Industrial Chemistry Mr Yassen AL-Quasmi

Prepared By : Wafaa M Ashour Anwar AL-Daghameen

WHAT Is A LIPOSOME

• Liposomes Are Small, Spherical Vesicles Which Consist Of Amphilic Lipids, Enclosing An Aqueous Core. These Are Phospholipids Which Form Bilayers Similar To Those Found Biomembranes.

ADVANTAGES

• Biocompatible , Completely Biodegradable ,Non-toxic.

• Liposomes Supply Both A Lipophilic Enviroment And Aqueous . Can Protect Encapsulated Drug.

• Reduce Exposure Of Sensitive Tissues To Toxic Drugs.

• Alter The pharmacokinetic property of Drugs(Reduced Elimination, Increased Circulation Life Time )

• Flexibility To Couple With Site Specific Ligands To Achieve Active Targeting (Anticancer Drug)

• Can Be Formulated Into Multiple Dosage forms.

DISADVANTAGES

• Production Cost Is High• Leakage And Fusion Of Encapsulated Drug• Sometimes Phospholipid Undergoes Oxidation

And Hydrolysis Like Reaction• Short Half-Life• Low solubility

• An Artificial Microscopic Vesicle Consisting Of An Aqueous Core Enclosed In One Or More Phospholipid Layers, Used To Convey Vaccines, Drugs, Enzymes, Or Other Substances To Target Cells Or Organs.

• In Most Cases The Major Component Is Phosphatidyl Choline. Depending On The Processing Conditions And The Chemical Compostion , Liposomes Are Formed With One Or Several Concentric Bilayers.

COMPOSITION OF LIPOSOME1. PHOSPHOLIPID

Naturally Occuring Phospholipids Used In Liposomes Are :

• PhosphatidylCholine• PhosphatidylEthanolamine• PhosphatidylSerineSynthetic Phospholipids Used In The Liposomes

Are:• Dioleoyl PhosphatidylCholine• Disteroyl PhoshatidylCholine • Dioleoyl PhosphatidylEthanolamine• Distearoyl PhosphatidyleEhanolamine

PHOSPHATIDYLCHOLINE (PC)• Phosphatidylcholine is an amphipathic molecule

in which exists - a hydrophilic polar head group,

phoshocholine. - a glycerol bridge. - a pair of hydrophopic acyl hydrocarbon

chain.

B. CHOLESTEROLFLUIDITY BUFFER

• Stablize the membrane.• Being an amphiphathic molecule, cholesterol

inserts into the membrane with its hydroxyl group of cholesterol oriented towards the aqueous surface and aliphatic chain aligned parallel to the acyl chains in the center of the bilayer.

CLASSIFICATION

• Structural Parameters• Method Of Preparation• Composition And Application

Based on Structural Parameters

MVVMultivesicularVesicles(.1um)

UV Unilamellar Vesicles

OLV oligolamellar vesicles(0,1-

1um)

MLV Multilamellar Vesicles(>0.5u

m)

GUV Giant Unilamellar

Vesicles(>1um)

LUV Large Unilamellar

Vesicles (>100nm)

SUV Small Unilamellar Vesicles (20-

100nm)

MUV Medium Unilamellar

Vesicles

Based on method

preparation

REV, SUV made by reverse phase evaporation

method

SPLV stable

plurilamenar

vesicles

VET Vesicles

prepared by

extrusion tech

FATMLV Frozen and thawed MLV

Composition and

Application

Conventional

PH sensitive

cationic

Long circulatory

fusogenicimmuno

LAMELLA

Lamella: A Lamella Is A Flat Plate Like Structure That Appears During The Formation Of Liposomes. The Phospholipid Bilayer First Exists As A Lamella Before Getting convered Into Spheres.

Based On Number Of Lamella There Are Two Types:

1. Unilamellar Vesicles2. Multilamellar Vesicles

DETERGENT DISPERTION

• Phospholipids And Aqueous Phase Comes In Contact With The Help Of Detergent.

CHARACTERIZATION OF LIPOSOME

• PHYSICAL1. Vesicle Shape And Lamellarity2. Vesicle size3. Surface Charge4. Druge Release5. Entrapped Volume : (Water Content Is

Determined)6. Encapsulation efficiency

CHEMICAL CHARACTREIZATION1. Quantitative Determination Of Phospholipids2. Phospholipd Hydrolysis3. Phospholipid Oxidation4. Cholesterol analysis

Application

• Pharmaceutical Application• Liposome can serve as an excellent drug-

delivery vehicle to the cell.• Liposome Can Be Used For Drug Targeting,

Anticancer drug.• Liposomes Can Be Applied To Protect The

Entrapped drug. against enzymatic degradation. as penicillins sensitive to beta lactamase ,protection encapsulated by liposome.

• Food application Stablization of food Components Against

Degradation ,Enhanced Efficiency of Antimicrobial peptides.

• Cosmetics Application Reduce The Dryness Of The Skin Treatment Of Hair Loss