title: [The influence of absorption enhancer and preparation of paclitaxel on its intestinal mucous membrane permeation detected by enhancement by using electron spin resonance technique].
abstract: 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.
authors.affiliation: College of Pharmacy, Soochow University, Suzhou 215007, China. zhangxuenong@163.com
authors.forename: Xue-Nong
authors.initials: XN
authors.lastname: Zhang
authors.forename: Li-Hua
authors.initials: LH
authors.lastname: Tang
authors.forename: Xue-Ying
authors.initials: XY
authors.lastname: Yan
authors.forename: Qiang
authors.initials: Q
authors.lastname: Zhang
mesh_terms: 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
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004655:Emulsions; D014677:Pharmaceutical Vehicles; D010743:Phospholipids; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D011092:Polyethylene Glycols; D017239:Paclitaxel