Application of Nanoparticles in Transdermal drug delivery system

1. Nanoparticles for Transdermal
Drug Delivery
By: Mr. Kiran Ankushrao Tengse
M.Pharm 2nd Year
Department of Pharmaceutical Sciences
RTMNU,Nagpur.

2. Contents
• Introduction to Nanoparticles
• Types of nanoparticles
• Types of polymeric carriers
• Strucrure of the skin
• Routes of drug permeation
• Factors affecting drug permeability
• Basic components of transdermal delivery
• Evaluation of nanoparticles
• References

3. Nanoparticles
• Nano particles are solid colloidal particles
ranging in size from 10 nm to 1000nm (1
micron). They consist of macromolecular
materials in which the active principle is
dissolved, entrapped or encapsulated and/or
to which the active principle is adsorbed or
attached to and can be used for therapeutic
disease management.

4. Types
• Nanospheres :Nanospheres are matrix
systems in which the drug is physically and
uniformly dispersed.
• Nanocapsules :Nano capsules are systems in
which the drug is confined to a cavity
surrounded by a unique polymer membrane.

5. TYPES OF POLYMERIC CARRIERS :
• Natural hydrophilic polymers
Protein Polysacharides
Gelatin Alginate
albumin Dextran
lectin Chitosan
legumin Agarose

6. • Synthetic hydrophobic polymers
Pre-polymerised Polymerized in process
Poly(ε-caprolactone) (PECL) Poly
(isobutylcyanoacrylates)(PICA)
Poly (Lactic acid) (PLA) Poly(butylcyanoacrylates)(PBC
A)
Poly(Lactide-co-
glycolide)(PLGA)
Polyhexylcyanoacrylates(PHCA
)
Polystyrene Polymethyl(methacrylate)
(PMMA)

7. Structure of The Skin
Fig.6. Anatomy of skin

8. Routes of drug absorption through
skin

9. FACTORS AFFECTING TRANSDERMAL
PERMEABILITY
1. Physicochemical properties of parent molecule
2. Physicochemical properties of drug delivery
system
3. Physiological and pathological condition of
skin
4. Biological factors

10. BASIC COMPONENTS OF TRANSDERMAL
DRUG DELIVERY SYSTEM
COMPONENT OF TRANSDERMAL DEVICE INCLUDE:
1) POLYMER MATRIX
2) THE DRUG
3) PERMEATION ENHANCER
4) OTHER EXCEPIENTS

11. Selection of Polymer
i) Molecular weight, glass transition temperature
and chemical functionality of the polymer should
be such that the specific drug diffuses properly and
gets released through it.
ii]The polymer should be stable, nonreactive with
the drug, easily manufactured and fabricated into
the desired product, and should be inexpensive.
(iii) The polymer and its degradation products must
be nontoxic or non antagonistic to the host.
(iv) The mechanical properties of the polymer
should not deteriorate excessively when large
amounts of active ingredients are incorporated into
it.

12. • Polymers used for Transdemal delivery
1.Natural Polymers:
Cellulose derivatives, zein , gelatin, waxes, proteins
and their derivatives , natural rubber , starch, chitosan.
2. Synthetic elastomers:
Polybutadiene , hydrin rubber, polysiloxane silicone
rubber, nitrile, acrylonitrile, butyl rubber rubber ,
styrene–butadiene rubber, neoprene,
etc.
3.Synthetic Polymers
Polyvinylalcohol,polyvinylchloride,polyethylene,polyprop
ylene,polyacrylate,polyurea,polyvinylpyrrolidone,polymet
hylmethacrylate,epoxy, ethylcellulose ,hydroxy propyl
cellulose, polyamide, etc.

13. • Selection of Drug
i]Compounds with low logP will not diffuse into
skin lipids
ii]However, compounds with high logP also have
difficulties, this time associated with their
diffusion out of the stratum corneum.
iii]The accepted range of logP values is between
1 and 3.
iv] Dose less than 20 mg per day
v] Mol. wt. less than 400 Da.
vi] Melting point less than 200 degree celcius.

14. • Selection of permeation enhancers.
They increase the permeability of the skin for
drug uptake .
Permeation enhancer types
Physical Chemical
enhancer enhancer
→ Chemical enhancers: sulphoxide (DMSO),
fatty acids (oleic acid), alcohol (methanol), glycol
(propylene glycol) and surfactant (anionic
surfactant), azone (lauracapran), etc.
→Physical enhancers: Sonophoresis is good
example

15. Other excipients
1. Adhesives: to make intimate contact with
skin at macro and micro level.
e.g.polyisobutylenes,acrylics,silicones.
2. Backing membrane:protect the product
during use on the skin .
e.g. polyethylene, polyester films, aluminum and
polyolefin films.

16. EVALUATION OF NANOPARTICLES
• Particle size
• Density
• Molecular weight
• Structure and crystallinity
• Specific surface area
• Surface charge & electronic mobility
• Surface hydrophobicity
• Invitro release
• Nanoparticle yield
• Drug entrapment efficiency

17. 1.PARTICLE SIZE
• Particle size and size distribution are the most
important characteristics of nanoparticle
systems.
• They determine the in vivo distribution,
biological fate, toxicity and the targetting ability
of nano particle systems
• In addition they can also influence the drug
loading, drug release and stability of nano
particles
-Photon correlation spectroscopy (PCS) : For
smaller particle.
-Laser diffractrometry : For larger particle.
-Electron microscopy (EM) : Required coating of
conductivematerial such as gold & limited to dry
sample.

18. -Transmission electron microscopy (TEM) :
Easier method & Permits differntiation
among nanocapsule & nanoparticle.
2.Density :
1.Helium or air using a gas pycnometer
2.Density gradiant centrifugation
3. Molecular weight :
Gel permeation chromatography using
refractive index detector.
4. Structure & Crystallinity :
X-ray diffractionThermoanalytical method
such as,DTA,DSC,TG.

19. 5. Surface charge & electronic mobility :
• Surface charge of particle can be determined
by measuring particle velocity in electrical
field.
• Laser Doppler Anemometry tech. for
determination of Nanoparticles velocities.
• Surface charge is also measured as electrical
mobility.
• Charged composition critically decides bio-
distribution of nanoparticle .
• Zeta potential can also be obtain by measuring
the electronic mobility.

20. 6. Drug entrapment efficiency :
%drug entrapment=
Initial wt.-final wt. ×100
Initial wt.

21. REFERENCES
1. Yadav Vaibhav Rastogi, Pragya Transdermal drug delivery
system: An overview, Asian Journal of Pharmaceutics · July
2012.
2. Novel drug delivery systems, 2nd edition, by Y.W. Chein page
no.: 338 – 380.
3. Brian C. Palmer 1 and Lisa A. DeLouise, Nanoparticle-Enabled
Transdermal Drug Delivery Systems for Enhanced Dose
Control and Tissue Targeting ,Molecule, December 2016