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Chitosan-coated liposomes: characterization and interaction with leuprolide
1Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China.
International Journal of Pharmaceutics
|July 5, 2003
Summary
Chitosan coating affects liposome properties. Low purity lipids form thicker, more stable coatings, but lead to greater drug leakage, impacting leuprolide delivery.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Biotechnology
Background:
- Liposomes are widely used drug delivery systems.
- Chitosan coating can enhance liposome properties.
- Understanding lipid type and chitosan concentration effects is crucial for optimizing liposomal formulations.
Purpose of the Study:
- To investigate how chitosan concentration and lipid purity influence chitosan-coated liposomes.
- To analyze the interaction between chitosan and liposomes with varying lipid purity.
- To evaluate the impact on physical characteristics, drug entrapment, and stability of leuprolide-loaded liposomes.
Main Methods:
- Preparation of liposomes using high and low purity lipids.
- Coating of liposomes with varying concentrations of chitosan.
- Characterization of physical properties (particle size, zeta potential).
- Assessment of drug entrapment efficiency and stability upon dilution.
Main Results:
- Liposomes from low purity lipid exhibited larger particle size increases and higher zeta potential, indicating thicker chitosan coatings and better resistance to flocculation.
- High purity lipid liposomes showed polymer bridging flocculation at low chitosan concentrations and steric stabilization at high concentrations.
- Drug entrapment efficiency decreased with increasing chitosan concentration due to bilayer disturbance.
- Leuprolide leakage upon dilution was greater from low purity lipid liposomes.
Conclusions:
- Low purity lipids, with their higher negative charge, form thicker adsorptive layers via stronger electrostatic attraction with chitosan.
- Chitosan interaction with phospholipid head groups can disrupt bilayers, affecting leuprolide entrapment and leading to leakage.
- Lipid purity significantly impacts chitosan coating effectiveness and drug retention in liposomal formulations.