosages
Better drug
utilization and less
side effects
Various routes of
administration

7. DISADVANTAGES :
7
 High cost
 Productivity more difficult
 Reduced ability to adjust the dose
 Highly sophisticated technology
 Requires skills to manufacture
 Difficult to maintain stability of dosage form.

8. Polymers Used in Preparation of Nanoparticles
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Polymers
SYNTHETIC HYDROPHOBICNATURAL HYDROPHILIC
Eg: Proteins
Polysacchrides
Eg: Polyesters
Polystyrene

9. IDEAL CHARACTERISTICS :
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 It should be biochemical inert , non toxic and non-
immunogenic.
 It should be stable both physically and chemically in
Invivo & invitro conditions.
 Restrict drug distribution to non-target cells or tissues or
organs & should have uniform distribution.
 Controllable & Predicate rate of drug release.

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 Drug release should not effect drug action
 Specific Therapeutic amount of drug release must be
possessed
 Carriers used must be biodegradable or readily
eliminated from the body without any problem and no
carrier induced modulation in disease state.
 The preparation of the delivery system should be easy or
reasonable
 simple, reproducible & cost effective.

11. Methods of preparation:
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A : Amphiphilic Macromolecules Cross Linking
1)Heat crosslinking.
2)chemical crosslinking.
B : Polymerization Methods
1) Emulsion polymerization
2) Dispersion polymerization
3) Interfacial condensation polymerization
4) Interfacial complexation
C : Polymer precipitation methods
1) Solvent evaporation method
2) Solvent displacement
3) Salting out

12. Aqueou
s
protein
Aqueous
phase,
Distilled
water,
stabilizer
O/W emulsion
Dilution with preheated oil (100oC)
(Heat cross-linking)
Or Addition of crosslinking agent
(Chemical cross-linking)
Centrifugation and isolation of
nanoparticles
Emulsification using high-
pressure homogenization or high
frequency sonication
Surfactant
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A : Molecular crosslinking in emulsion

13. B : Polymerization Methods
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Emulsion polymerization :
It consists of
a) Micellar nucleation and polymerization :
Monomer is insoluble in continuous phase.(O/W phase)
Aqueous phase
b)Homogenous nucleation and
polymerization :
Monomer is soluble in continuous phase.(W/O phase)
Organic phase.

14. Monomer bearing Nucleated micelle Stabilized polymeric micelle
nanospheres
Catalyst
Monomer dropletCatalystDrug Monomer
monomer supply
(micelle) (nanospheres)
Micellar nucleation and polymerization

15. Homogenous nucleation and polymerization
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16. Dispersion polymerization:
16

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(Acrylamide or Methyl
methacrylate) Monomer is
dissolved
in an aqueous medium
Further, By chemical initiation
(ammonium or potassium per oxo
disulphate)
Heated to above 65˚C
Oligomers aggregate &
precipitates
Isolation of Nanospheres

18. Interfacial polymer condensation
18
Core + Drug
Polymer
phase
Non solvent which
precipitates out
polymer from either
of phases
Core dispersed
polymer phase (O/W
emulsion)
Nancapsules 30-
300nm

19. C : Polymer Precipitation Methods:
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The polymer precipitation occurs as a consequence of
solvent evaporation which can be brought about by
increasing solubility of organic solvent in external
medium by adding alcohol (Eg. Isopropanolol)
They are 3 types
1. Solvent evaporation method
2. Solvent displacement
3. Salting out

20. Solvent Evaporation Method
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21. Solvent Displacement Method
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Organic phase,
organic solvent,
polymer+drug
Organic phase,
Polarsolvent,
Oil+polymer+drug

22. Salting out of Polymer
22
stirring
Nanoparticles

23. Evaluation of Nanoparticles :
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1. Particle size :
 Photon correlation spectroscopy(PCS) : For smaller
particle.
 Laser diffractrometry : For larger particle.
 Electron microscopy (EM) : Required coating of conductive
material such as gold & limited to dry sample.
 Transmission electron microscopy (TEM) : Easier method
& Permits differntiation among nanocapsule & nanoparticle .
 Atomic force microscope
 Laser force microscope
 Scanning electron microscope
High resolution
microscope

24. Photon correlation spectroscopy(PCS)
: For smaller
particle is also known as Dynamic light scattering
(DLS)
24 Ref. www.malvernpananitical.com/en/learn/knowldge-centre

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2.Density :
Helium or air using a gas pycnometer
Density gradiant centrifugation
3. Molecular weight :
Gel permeation chromatography using refractive index
detector.
4. Structure & Crystallinity :
X-ray diffraction Thermoanalytical method such as,
1) Differential scanning calorimetry
2) Differential thermal analysis
3) Thermogravimetry
5. Surface charge:
Surface charge of particle can be determined by measuring
particle velocity in electrical field.

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6. Invitro release :
Diffusion cell
Media used : phosphate buffer
7. Nanoparticle yield :
8. Drug entrapment efficiency :

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COMPANY TRADE
NAME
COMPOSITIO
N
INDICATION ROUTE
Enzon Abelect Liposomal
Amphotericin
B
Fungal
Infection
IV
Berna Biotech Epaxal Liposomal
IRIV Vaccine
Hepatitis A IM
Novavax Estrasorb Micellular
estradiol
Menopausal
Therapy
Topical
Nektar,
Hoffmann-La
Roche
Pegasys PEG-
ainterferon 2a
Hepatitis B,
Hepatitis C
Subcutaneous
Elan,Merck Emend Nanocrystallin
e aprepitant
Antiemetic Oral
Genzyme Renagel Poly(allylamin
e
hydrochloride)
End-stage
renal disease
Oral
Elan,Abbott Tricor Nanocrystallin
e fenofibrate
Anti
hyperlipidemc
OralRef. Garg, A., Visht, S., Sharma, P. K., & Kumar, N. (2011). Formulation,
characterization and application on nanoparticle: a review. Der Pharmacia Sinica,
COMMERICAL PRODUCTS OF NANOPARTICLES

28. Recent Advances in Nanoparticles
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Solid lipid nanoparticle:
 SLN are submicron colloidal carriers (50-1000nm) which
are composed of physiological lipid.
Ref. https://www.researchgate.net/figure/Solid-Lipid-Nanoparticles

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Dry Powder Aerosol:
 Lung cancer treatment can be achieved by using
nanoparticles in dry powder aerosol form .
Ref.

30. Application Purpose Material
Cancer therapy Targeting, Reduced toxicity,
enhance uptake of anti-
tumor agent
Polyalkylcyanoacrylate
with anticancer agent
Intra cellular targeting Target reticuloendothelial
system for intracellular
infection
Poly alkyl cyanoarylate
Vaccine adjuvant Prolong systemic drug
effect. Enhance immune
response
Poly methyl metha
acrylate nanoparticles
with vaccines
DNA delivery Enhanced bioavailability and
significantly higher
expression level
DNA gelatin
nanoparticles, DNA
chitosan nanoparticles
Ocular delivery Improved retention of the
drug and reduced washed
out.
Poly alkyl cyanoacrylate
nanoparticles , anti-
inflammatory agent
Applications:
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31. References:
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 Targetted and controlled drug delivery by S.P. VYAS and
R.K. KHAR
 Jain N.K Advances in controlled and noval drug delivery ,
CBS publisher & Distributer, edition 1 st ,pg 408
 Nanotechnology in drug delivery - A Review, Indian
Drugs, Issue 11,november 2011.
 http://en.wikipedia.org/wiki/Nanoparticle
 https://www.sciencedirect.com/science/article/abs/pii/S0169
409X16301533
 http://www.pharmainfo.net/reviews/nanoparticles-review

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