Abstract
Objective: In order to prolong the duration of drug in the circulation, multivesicular liposome (MVL, namely DepoFoam™) was utilized as a sustained-release delivery system for hydroxycamptothecin (HCPT). Methods: HCPT is insoluble in both water and physiological acceptable organic solvents; therefore, HCPT–phospholipid complex (HCPT–PCC) was prepared by solvent evaporation method to improve its liposolubility. In this study, preparation, characterization, in vitro release, and in vivo pharmacokinetics of HCPT–phospholipid complex-loaded MVLs (HCPT-MVLs) were investigated. Results: The results showed that the average particle size of HCPT-MVL was 9 μm and the encapsulation efficiency was 90%. In addition, HCPT-MVLs could improve both in vitro release and in vivo pharmacokinetic behaviors of the original drug, with a sustained release of drugs over 5–6 days. Conclusion: These data suggested that by combined use of DepoFoam™ and phospholipid complex formation technique HCPT could be successfully entrapped into the MVLs, which might provide a paradigm for sustained release of insoluble drugs.
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