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Stabilization of topotecan in low pH liposomes composed of distearoylphosphatidylcholine

✍ Scribed by Thomas G. Burke; Xiang Gao

Book ID
102413357
Publisher
John Wiley and Sons
Year
1994
Tongue
English
Weight
310 KB
Volume
83
Category
Article
ISSN
0022-3549

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✦ Synopsis

Topotecan is a promising anticancer agent presently undergoing clinical evaluation worldwide. Topotecan, camptothecin, 9-aminocamptothecin, and CPT-11 have aroused considerable interest in recent years for their ability to halt the growth of a wide range of human tumors. For each analogue an important structural requirement for biological activity is a closed a-hydroxy lactone ring moiety. Unfortunately, this functionality hydrolyses rapidly in aqueous solution under physiological conditions (i.e. pH 7 or above), resulting in an inactive carboxylate form of the drug. In this report, we demonstrate that topotecan's half-life in human plasma (pH 7.6) can be enhanced

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