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Liposomes: Introduction, Structural Composition, Types, Preparation & Characterization

Introduction:

  • Liposomes are tiny spherical vesicles, which have been widely used as delivery systems for a range of bioactive molecules.

  • They are formed when certain lipid molecules are hydrated in an aqueous environment.

  • Their structure resembles that of cell membranes, making them biocompatible and capable of interacting with human cells in various ways.

Structural Composition:

  • Liposomes consist of an aqueous core surrounded by one or multiple concentric lipid bilayers.

  • These lipid layers are composed primarily of phospholipids, which naturally organize into a bilayer structure when exposed to water due to their amphiphilic nature. Each phospholipid molecule consists of a hydrophilic "head" and two hydrophobic "tails".

  • The tails associate with each other, forming the internal section of the bilayer, while the hydrophilic heads face outwards, interacting with the surrounding aqueous environment.

Types of Liposomes:

Based on size and the number of lipid bilayers, liposomes can be categorized into:

1. Small Unilamellar Vesicles (SUVs):

  • These are small vesicles with a single bilayer. They typically range from 20 to 100 nm in diameter.

2. Large Unilamellar Vesicles (LUVs):

  • These have a single bilayer but are larger than SUVs, with diameters usually ranging from 100 to 1000 nm.

3. Multilamellar Vesicles (MLVs):

  • These consist of multiple concentric lipid bilayers. They typically resemble an "onion structure" and are larger, usually ranging from 500 nm to several micrometers in diameter.

4. Multivesicular Vesicles (MVVs):

  • These are large vesicles containing many smaller vesicles inside them.

Preparation of Liposomes

here's a concise summary of the preparation of liposomes for targeted drug delivery:

  1. Lipid Selection: Choose appropriate lipids, like phosphatidylcholine, and possibly cholesterol for stability. Include targeting ligands if specific targeting is desired.

  2. Liposome Formation:

    1. Thin Film Hydration: Dissolve lipids in an organic solvent, create a thin lipid film by evaporating the solvent, and hydrate the film with an aqueous solution (containing the drug).

    2. Other Methods: Use techniques like reverse-phase evaporation, solvent injection, or microfluidic methods, depending on the required liposome characteristics.

  1. Size Reduction and Homogenization: Utilize methods like sonication, extrusion, or high-pressure homogenization to achieve uniform liposome size.

  2. Purification: Remove unencapsulated drugs and solvents through dialysis, centrifugation, or size-exclusion chromatography.

  3. Characterization: Assess liposome size, stability, encapsulation efficiency, and drug release profile.

  4. Functionalization for Targeting: Attach targeting ligands to liposome surface if targeted delivery is required.

Liposomes can be prepared using several methods, including:


1. Thin Film Hydration:

  • This involves evaporating a solvent from a lipid solution to form a thin film of lipid, which is then hydrated with an aqueous solution.

2. Sonication:

  • This method uses ultrasonic waves to break down larger liposomal structures into smaller vesicles.

3. Extrusion:

  • In this method, a liposome suspension is forced through a polycarbonate membrane to control vesicle size.

Characterization of Liposomes

  • Liposomes are small spherical vesicles composed of one or more phospholipid bilayers surrounding an aqueous core.

  • They can encapsulate both hydrophilic (in the aqueous core) and hydrophobic (within the lipid bilayer) drugs.

1. Size and Lamellarity:

  • Liposomes can be unilamellar (single bilayer) or multilamellar (multiple concentric bilayers).

  • Their size can range from nanometers (nanosomes) to micrometers.

2. Surface Charge:

  • Based on the lipids used, liposomes can be cationic, anionic, or neutral.

3. Composition:

  • The specific phospholipids and cholesterol content.

4. Drug Entrapment Efficiency:

  • The efficiency with which the drug is encapsulated within the liposome.

5. Release Profile:

  • The rate and mechanism by which the drug is released from the liposome.



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