niosome ndds- by ankita rai
TRANSCRIPT
NIOSOME A Novel Drug Delivery System
Presented by:
Ankita Rai
M.Pharmacy 2nd
semester
0106PY14MP07
CONTENTS
Introduction
General characteristics
Types
Method of Preparation
Factors affecting the physicochemical properties
Evaluation Parameters
Advantages
Disadvantages
Therapeutic Applications
Marketed Products
References
• Definition: Non-ionic surfactant based vesicle.
Nios = non ionic surfactant
somes = vesicles
• Very small and microscopic in size.
• Vesicles are prepared from self assembly of hydrated non
ionic surfactant molecules.
GENERAL CHARACTERISTICS
Biocompatible
Biodegradable
non-toxic
non immunogenic
non-carcinogenic
High resistance to hydrolytic degradation.
The properties of niosomes depends on both composition
of the bilayer & on method of their production.
STRUCTURE
•Hydrophobic drugs
localized in hydrophobic
lamella
•Hydrophilic drugs
localized in
encapsulated aqueous
region
TYPES
Small
Unilamellar
Vesicle
(SUV)
Large
Unilamellar
Vesicle
(LUV)
Multilamellar
Vesicle
(MLV)
Typical Size Ranges: SLV: 20-50 nm – MLV:100-1000 nm
METHOD OF PREPARATION:
1. Ether Injection method(LUV)
2. Hand shaking method(MLV)
3. Reverse phase evaporation technique(LUV)
4. The “Bubble” method
5. Sonication(SUV)
6. Micro fluidization(SUV)
7. Formation of Niosomes from Proniosomes
8. Multiple membrane extrusion method
9. Trans membrane pH gradient drug uptake
process (remote loading) (MLV)
Common stages of all methods of preparation of
Niosomes
Cholesterol+Non ionic surfactant
Solution in organic solvent
Thin film
Niosome suspension
Dissolve in organic solvent
drying
Dispersion(hydration)
Ether Injection
Surfactant+cholester
ol
Dissolve in Diethyl
ether
Inject into aqueous media(60 ̇C)
14 gauge needle syringe
Niosomes(LUV)
Surfactant+Cholesterol
Dissolve in diethyl ether
Evaporate in rotary evaporator
Hydration(with agitation)
Niosomes(MLV)
Hand shaking Method
Surfactant chloroform+PBS w/o emulsion
Surfactant+Cholesterol aqueous phase in vial
ULV ultrasonic vibration probe sonication
(5min at 60 ̇C)
Reverse phase evaporation technique:
Sonication & evaporation hydration Vesicle
s
Sonication:
ML
V
BUBBLE METHOD:
The bubbling unit consists of round-bottomed flask with three necks positioned in water bath to control the temperature.
Water-cooled reflux and thermometer is positioned in the first and second neck and nitrogen supply through the third neck.
Surfactant+cholesterol Dissolved in buffer at pH 7.4 at 70 0
C
Homogenization for 15 min Bubbled at 70 0 c using N 2
gas
Niosome
s
MULTIPLE MEMBRANE EXTRUSION METHOD
Surfactant, cholesterol, diacetyl
phosphate in chloroform Thin film
evaporatio
n Hydration with
aqueous drug
Suspension extruded through
polycarbonate membranes Upto 8 passages
forms vesicles Niosomes
(of controlled size)
MICROFLUIDIZATION: •1submerged jet principle in which two fluidized streams interact at ultra high velocities,
in precisely defined micro channels within the interaction chamber.
• The impingement of thin liquid sheet along a common front is arranged such that the
energy supplied to the system remains within the area of niosomes formation.
•The result is a greater uniformity, smaller size and better reproducibility of niosomes
formed.
FORMATION OF NIOSOMES FROM PRONIOSOMES
Another method of producing niosomes is to coat a water-soluble carrier such as sorbitol with
surfactant.
The result of the coating process is a dry formulation. In which each water-soluble particle is
covered with a thin film of dry surfactant.
This preparation is termed “Proniosomes”.
The niosomes are recognized by the addition of aqueous phase at T > Tm and brief agitation.
T = Temperature.
Tm = mean phase transition temperature
TRANS MEMBRANE PH GRADIENT DRUG UPTAKE
PROCESS (REMOTE LOADING)
Surfactant+chlolester
ol in chloroform evaporatio
n
Hydration using
citric acid
ML
V
3 freeze thaw cycles sonication
Niosomal
suspension
Aqueous solution of
drug
pH 7.0-7.2 using 1M disodium
phosphate
Heat at 60 ̇C for 10 min
niosome
s
FACTORS AFFECTING THE PHYSICOCHEMICAL
PROPERTIES OF NIOSOMES
NIOSOMES
Hydration temperature
Non-ionic surfactant
nature
Nature of encapsulated
drug
Size reduction technique
Membrane additives
EVALUATION PARAMETERS
1. %Entrapment Efficiency:
%EE= (Amount entrapped/Total amount) * 100
2. Size, shape & morphology:
Transition electron microscopy
Freeze fractured microscopy
Optical microscopy
3. Invitro release
4. Invivo release
5. Stability study
6. Membrane rigidity
7. Number of lamellae:
NMR
Small angle X-ray scattering
8. Vesicular surface charge:
Microelectrophoresis
Dynamic light scattering
ADVANTAGES
• Targeted drug delivery
• Reduction in dose
• Decrease in side effects
• Both hydrophilic and lipophilic drugs can be encapsulated
• Improve therapeutic efficacy
• Osmotically active and stable
• Improve oral bioavailability of poorly soluble drug
• Enhance the skin permeability when applied topically
• Can be use through various routes eg. Oral, parentral, topical, ocular etc.
• The bilayer of niosomes protect the enclosed drug from various factors present both inside and outside the body.
S.No, LIPOSOMES NIOSOMES
1. Vesicles made up of concentric
bilayer of phospholipids
Vesicles made up of surfactants with or
without incorporation of cholesterol
2. Size ranges from 10-3000nm Size ranges from 10-1000nm
3. Comparatively expensive Inexpensive
4. Special storage condition are
required
No such requirement
5. Phospholipids used are unstable Non-ionic surfactants are stable
6 Comparatively more toxic Less toxic
Comparison between liposomes &
niosomes:
DISADVANTAGES
• Physicochemical instability
• Time consuming
• Requires specialized equipment
• Insufficient drug loading
THERAPEUTIC APPLICATIONS
1.Targeting of bioactive agents
a) To reticulo - endothelial system (RES)
b) To organs other than RES
2. Neoplasia
eg.Doxorubicin
3. Leishmaniasis
eg.Sodium stibogluconate
4. Delivery of peptide drugs
5. Immunological applications
6. Carrier for hemoglobin
7. Transdermal delivery of drugs
8. Other applications
a)Sustained release
b)Localized drug action
MARKETED PRODUCTS
• Lancome has come out with a variety of anti-
ageing products which are based on
niosome formulations.
L’Oreal is also conducting anti-ageing
products.
REFERENCES
• Malhotra M, Jain NK, Niosomes as drug carriers. Indian drugs 1994;31:81-6.
• Dr Rakesh P. Patel, Niosomes: A unique drug delivery system, vol5 Issue6, 2007, Pharmainfo.net.
• Uchegbu IF, Vyas SP, Non ionic surfactant based vesicles(niosomes) in drug delivery.lnt J Pharm1998;172:33-70.
• Chouhan S. and Luorence M.J., The preparation of polyoxyethylene containing non ionic surfactant vesicles. J.Pharm.Pharmacol 1989;41:6p.