[The influence of absorption enhancer and preparation of paclitaxel on its intestinal mucous membrane permeation detected by enhancement by using electron spin resonance technique].
OBJECTIVE
To investigate the permeation mechanism of paclitaxel by enhancers and preparation factors.


METHODS
The 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.


RESULTS
Polyethylene 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.


CONCLUSIONS
Characteristics of enhancing intestinal absorption of poor dissolution drug had been provided with enhancer the change of membrane fluid.
Zhang
Xue-Nong
XN
College of Pharmacy, Soochow University, Suzhou 215007, China. zhangxuenong@163.com
Tang
Li-Hua
LH
Yan
Xue-Ying
XY
Zhang
Qiang
Q
D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004357:Drug Synergism; D004578:Electron Spin Resonance Spectroscopy; D004655:Emulsions; D007267:Injections; D007408:Intestinal Absorption / Q000187:drug effects*; D007413:Intestinal Mucosa / Q000187:drug effects*; D008560:Membrane Fluidity / Q000187:drug effects*; D017239:Paclitaxel / Q000008:administration & dosage / Q000493:pharmacokinetics*; D014677:Pharmaceutical Vehicles / Q000494:pharmacology; D010743:Phospholipids / Q000494:pharmacology; D011092:Polyethylene Glycols / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D047392:beta-Cyclodextrins / Q000494:pharmacology
D000972:Antineoplastic Agents, Phytogenic; D004655:Emulsions; D014677:Pharmaceutical Vehicles; D010743:Phospholipids; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D011092:Polyethylene Glycols; D017239:Paclitaxel