Designing a novel in vitro drug-release-testing method for liposomes prepared by pH-gradient method

In order to evaluate the drug-release behavior from pH-gradient liposomal formulation, a simple release-testing method without using biological components was newly designed on the basis of inversed ammonia gradient principle. Various factors influencing drug-release (releasing factor) were examined...

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Bibliographic Details
Published in:International journal of pharmaceutics 2012-07, Vol.430 (1-2), p.381-387
Main Authors: Nakamura, Koji, Yoshino, Keisuke, Yamashita, Keiko, Kasukawa, Hiroaki
Format: Article
Language:English
Subjects:
ammonia
Ammonia - chemistry
Antineoplastic Agents - chemistry
Chemistry, Pharmaceutical
cholesterol
Delayed-Action Preparations
Doxorubicin - chemistry
Drug-release test
drugs
Hydrogen-Ion Concentration
Inversed ammonia gradient principle
Kinetics
lipid composition
Lipids - chemistry
Liposome
Liposomes
manufacturing
Molecular Structure
Osmolar Concentration
osmolarity
pH-gradient loading method
quality control
researchers
Solubility
Sustained release
Technology, Pharmaceutical - methods
Vincristine - chemistry
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Summary:In order to evaluate the drug-release behavior from pH-gradient liposomal formulation, a simple release-testing method without using biological components was newly designed on the basis of inversed ammonia gradient principle. Various factors influencing drug-release (releasing factor) were examined. As a result, releasing factor's concentration, pH, osmolarity in test fluid, and releasing factor's structure were found to be the critical factors to be optimized. Various vincristine-loaded liposomes with different lipid compositions or with different lipid/cholesterol ratio were tested for drug-release behavior and successfully obtained drug-release profiles reflecting differences in the physicochemical properties of individual liposomes. Furthermore, since the comparative release study of vincristine-loaded liposomes and doxorubicin-loaded liposomes could reproduce the phenomena as other researchers recently reported, a possibility was suggested for the proposed method to estimate the physicochemical status of drug inside of liposomes. Proof of concept study concluded, as a whole, that the novel release-testing method would be useful for a formulation study and also useful as a tool for the quality assurance or quality control in the manufacturing of pH-gradient liposomal products.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2012.04.011