PVP and surfactant combined carrier as an effective absorption enhancer of poorly soluble astilbin in vitro and in vivo.
BACKGROUND
Astilbin is considered to be a new and promising immunosuppressant for immune related diseases, but limited in clinical application due to its poor water solubility, difficult oral absorption and low bioavailability.


OBJECTIVE
The present work studied the effect of PVP and surfactant combined carrier on its capability to improve drug absorption.


METHODS
PVP K30-Tween 80 combined carries was applied into the astilbin solid dispersions, tested both in vivo in beagle dogs and in vitro in transport experiments across Caco-2 cell monolayers.


CONCLUSIONS
In the animal studies a many fold increase in plasma AUC was observed for the solid dispersions of drug in PVP K30-Tween 80 combined carries compared to active pharmaceutical ingredient (API). The applicability of Caco-2 monolayers as a tool for predicting the in vivo transport behavior of Astilbin in combination with a solubility enhancing carries was shown. In vitro transport studies confirmed the effect of combined carries on the absorption behavior of the astilbin. MTT studies showed the cell viability gradually decreased with the increase of the drug concentration in a dose dependent manner for astilbin and that in solid dispersions. The permeability and apparent permeability coefficients (Papp) increased with drug in the Caco-2 cell.


CONCLUSIONS
In this study, it was found that PVP K30 and Tween 80 promoted the permeability of drugs best within a certain amount. For astilbin PVP K30 and surfactant combined carrier had a strong potential to improve oral bioavailability.
School of Chemical Engineering and Light Industry , Guangdong University of Technology, Guangzhou, Guangdong, PR China .
Yan
Y
He
Hongfei
H
Liu
Zhiyong
Z
Xie
Qiongfeng
Q
Liao
Xiaoping
X
Lai
Zhiyun
Z
Du
D000284:Administration, Oral; D000818:Animals; D018938:Caco-2 Cells; D018592:Cross-Over Studies; D004285:Dogs; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D005260:Female; D044948:Flavonols / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects* / Q000502:physiology; D008297:Male; D011136:Polysorbates / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D011145:Polyvinyls / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D011759:Pyrrolidines / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D012995:Solubility; D013237:Stereoisomerism; D013501:Surface-Active Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism
D004337:Drug Carriers; D044948:Flavonols; D011136:Polysorbates; D011145:Polyvinyls; D011759:Pyrrolidines; D013501:Surface-Active Agents; C505150:poly(N-vinylpyrrolidine); C099069:astilbin