This document provides an overview of nanoparticles for drug delivery. It defines nanoparticles as sub-nano sized colloidal structures composed of synthetic or semi-synthetic polymers with a size range of 10-1000 nm. The document then classifies nanoparticles and discusses commonly used polymer materials. It describes advantages such as improved drug stability and targeting abilities. Preparation methods like emulsion polymerization and solvent evaporation are summarized. Key characterization techniques and applications for cancer therapy and prolonged circulation are also highlighted.
2. CONTENTS:
INTRODUCTION
CONCEPT
CLASSIFICATION
POLYMERS FOR NANOPARTICLE
ADVANTAGES AND DISADVANTAGES
IDEAL CHARACTERICTICS
METHOD OF PREPARATION
CHARACTERIZATION AND EVALUATION
APPLICATIONS
CONCLUSION
REFERENCE
3. INTRODUCTION:
DEFINATION:
Nanoparticles are sub-nano sized colloidal
structures composed of synthetic or semi-synthetic
polymers.”
Size range : 10–1000 nm .
The drug is dissolved, entrapped, encapsulated or
attached to a nanoparticle matrix.
4. CONCEPT :
The basic Concept involved is :
Nanoparticles are mainly taken by :
» Reticulo Endothelial System (RES), After the administration;
» Hence are useful to carry drugs to the liver and to cells that are
phagocytically active.
Control the particle size, surface properties and release of
pharmacologically active agents in order to achieve the site-
specific action of the drug at the therapeutically optimal rate and
dose regimen.
7. Advantages Of Nanoparticle:
Nanoparticle can be administered by
parenteral,
oral,
nasal,
, occular routes.
Improves stability and therapeutics index and reduce toxic affects.
Both active & passive drug targetting can be achieved.
Reduction in the frequency of the dosages taken by the patient.
Avoids hepatic first pass metabolism.
8. Disadvantage Of Nanoparticle:
Toxic metabolites may form.
Limited drug loading.
Small size & large surface area can lead to particle
aggregation .
Physical handling of nanoparticles is difficult in liquid and
dry forms.
High cost.
9. IDEAL CHARACTERISTICS:
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.
simple, reproducible & cost effective.
10. Method Of Preparation:
A) Amphiphilic macromolecule cross linking
1)Heat cross linking/Chemical crosslinking
2)Emulsion chemical dehydration
B) : Polymerization based
1) Emulsion (micellar) polymerization
2) Dispersion polymerization
3) Interfacial condensation polymerization
11. C) Polymerization precipitation method
1) Solvent extraction/evaporation
2) Solvent displacement(Nanoprecipitation)
3) Salting out
12. A) Nanoparticle preparation by cross-linking of
Amphiphilic macromolecule :
Nanoparticles can be prepared from Amphiphilic
macromolecules, proteins and polysaccharides (which have
affinity for aqueous and lipid solvents).
The method involves Aggregation of Amphiphiles followed
by stabilization either by heat denaturation or chemical
cross-linkining
13. Heat cross linking / Chemical cross linking
The cross linking method is exhaustively used for nano –
encapsulation of drug.
»This method involve emulsification of bovine serum
albumin (BSA) OR human serum albumin (HSA) or
protein aqueous solution in oil using high-pressure
homogenization or high frequency sonication.
14.
15. Emulsion chemical dehydration:
Stabilization can also be achieved by emulsion chemical
dehydration.
» Hydroxy propyl cellulose solution in chloroform is used
as a continuous phase
» 2,2, di-methyl propane (Dehydrating agent) is used to
disperse into the internal aqueous phase to form an
Emulsion.
Produce nanoparticle of size ( 300 nm ).
16. B) : Polymerization based method:
1) 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.
17. A] Micellar nucleation and polymerization
In this the monomer is emulsified in non- solvent phase
using surfactant molecule.
This lead to the formation of :
• Monomer – swollen micelle
• Stabilised monomer droplet
• The monomer molecule reaches the micelle by diffusion
from the monomer droplets through continuous phase,
thus allowing polymerization to progress within micelle.
Here monomer droplet act as a reservoirs of monomer.
18.
19. B] Homogenous nucleation and polymerization
In this both micelle and droplet act as monomer reservoir
throught polymer chain length . When oligomers reach
certain length, they precipitate and form primary particle
and stabilized by surfactant molecules provided by miceiie
and droplets in which the drug will entrapped to form
nanoparticles.
20.
21. Dispersion polymerization
In emulsion polymerization , monomer is emulsified in
non –sollvent phase by means of surfactants .In case of
dispersion polymerization ,monomer is dissolved on
aqueous medium.
The nucleation is directly induced in aqueous monomer
solution and presence of stabilizer or surfactant is not
necessary for formulation of stable nanospheres.
22.
23. Interfacial polymerization:
In this method ,a polymer that becomes core of
nanoparticle and molecule to be loaded is dissolved in
volatile solvent.
Solution is then placed in to a non-solvent for both
polymer and core phase.
polymer phase is separated at o/w interface. Resultant
mixture instantly turns to milky owing to formulation of
nanocapsules.
24.
25. C) Polymerization precipitation method:
1) Solvent extraction/evaporation:
This method involves the formation of o/w emulsion
between partially water miscible solvent containing
the polymer and the drug ,and aqueous phase
containing the stabilizer.
The first step requires emulsification of the
polymer solution into an aqueous phase. During the
second step polymer solvent is evaporated, inducing
polymer precipitation as nanospheres
26.
27. Salting Out Method
Salting-out is based on the separation of a water
miscible solvent from aqueous solution via a
salting-out effect.
Polymer and drug are initially dissolved in a
solvent which is subsequently emulsified into an
aqueous gel containing the saltingout agent
(electrolytes,)
28.
29. Solvent Displacement / Precipitation
method:
Solvent displacement involves the precipitation of
a preformed polymer from an organic solution and
the diffusion of the organic solvent in the aqueous
medium in the presence or absence of surfactant.
The solution is then poured or injected into an
aqueous solution containing stabilizer under
magnetic stirring. Nanoparticles are formed
instantaneously by the rapid solvent diffusion.
34. APPLICATIONS:
1) Widely used in case of Cancer Therapy.
2) In lntracellular Targeting
3) Used for Prolonged Systemic Circulation.
4) As a Vaccine Adjuvant
.
5) In Case of Ocular delivery
.
6) Used in DNA Delivery.
7) Enzyme immunoassays
8) To cross BBB.
35. CONCLUSION
The sustained drug release allows pharmacological
effects to be extended due to the prolonged presence
tine of the carrier system at the targeted inflammed
area.
This new delivery system allows the desired drug to
accumulate in the inflammed tissue with high
efficiency.
36. REFERENCE:
» Targetted and controlled drug delivery by S.P . VYAS and
R.K. KHAR
» Jain N.K. “Advances in controlled and novel Drug
Delivery”, CBS publisher & Distributers, Edition 1st 2001,.
» Nanotechnology in drug delivery - A Review, Indian
Drugs, Issue 11,november 2011.
» http://en.wikipedia.org/wiki/Nanoparticle
http://www.pharmainfo.net/reviews/nanoparticles-review