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Nanoparticles
1. PRESENTED BY- GUIDED BY-
DEEPALI MR. MANOJ K. SARANGI
M.PHARMA (ASSISTANT PROFESSOR)
2ND SEM
(Pharmaceutics)
SARDAR BHAGWAN SINGH P.G. INSTITUTE OF BIO-MEDICAL
SCIENCES & RESEARCH, BALAWALA, DEHRADUN (UTTARAKHAND)
A SEMINAR ON NANOPARTICLES
2. PRESENTATION FOCUS
INTRODUCTION
IDEAL PROPERTIES OF NANOPARTICLES
ADVANTAGES
DISADVANTAGES
TYPES OF NANOPARTICLES
POLYMER USED IN PREPARATION
TECHNIQUES OF PREPARATION
EVALUATION
MARKETED FORMULATION
APPLICATION
CONCULSION
REFERENCE
3. INTRODUCTION
The prefix nano comes from the ancient Greek vavoc through
the Latin nanus meaning very small.
Nanoparticles are defined as particulate dispersions or solid
particles with a size in the range of 10-1000nm.
The drug dissolved, entrapped, encapsulated or attached to a
nanoparticle matrix.
•TIRUWA, R. (2015).A review on nanoparticles–preparation and evaluation parameters, Indian
Journal of Pharmaceutical and biological Research(IJPBR),4(2), 27-31.
•Mohanraj, V. J., & Chen, Y. (2006).Nanoparticles-a review. Tropical Journal of Pharmaceutical
Research, 5(1), 561-573.
4. NANOPARTICLES
NANOCAPSULES-
The nanocapsules are
system in which the
drug is confined to a
cavity surrounded by
a unique polymer
membrane.
NANOSPHERES-
The nanospheres are
matrix systems in
which the drug is
physically and
uniformly dispersed.
•Nagavarma, B. V. N., Yadav, H. K., Ayaz, A., Vasudha, L. S., & Shivakumar, H. G. (2012). Different
techniques for preparation of polymeric nanoparticles—a review. Asian J. Pharm. Clin. Res, 5(3), 16-23.
•Jawahar, N., & Meyyanathan, S. N. (2012). Polymeric nanoparticles for drug delivery and targeting: A
comprehensive review. International Journal of Health & Allied Sciences, 1(4), 217.
5. IDEAL PROPERTIES OF NANOPARTICLES
NECESSARY FOR DRUG DELIVERY
Stable in blood
Nontoxic
Non-thrombogenic
Non-
inflammatory
Non-immunogenic
Biodegradable
Athar, M., & Das, A. J. (2014). Therapeutic nanoparticles: State-of-the-art of
nanomedicine. Adv. Mater. Rev, 1(1), 25-37.
6. ADVANTAGES OF NANOPARTICLES
Fairly easy preparation
Good protection
of the
encapsulated drug
Increased
therapeutic
efficacy
Targeted and drug
delivery
Retention of drug
at the active site
Increased
bioavailability
Good control over size
and size distribution
Longer clearance
time
Dose
proportionality
•Shinde, N. C., Keskar, N. J., & Argade, P. D. (2012). Nanoparticles: Advances in drug delivery
systems. Res. J. Pharm. Biol. Chem. Sci, 3, 922-929.
7. DISADVANTAGES OF NANOPARTICLES
Limited targeting
abilities
Discontinuation of
therapy is not possible
Toxicity
Disturbance of
Autonomic
imbalance
Cytotoxicity
•Shinde, N. C., Keskar, N. J., & Argade, P. D. (2012). Nanoparticles: Advances in drug
delivery systems. Res. J. Pharm. Biol. Chem. Sci, 3, 922-929.
8. NANOMEDICINES FOR DRUG DELIVERY
Tinkle, S., McNeil, S. E., Mühlebach, S., Bawa, R., Borchard, G., Barenholz, Y. C., & Desai N.
(2014). Nanomedicines: addressing the scientific and regulatory gap. Annals of the New York
Academy of Sciences, 1313(1), 35-56.
9. S.NO TYPES OF NANOPARTICLE MATERIALS UED APPLICATION
1 NANOSUSPENSIONS AND
NANOCRYSTALS
Drug powder is disperse
d in surfactant solution
Stable system for
controlled delivery of
poorly soluble drug
2
Solid lipid Nanoparticles
Melted lipid dispersed in
Aqueous surfactant
Least toxic and more
stable
Colloidal carrier systems
as
alternative materials To
polymers
3
Polymeric nanoparticles Biodegradable polymer
Controlled and targeted
drug delivery
4
Polymeric micelles
Amphiphilic block co
polymers
Controlled and systemic
Delivery of water
insoluble
Drugs
5
Magnetic Nanoparticles
Magnetite Fe2O3,Meghe
Mite coated with dextran
Drug targeting
diagnostics
to in medicine
6 Carbon Nanotubes Metals ,semiconductors Gene and DNA delivery
Shinde, N. C., Keskar, N. J., & Argade, P. D. (2012). Nanoparticles: Advances in drug
delivery systems. Res. J. Pharm. Biol. Chem. Sci, 3, 922-929.
10. ROUTES
Bennet, D., & Kim, S. (2014). Polymer nanoparticles for smart drug delivery. In Application of
Nanotechnology in Drug Delivery. InTech.
11. POLYMER USED IN PREPARTION
Natural
Hydrophilic
PROTEINS
POLYSACCHARIDES
Synthetic
Hydrophobic
PRE-
POLYMERIZED
POLYMERIZED IN
PROCESS
12. NATURAL HYDROPHILIC POLYMER
PROTEINS POLYSACCHARIDES
Gelatin Alginates
Albumin Dextran
Lectins Chitosan
Legumin Agarose
Vicilin Pullulan
Vyas, S. P., & Khar, R. K. (2012). Targeted & controlled drug delivery: Novel carrier systems. CBS publishers
& distributors, 332-333.
13. SYNTHETIC HYDROPHOBIC POLYMER
PRE-POLYMERIZED POLYMERIZED IN PROCESS
Poly (e-caprolactone) (PECL) Poly(isobutylcyanoacrylates) (PICA)
Poly(lactic acid) (PLA) Poly(butylcyanoacrylates) (PBCA)
Poly ( lactide -co- glycolide )
(PLGA)
Polyhexylcyanoacrylate (PHCA)
Polystyrene Poly methyl
(methacrylate)(PMMA)
Vyas, S. P., & Khar, R. K. (2012). Targeted & controlled drug delivery: Novel carrier systems.
CBS publishers & distributors, 332-333.
15. METHODS OF PREPARATION OF NANOPARTICLES
BY DISPERSION OF PREFORMED POLYMER
•Nagavarma, B. V. N., Yadav, H. K., Ayaz, A., Vasudha, L. S., & Shivakumar, H. G. (2012). Different
techniques for preparation of polymeric nanoparticles—a review. Asian J. Pharm. Clin. Res, 5(3), 16-23.
16. METHOD FOR PREPARATION OF NANOPRATICLES
BY POLYMERIZATION OF MONOMERS
EMULSION
POLYMERIZATION
MINI- EMULSION
POLYMRIZATION
MICRO-EMULSION
POLYMRIZATION
INTERFACIACL
POLYMERIZATION
CONTROLLED/
LIVING
RADICAL
POLYMERIZATION
•Nagavarma, B. V. N., Yadav, H. K., Ayaz, A., Vasudha, L. S., & Shivakumar, H. G. (2012). Different
techniques for preparation of polymeric nanoparticles—a review. Asian J. Pharm. Clin. Res, 5(3), 16-23.
17. Bennet, D., & Kim, S. (2014). Polymer nanoparticles for smart drug delivery. In Application of
Nanotechnology in Drug Delivery. InTech.
18. EVALUATION PARAMETER OF NANOPARTICLES
1) YIELD OF NANOPARTICLES:-
Precentage Yield = Amount of particle (100)
Amount of drug+ polymer
2) DRUG CONTENT/SURFACE ENTRAPMENT/ DRUG
ENTRAPMENT:-
Precentage drug entrapment = W-w (100)
W
3) PARTICLE SIZE:- Particle size and its distribution is important characteristics in
nanoparticles as they plays major role in distribution, pharmacological activity, toxicity and
targeting to specific sites.
Advanced methods to determine the particle size of nanoparticles is by photon-correlation
spectroscopy or dynamic light scattering, scanning electron microscopy
Sriharitha, J Preethi, Hemanth S (2016).A Review on Nanoparticles in Targeted Drug Delivery
System”,Research & Reviews: Journal of Material Science ,4(4), 1-6.
TIRUWA, R. (2015). A review on nanoparticles–preparation and evaluation parameters, Indian
Journal of Pharmaceutical and biological Research(IJPBR), 4(2), 27-31.
19. 4) PARTICLE SHAPE:- Particle shape of the nano suspensions is determined by
scanning electron microscopy (SEM). In order to form the solid particles these
nano suspensions were subjected to lyophilisation.
5) ZETA POTENTIAL:- Zeta potential is the potential difference existing
between the surface of a solid particle immersed in a conducting liquid and the bulk
of the liquid. The surface charge of the nanoparticles is usually measured by zeta
potential.
4) DIFFERENTIAL SCANNING CALORIMERTY (DSC):- It is used to
determine the nature of crystallinity within nanoparticles through the measurement
of glass and melting point tempertures and their associated enthalpies.
5) ATOMIC FORCE MICROSCOPY (AFM):- It offers a ultra-high resolution
in particle size measurement and is based on a physical scanning of sample at sub-
micron level using a probe tip of atomic scale. AFM provides the most accurate
description of size and size distribution and requires nom mathemical treatment.
•Pandey P, Mandeep D (2016). A Brief Review On Inorganic Nanoparticles”, Journal of Critical
Reviews,3(3), 18-26.
• Sriharitha, J Preethi, Hemanth S (2016).A Review on Nanoparticles in Targeted Drug Delivery
System”,Research & Reviews: Journal of Material Science ,4(4), 1-6.
20. DRUG LOADING
INCORPORATION METHOD
INCUBATION METHOD
INCORPORATION METHOD- Incorporating at the time of nanoparticle production
INCUBATION METHOD- Adsorbing the drug after the formation of nanoparticles
by incubating the carrier with the concentrated drug solution.
Both methods result in:
A solid solution of the drug in the polymers
Solid dispersion of the dug in the polymer.
Surface adsorption of the drug.
Chemical bonding of the drug in the polymer.
Ranjit, K., & Baquee, A. A. (2013). Nanoparticle: an overview of preparation,characterization
and application. Int. Res. J. Pharm, 4(4), 47-57.
21. DRUG RELEASE AND RELEASE KINETIC
The release of drug from the
particulate system depends upon
three different mechanism:
Release from the surface of
particles.
Diffusion through the
swollen rubbery matrix.
Release due to erosion.
•Ranjit, K., & Baquee, A. A. (2013). Nanoparticle: an overview of preparation, characterization and
application. Int. Res. J. Pharm, 4(4), 47-57.
• Jawahar, N., & Meyyanathan, S. N. (2012). Polymeric nanoparticles for drug delivery and targeting: A
comprehensive review. International Journal of Health & Allied Sciences, 1(4), 217.
22. EVALUATION FOR RELEASE OF DRUG
Various methods which can be used to study the in vitro release of the drug
from nanoparticles are:
1. Side-by- side diffusion cells with artifical or biological membranes
2. Dialysis bag diffusion technique
3. Reverse dialysis bag technique
4. Agitation followed by ultracentrifugation/ centrifugation
5. Ultra- filtration or centrifugal ultra- filtration techniques
23. IN VITRO DRUG RELEASE STUDIES
• DISSOLUTION:-
USP Type 2
RPM 50
Immersed in 900
ml of phosphate
buffer solution
Temperature 37+
0.02 degree
Celsius
Withdrawn 5ml
solution from the
medium
Specific time
periods
Same vol. of
dissolution
medium replaced
in the flask
Maintain the
constant volume
Withdrawn
samples analyzed
using UV
Spectrophotomete
rer
RUWA, R. (2015). A review on nanoparticles–preparation and evaluation parameters, Indian
Journal of Pharmaceutical and biological Research(IJPBR),4(2), 27-31.
24. • STABILITY OF NANOPARTICLES:-
• Nanoparticles
detemination
• Storing
optimized
formulation
4 degree Celsius + 1
degree Celsius & 30
dergree celsius + 2
dergree celsius
• Sample
analyzed
• Stability
chamber for 90
days
0,1,2 & 3 month
time period
• Any changes in
physical
appearance
Their drug
content, drug
release rate
TIRUWA, R. (2015). A review on nanoparticles–preparation and evaluation parameters, Indian
Journal of Pharmaceutical and biological Research(IJPBR), 4(2), 27-31.
25. APPLICATIONS
USED IN TARGETED DRUG DELIVERY TO BRAIN THERAPY
USED IN TARGETING OF NANOPRATICLES
TO EPITHELIAL CELLS IN THE GI TRACT
USING LIGANDS
USED IN BIO
DECTECTION OF
PATHOGENS
STEM CELL
THERAPY
NANOPARTICLES
FOR GENE
DELIVERY
CANCER THERAPY
•Sriharitha, J Preethi, Hemanth S (2016).A Review on Nanoparticles in Targeted Drug Delivery
System”,Research & Reviews: Journal of Material Science ,4(4), 1-6.
•Mohanraj, V. J., & Chen, Y. (2006). Nanoparticles-a review. Tropical Journal of Pharmaceutical
Research, 5(1), 561-573.
26. COMMERICAL PRODUCTS OF NANOPARTICLES
COMPANY TRADE
NAME
COMPOSITION 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-a-
interferon
2a
Hepatitis B,
Hepatitis C
Subcutaneous
Elan,Merck
Emend
Nanocrystalline
aprepitant
Antiemetic Oral
Genzyme Renagel Poly(allylamine
hydrochloride)
End-stage
renal
disease
Oral
Elan,Abbott Tricor Nanocrystalline
fenofibrate
Anti
hyperlipidemc Oral
Garg, A., Visht, S., Sharma, P. K., & Kumar, N. (2011). Formulation, characterization and application on
nanoparticle: a review. Der Pharmacia Sinica, 2(2), 17-26.
27. COMMERICAL PRODUCTS OF NANOPRATICLES
COMPANY TRADE
NAME
COMPOSITION INDICATION ROUTES
Astra Zeneca
Pharma
Diprivan Propofol
liposomes/lipid
Anesthetic IV
Teva Pharma Copaxone Copolymeric
mixture of L-
glutamic acid, L-
alanine, L-
tyrosine & L-
lysine
Relapsing
remitting
multiple
sclerosis
subcutaneous
Bio Sante Elestrin Estradiol gel
(0.06%)
Moderate to
severe hot
flashes in
menopausal
women
Transdermal
Abraxis
Bioscience
Abraxane Paclitaxel (Taxol)
bound albumin
nanoparticles
Various cancers IV
28. CONCLUSION
• The main goal of this review was to describle the different preparation
technique available for production of polymeric nanoparticles.
• The drug-loded nanospehere or nanocapsules now can be produced by
simple,safe and reproducible techniques available.
• The limitation like one particulae process or technique is not suitable to all
drugs,post prepartive steps, such as purifaction and preservation,
incomplete or discontinuous film, inadequate stability of certain active
components are remained to solve.
• Despite these technological challenges,naonparticles have been showed
great promise for the development.
•Nagavarma, B. V. N., Yadav, H. K., Ayaz, A., Vasudha, L. S., & Shivakumar, H. G. (2012).
Different techniques for preparation of polymeric nanoparticles—a review. Asian J.
Pharm. Clin. Res, 5(3), 16-23.