This presentation is for the subject of sterile product and formulation technology

1. Presented by Under The Guidance
Khan Ramiz V DR. N.A. Gujarathi sir
M. Pharm (1st year) M.Pharm, PHD
Dept. of Pharmaceutics
SIPS

2. CONTENTS
 Introduction
 Classification of NNDS
 Definition of Nanoparticles
 Classification NP
 Advantages and disadvantages of NP
 Definition of Liposomes
 Classification of liposomes
 Method of preparation
 Advantages and disadvantages of liposomes
 Application of liposomes
 Definition of Niosomes
 Types of Niosomes
 Method of preparation
 Advantages and disadvantages
 application

3. INTRODUCTION
 NOVEL DRUG DELIVERY SYSTEM (NDDS)
 It refers to approaches, formulation, technologies, and
system for transporting a pharmaceutical compound in the
body as needed to safely achieve its desired therapeutic
effect.
 Technologies modify drug release profile, absorption,
distribution and elimination for the benefit of
a) improving product efficacy and safety
b) patient convenience and compliance.

4. Classification
 Nanoparticals
 Liposomes
 Niosomes
 Microspheres
 Monoclonal antibodies
 Micro emulsions
 Magnetic microcapsules
 Implantable pumps

5.  Nanoparticles
“Nano particles are sub-nanosized colloidal structures
composed of synthetic or semi-synthetic polymers”
 Size range : 10-1000nm
 The drug is dissolved, entrapped, encapsulate or attached to
a nanoparticles matrix.
Based on method of preparation:
 Nanocapsules:-
Nano capsules are systems in which the drug is confined
to a cavity surrounded by unique polymer membrane.
Nanosphere:-
Nano sphere are matrix system in which the drug is
physically an uniformly dispersed.

6. Classification
 Solid lipid Nanoparticles
 Polymeric Nanoparticles
 Ceramic Nanoparticles
 Hydrogel Nanoparticles
 Copolymerized Peptide nanoparticles
 Nanocrystals and nanosuspension
 Nanotubes

7.  Solid Lipid Nanoparticles:
 New type of colloidal drug carrier system for I.V.
 Consist of spherical solid particles in the nm range, dispersed
in water or in aqueous surfactant solution.
 Polymeric nanoparticles (PNPs) :
 Are defined as particulate dispersion or solid particles with
size in the range of 10-1000nm.
 Composed of synthetic or semi-synthetic Polymers.
 Biodegradable polymeric nanopaticles Polylactic acid (PLA),
polyglycolic acid (PGA), Polylactic- glycolic acid (PLGA), and
Polymethyl methacrylate (PMMA)

8.  Ceramic Nanoparticles :
 These are the nanoparticles made up of inorganic (ceramic)
compounds silica, ( inorganic/metal) titania and alumina.
The size less than 50 nm, which helps them in penetrate
deeper parts of the body.
 Hydrogel Nanoparticles :
 Polymeric system involving the self-assembly and self
aggregation natural polymer amphiphiles cholesteroyl
pullulan, cholesteroyl dextran and agarose cholesterol
groups provide cross linking point.

9. Copolymerized Peptide Nanoparticles :
 drug moiety is covalently bound to the carrier instead of
being physically entrapped.
 Nanocrystals and Nanosuspension :
 Pure drug coated with surfactant, particles in aggregation of
these particles crystalline form. Drug powder dispersed in
aqueous surfactant solution.
 Functionalized Nanocarriers :
 Biological materials like proteins, enzymes, peptide etc… are
being utilized as a carriers for the drug delivery.

10. Advantages
 Nano particles can be administered by parenteral, oral, nasal,
occular routes.
 Improving stability and therapeutics index and reduce toxic
affects.
 Both active and passive drug targetting can be achieved by
manipulating the particle size and surfactant characterized of
nanoparticles.
disadvantages :
 Small size and large surface area can lead to particle
aggregation.
 Physical handling of nano particles is difficult in liquid and dry
form.
 Toxic metabolism may form.

12. LIPOSOMES
 Liposomes are simple microscopic, concentric bilayered
vesicles in which an aqueous volume is entirely enclosed by a
membranous lipid bilayer mainly composed of natural or
synthetic phospholipid.
 Discovered in 1960s by Bangham and coworkers.
 The structure main components are phospholipid and
cholesterol.

15. Classification
On the basis of structural parameters:
1) Multilamellar vesicles (>0.5 µm) MLV
2) Unilamellar vesicles (all size range) UV
 Small unilamellar vesicles (20-100 nm) SUV
 Medium sized unilammelar vesicles MUV
 Large unilammelar vesicles (>100 nm) LUV

16. Method of liposome preparation
 Physical dispersion method:-
1. Hand shaking MLVs
 To reduce liposomes size :
1. Micro emulsification
 To increase liposome size :
1. Dried reconstituted vesicles

17. Hand shaken MLVs
Lipid + solvent (chloroform: Methanol)
↓ (In 250 ml RBF)
Evaporate for 15 min above phase transition temperature
↓ (Flush with nitrogen)
Till residue dry
↓
Add 5ml buffer containing material to be entrapped
↓
Rotate flask at room temp, at 60 RPM for 30 min until lipid
remove
from wall of RBF
↓
Milky white dispersion (stand for 2 hrs to get MLV)

18. Micro emulsification liposomes (MEL)
 MEL is prepared by the “Micro fluidizer” which pumps fluid
at very high pressure (10,000psi) through a 5 µm orifice.
 Then, it is forced along defined micro channel, which direct
two stream of fluid to colloid together at right angle at very
high velocity.
 After a single pass, size reduced to a size 0.1 and 0.2 µm in
diameter.

19. Freeze thaw sonication
 SUV in aqueous phase + Solute
↓
freeze drying
↓
FTS method, thawing = melting
↓
Sonication (15-30 sec)
↓
Solute in unilamellar vesicle

20. Advantage :
 Provide selective passive targeting to tumor tissues.
(liposomal doxorubicin)
 Increased efficacy and therapeutic index.
 Reduction in toxicity of the encapsulated agent.
 Site avoidance effect ( avoids non target tissues).
 Improved pharmacokinetic effects.

21. Disadvantages
 Production cost is high.
 Leakage and fusion of encapsulated drug / molecules.
 Sometimes phospholipid undergoes oxidation and
hydrolysis like reaction.
 Short half life
 Low solubility.

22. Application
 Chelation therapy for treatment of heavy metal poisoning.
 Liposomes as Protein carriers in immunology
 Sustained or controlled delivery
 Site specific delivery
 Study of membrane
 Oral drug delivery
 Formulation aid
 Cosmetic

23. NIOSOMES
 Novel drug delivery system, in which the medication is
encapsulated in a vesicle which is composed of a bilayer of
non-surface active agents.
 It is very small, and microscopic in size.
 Although structurally similar to liposomes, they offer
several advantages over them.
 Similar to liposomes , in that they are also made up of a
bilayer.

24. TYPES OF NIOSOMES
 According to the nature of lamellarity
1. Multilamellar vesicles (MLV) 1-5 µm in size.
2. Large Unilamellar vesicles (LUV) 0.1-1µm in size.
3. Small Unilamellar vesicles (SUV) 25-500 nm in size.
 According to the size
1. Small Niosomes (100 nm-200 nm)
2. Large Niosomes (800 nm-900 nm)
3. Big Niosomes (2 µm-4 µm)

25. Fig. Niosomes

26. METHODS OF PREPARATION
 Film Method
 Ether Injection method
 Sonication
 Reverse Phase Evaporation
 Heating Method
 Microfluidization
 Multiple Membrane Extrusion Method

27. FILM METHOD
 Also known as hand shaking method
Take a mixture of surfactant and cholesterol
↓
Dissolved in an organic solvent in a round bottomed flask.
(eg. Diethyl ether, chloroform,etc)
↓
organic solvent is removed by low pressure/vaccume at
room temperature.(by using rotary evaporator)
↓
The resultant dry surfactant film is dehydrated by agitation
at 50-60⁰C
↓
multilamellar vesicle (MLV) are formed.

28. ADVANTAGES
 Since the structure of the niosomes offers place to
accommodate hydrophilic, lipophilic as well as ampiphilic
drug moieties, they can be used for a varietey of drug.
 The vesicles can act as a depot to release the drug slowely and
of controlled release.
 Biodegradable and biocompatible.
DISADVANTAGES
 Time consuming .
 Required specialized equipment .
 Inefficient drug loading.
 Aqueous suspension of niosomes may exihibit fusion,
aggregation, leaching of entrapped drug.

29. APPLICATION
 Noisomes as Drug Carriers
 Drug Targeting
a) delivery to the brain
b) Anti cancer drug
c) Anti infection
 Ophthalmic drug delivery
 Transdermal delivery of drugs by Niosomes
 Sustained Release
 Localized drug action

30. References
 The theory & practical of industrial pharmacy by Leon
Lachman, Herbert A. Lieberman, Joseph L. kening, 3rd
edition, published by Varghese Publishing house,
page no 872

31. THANK YOU