title: Lymphatic transport of orally administered probucol-loaded mPEG-DSPE micelles.
abstract: BACKGROUND
  Transporting drugs through the lymphatic system has attracted increasing attention. Lipid-based formulations have been proved to be an effective way to improve systemic bioavailability of highly lipophilic drugs by increasing intestinal lymphatic transport.
  
  
  OBJECTIVE
  The formulation of polymer micelle was developed for probucol to improve its intestinal lymphatic transport.
  
  
  METHODS
  Methoxy-polyethylenelglycol-distearyl phosphatidyl-ethanolamine (mPEG-DSPE) polymer was chosen to develop the micelles for probucol. The physicochemical properties were characterized. Caco-2 cell model, unconscious and conscious lymph duct cannulated rat models were established for in vitro and in vivo evaluation of lymphatic transport.
  
  
  RESULTS
  In vitro evaluation in the Caco-2 cell model showed that the micellar formulation could significantly increase the uptake and transport of probucol. The study in unconscious and conscious lymph duct cannulated rat models further verified the significant enhancement of lymphatic transport of probucol by mPEG-DSPE micelles.
  
  
  CONCLUSIONS
  These results suggested that mPEG-DSPE micellar formulation could provide a useful alternative approach for improving the lymphatic transport of hydrophobic compounds.
authors: a Department of Pharmaceutics , School of Pharmacy, Fudan University , Shanghai , People's Republic of China and.|b Key Laboratory of Smart Drug Delivery , Ministry of Education , Shanghai , People's Republic of China.
authors: Limei
authors: L
authors: Han
authors: a Department of Pharmaceutics , School of Pharmacy, Fudan University , Shanghai , People's Republic of China and.|b Key Laboratory of Smart Drug Delivery , Ministry of Education , Shanghai , People's Republic of China.
authors: Qiushi
authors: Q
authors: Yang
authors: a Department of Pharmaceutics , School of Pharmacy, Fudan University , Shanghai , People's Republic of China and.|b Key Laboratory of Smart Drug Delivery , Ministry of Education , Shanghai , People's Republic of China.
authors: Teng
authors: T
authors: Shen
authors: a Department of Pharmaceutics , School of Pharmacy, Fudan University , Shanghai , People's Republic of China and.|b Key Laboratory of Smart Drug Delivery , Ministry of Education , Shanghai , People's Republic of China.
authors: Jin
authors: J
authors: Qing
authors: a Department of Pharmaceutics , School of Pharmacy, Fudan University , Shanghai , People's Republic of China and.|b Key Laboratory of Smart Drug Delivery , Ministry of Education , Shanghai , People's Republic of China.
authors: Jianxin
authors: J
authors: Wang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D018938:Caco-2 Cells / Q000737:chemistry* / Q000378:metabolism; D004337:Drug Carriers; D006801:Humans; D007408:Intestinal Absorption; D008208:Lymphatic System / Q000737:chemistry* / Q000187:drug effects*; D008823:Micelles; D010714:Phosphatidylethanolamines / Q000737:chemistry* / Q000493:pharmacokinetics; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000493:pharmacokinetics; D011341:Probucol / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats
chemical_list: D004337:Drug Carriers; D008823:Micelles; D010714:Phosphatidylethanolamines; C107570:polyethylene glycol-distearoylphosphatidylethanolamine; D011092:Polyethylene Glycols; D011341:Probucol
keywords: Lymph duct cannulated rat model; lymphatic transport; mPEG-DSPE; micelles; probucol