The role of pH and ring-opening hydrolysis kinetics on liposomal release of topotecan.

ABSTRACT: The use of liposomal delivery systems for the treatment of cancer has been extensively researched because of their passive targeting to the vasculature of solid tumors. While their potential to provide prolonged retention and high drug encapsulation is desirable for anticancer agents, a mechanistic understanding is required to optimize and design liposomal drug delivery systems capable of controllable release tailored to tumor type and patient. Topotecan (TPT) is a topoisomerase I inhibitor that undergoes reversible, pH-sensitive ring-opening hydrolysis. TPT may benefit from liposomal formulation using active loading strategies to generate low intravesicular pH to prolong drug retention and increase drug encapsulation. This paper develops a mathematical model to describe TPT's permeability

SUBMITTER: Fugit KD 

PROVIDER: S-EPMC4104781 | biostudies-literature | 2014 Jan

REPOSITORIES: biostudies-literature