Enhancement of water-solubility and bioactivity of paclitaxel using modified cyclodextrins.
We investigated the aqueous solubility of paclitaxel using 11 kinds of cyclodextrins (CDs) and the bioactivity of the paclitaxel-CD inclusion complex. 2,6-Dimethyl beta-cyclodextrin was the most effective and its solubility was 2.3 mM in a 0.1 M 2,6-dimethyl beta-cyclodextrin aqueous solution. The inclusion complex of paclitaxel and 2,6-dimethyl beta-cyclodextrin had a 1.23-fold polymerization activity as paclitaxel in a tubulin assay.
Hamada
Hiroki
H
Department of Life Science, Okayama University of Science, 1-1 Ridai-cho, Okayama 700-0005, Japan. hamada@das.ous.ac.jp
Ishihara
Kohji
K
Masuoka
Noriyoshi
N
Mikuni
Katsuhiko
K
Nakajima
Nobuyoshi
N
D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry; D003505:Cyclodextrins / Q000737:chemistry*; D004355:Drug Stability; D017239:Paclitaxel / Q000737:chemistry*; D012995:Solubility; D012996:Solutions; D014867:Water / Q000737:chemistry*
D000972:Antineoplastic Agents, Phytogenic; D003505:Cyclodextrins; D012996:Solutions; D014867:Water; D017239:Paclitaxel