Liposome ppt by P Rathore & Dr S Nayak

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1 Dr. S. Nayak Principal & Professor Principal.bcp@gmail.com Priyanka Rathore Assistant Professor priyankarathore1jan@gmail.com Liposomes: Advancement in Novel Drug Delivery www.bansalpharmacy.com

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2 Phospholipids Polar Head Groups Three carbon glycerol

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3 What is a liposome? Spherical vesicles with a phospholipid bilayer Hydrophilic Hydrophobic

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Influence of Lipids on Membrane Properties Permeability and stability of liposomes are determined by rigidity of lipid bilayer and determined by : Size & Shape of liposomes Lipid composition

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Membrane Properties: Lipid Composition Gel-liquid phase transition occurs in a narrow temperature range for pure lipids (T c ) T c is affected by : Fatty acid side chains Degree of unsaturation Chain length of Polar head group

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Active Moiety The “active moiety” is the drug (e.g., doxorubicin, amphotericin B) responsible for the therapeutic effect. The lipids are “functional excipients.” All approved liposome drug products use drugs already approved in other dosage forms.

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Storage and Reconstitution Liposome preparations can be stored: frozen, in liquid form as a lyophilized powder. Reconstitution of lyophilized liposomes may affect particle size and size distribution.

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Drug Release Release controlled by: Fluidity/stability (lipids/co-lipids): Size: MLV or a SUV Physicochemical properties of drug Drug/lipid interaction

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Electron Micrograph of lyophilized liposomes

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Why Use Liposomes in Drug Delivery? Inactive: Unmodified liposomes gather in specific tissue reticuloendothelial system Active: alter liposome surface with ligand (antibodies, enzymes, protein A, sugars) Physical: temperature or pH sensitive liposomes directly to site Drug Targeting :

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- Affect the time in which the drug is released - Prolong time -increase duration of action and decrease administration - Dependent on drug and liposome properties Conti..

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Modes of Liposome/Cell Interaction Adsorption Endocytosis Fusion Lipid transfer

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Classes of Liposomes Conventional Long circulating Immuno Cationic

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Various liposomal drug preparations Type of Agents Examples Anticancer Drugs Anti bacterial Antiviral DNA material Enzymes Radionuclide Fungicides Vaccines *Currently in Clinical Trials or Approved for Clinical Use Malaria merozoite, Malaria sporozoite Hepatitis B antigen, Rabies virus glycoprotein Amphotericin B* In-111*, Tc-99m Hexosaminidase A , Glucocerebrosidase, Peroxidase Duanorubicin, Doxorubicin *, Epirubicin Methotrexate, Cisplatin*, Cytarabin Triclosan, Clindamycin hydrochloride, Ampicillin, peperacillin, rifamicin AZT cDNA - CFTR*

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Problems with Liposomal Preparations of Drugs - Fungizone $40.58 Amphotec $2334 - Lack long term stability (short shelf life) - Freeze dry and pH adjustment - Low “Pay Load” - Physical and chemical instability - Polar drugs and drugs without opposite charge - Modifications

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Thanks Priyanka Rathore Assistant Professor priyankarathore1jan@gmail.com Dr. S. Nayak Principal & Professor Principal.bcp@gmail.com BANSAL COLLEGE OF PHARMACY, BHOPAL www.bansalpharmacy.com

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