Liposomes: Formation, preparation, properties and applications

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Presentation transcript:

Liposomes: Formation, preparation, properties and applications Dr. S.S.Apte Professor, Univ. College of Pharm. Sci., Kakatiya University, Warangal Presently: NDDS Divn, Natco Research Centre Hyderabad

Liposomal Anthracycline Antibiotics Used in Therapy Product Drug Marketed By Registration Year DaunoXome Daunorubicin citrate NeXstar Pharmaceutical Inc. England Sweden USA 1995 r. 1995 r. 1996 r. Doxil Doxorubicin Sequus Pharmaceutical Inc. USA 1995 Caelix   Schering-Plough Selected European Countries 1995 r.

Definition of Liposomes Liposomes are spherical, self closed structures composed of curved lipid bilayers which entrap part of the solvent, in which they freely float, into their interior. They may consist of one or several concentric membranes; their size ranges from 20 nm to several dozens µm, while thickness of the membrane is around 4 nm.

Salient features Discovered in 1968 by Alec Bangham Delivery system for hydrophilic, lipophilic, and amphiphilic APIs Solubilization of lipophilic and amphiphilic APIs Protection of the API Reduction of side effects - toxicity of the active Sustained release Drug targeting Low application dose

Classification of Liposomes SUV = Small Unilamellar Vesicles LUV = Large Unilamellar Vesicles MLV = Multilamellar Vesicles LLC = Lamellar Liquid Crystalline Phase MVV = Multivesicular vesicles Liposomes are composed of one to several hundreds concentric membranes

liposomes (phospholipids + Cholesterol) Vesicular delivery systems liposomes (phospholipids + Cholesterol) Vesicles Niosomes (Nonionic surfactants +cholesterol)

Preparation of vesicles: Film casting via organic solvent film hydration ether-ethanol injection Reverse phase evaporation Through mixed micellar solution Mechanical methods

Characterization of vesicles: Size and size distribution - Dynamic light scattering Electron microscopy Coulter counter Number of lamellae - NMR spectroscopy small angle X ray scatter Charge - Microelectrophoresis Entrapment efficiency - Gel filtration Capture volume - ultrafiltration dialysis protamine aggregation ultracentrifugation Release - Dialysis

Liposomal Delivery of Anti-Cancer Agents Slow Release: reduced peak levels of free drug and prolonged tumor exposure Change in Biodistribution: avoiding drug deposition in certain tissues will reduce tissue-specific toxicities Tumor Targeting: passive accumulation by enhanced permeability and retention (EPR) effect

Phospholipids in topical pharmaceutical applications Drug Effects Benzoyl peroxide Flurbiprofen Diclofenac Heparin Clindamycin phosphate Aciclovir Menthol & camphor N,N-diethyl-meta-toluamide (DEET) Povidone-Iodine Tamoxifen Econazol, Miconazol Glycolic acid Bethametasone 17-benzoate improved drug delivery; higher anti-bacterial efficacy better penetration; improved efficacy in pain treatment improved drug delivery; higher drug efficacy improved penetration; higher drug efficacy sustained release, drug efficacy improvement enhanced penetration enhanced penetration, rapid onset of action controlled release, inhibition of absorption improved drug delivery & efficacy improved penetration and drug retention in the skin drug retention in the skin controlled release penetration enhancement