Transporter-Targeted Bile Acid-Camptothecin Conjugate for Improved Oral Absorption.

Transporter-Targeted Bile Acid-Camptothecin Conjugate for Improved Oral Absorption.
Chem Pharm Bull (Tokyo). 2019 Aug 06;:
Authors: Xiao L, Zhou Y, Zhang X, Ding Y, Li Q
Abstract
Camptothecin (CPT), a natural alkaloid, possesses potent anticancer activity. However, its application was terminated due to its low bioavailability and high toxicity. This work evaluated the potential of deoxycholic acid-CPT conjugate (G2) to improve the oral absorption of CPT. Deoxycholic acid significantly reduced cytotoxicity and inhibited the uptake of G2, in vitro. And G2 showed sodium-dependent uptake. In addition, in vivo study in rats indicated that the oral bioavailability of G2 was 2.06-fold higher than that of CPT. The present study suggested that using bile acid as the conjugated moiety is a hopeful strategy to improve the oral bioavailability of CPT.
PMID: 31391385 [PubMed - as supplied by publisher]

Source: Chemical and Pharmaceutical Bulletin - August 5, 2019 Category: Drugs & Pharmacology Authors: Xiao L, Zhou Y, Zhang X, Ding Y, Li Q Tags: Chem Pharm Bull (Tokyo) Source Type: research