The influence of absorption enhancer and preparation of paclitaxel on its intestinal mucous membrane permeation detected by enhancement by using electron spin resonance technique.
- Author:
Xue-Nong ZHANG
1
;
Li-Hua TANG
;
Xue-Ying YAN
;
Qiang ZHANG
Author Information
- Publication Type:Journal Article
- MeSH: 2-Hydroxypropyl-beta-cyclodextrin; Animals; Antineoplastic Agents, Phytogenic; administration & dosage; pharmacokinetics; Drug Synergism; Electron Spin Resonance Spectroscopy; Emulsions; Injections; Intestinal Absorption; drug effects; Intestinal Mucosa; drug effects; Membrane Fluidity; drug effects; Paclitaxel; administration & dosage; pharmacokinetics; Pharmaceutical Vehicles; pharmacology; Phospholipids; pharmacology; Polyethylene Glycols; pharmacology; Rats; Rats, Sprague-Dawley; beta-Cyclodextrins; pharmacology
- From: Acta Pharmaceutica Sinica 2005;40(9):861-864
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo investigate the permeation mechanism of paclitaxel by enhancers and preparation factors.
METHODSThe fluidity of mucous membrane and membrane protein conformation changes were determined by using electron spin resonance (ESR) when mucous membrane was treated by several enhancers. At the same time, the factors of penetration of lower dissolution drug across the intestinal mucous membrane were studied in three formulas inclusion complex, microemulsion and injection.
RESULTSPolyethylene glycol (PEG) 1500, hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and phospholipid as enhancers could reinforce the permeation of paclitaxle because of loosening of protein conformation in intestinal mucous membrane. Paclitaxel-HP-beta-CD inclusion complex and paclitaxel microemulsion as vehicle could significantly increased permeation kinetic rate of paclitaxel with fluid diffuse method.
CONCLUSIONCharacteristics of enhancing intestinal absorption of poor dissolution drug had been provided with enhancer the change of membrane fluid.
