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Niosome ndds- By Ankita Rai
- 1. NIOSOME A Novel DrugDelivery System Presented by: Ankita Rai M.Pharmacy 2nd semester 0106PY14MP07
- 2. CONTENTS Introduction General characteristics Types Method ofPreparation Factors affecting the physicochemical properties Evaluation Parameters Advantages Disadvantages Therapeutic Applications Marketed Products References
- 3. • Definition: Non-ionicsurfactant 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.
- 4. 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.
- 5. STRUCTURE •Hydrophobic drugs localized inhydrophobic lamella •Hydrophilic drugs localized in encapsulated aqueous region
- 6. TYPES Small Unilamellar Vesicle (SUV) Large Unilamellar Vesicle (LUV) Multilamellar Vesicle (MLV) Typical Size Ranges:SLV: 20-50 nm – MLV:100-1000 nm
- 7. 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)
- 8. Common stages ofall methods of preparation of Niosomes Cholesterol+Non ionic surfactant Solution in organic solvent Thin film Niosome suspension Dissolve in organic solvent drying Dispersion(hydration)
- 9. Ether Injection Surfactant+cholester ol Dissolve inDiethyl ether Inject into aqueous media(60 ̇C) 14 gauge needle syringe Niosomes(LUV)
- 10. Surfactant+Cholesterol Dissolve in diethylether Evaporate in rotary evaporator Hydration(with agitation) Niosomes(MLV) Hand shaking Method
- 11. Surfactant chloroform+PBS w/oemulsion Surfactant+Cholesterol aqueous phase in vial ULV ultrasonic vibration probe sonication (5min at 60 ̇C) Reverse phase evaporation technique: Sonication & evaporationhydrationVesicle s Sonication: ML V
- 12. BUBBLE METHOD: Thebubbling 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 minBubbled at 70 0 c using N 2 gas Niosome s
- 13. MULTIPLE MEMBRANE EXTRUSIONMETHOD 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.
- 14. FORMATION OF NIOSOMESFROM 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
- 15. TRANS MEMBRANE PHGRADIENT DRUG UPTAKE PROCESS (REMOTE LOADING) Surfactant+chlolester ol in chloroform evaporatio n Hydration using citric acid ML V 3 freeze thaw cyclessonication Niosomal suspension Aqueous solution of drug pH 7.0-7.2 using 1M disodium phosphate Heat at 60 ̇C for 10 min niosome s
- 16. FACTORS AFFECTING THEPHYSICOCHEMICAL PROPERTIES OF NIOSOMES NIOSOMES Hydration temperature Non-ionic surfactant nature Nature of encapsulated drug Size reduction technique Membrane additives
- 17. EVALUATION PARAMETERS 1. %EntrapmentEfficiency: %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
- 18. ADVANTAGES • Targeted drugdelivery • 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.
- 19. 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:
- 20. DISADVANTAGES • Physicochemical instability •Time consuming • Requires specialized equipment • Insufficient drug loading
- 21. THERAPEUTIC APPLICATIONS 1.Targeting ofbioactive 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
- 22. MARKETED PRODUCTS • Lancomehas come out with a variety of anti- ageing products which are based on niosome formulations. L’Oreal is also conducting anti-ageing products.
- 23. 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.