Preparation and evaluation of self-microemulsifying drug delivery system of oridonin.
The objective of this study was to develop self-microemulsifying drug delivery system (SMEDDS) to enhance the oral bioavailability of the poorly water-soluble drug, oridonin. The influence of the oil, surfactant and co-surfactant types on the drug solubility and their ratios on forming efficient and stable SMEDDS were investigated in detail. The SMEDDS were characterized by morphological observation, droplet size and zeta-potential determination, cloud point measurement and in vitro release study. The optimum formulation consisted of 30% mixture of Maisine 35-1 and Labrafac CC (1:1), 46.7% Cremopher EL, and 23.3% Transcutol P. Invitro release test showed a complete release of oridonin from SMEDDS in an approximately 12h. The absorption of oridonin from SMEDDS showed a 2.2-fold increase in relative bioavailability compared with that of the suspension. Our studies demonstrated the promising use of SMEDDS for the delivery of oridonin by the oral route.
Zhang
Ping
P
School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 210203, PR China.
Liu
Ying
Y
Feng
Nianping
N
Xu
Jie
J
D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D045786:Diterpenes, Kaurane / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D004339:Drug Compounding; D016503:Drug Delivery Systems; D004563:Electrochemistry; D004655:Emulsions; D007202:Indicators and Reagents; D008297:Male; D046529:Microscopy, Electron, Transmission; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry
D000972:Antineoplastic Agents, Phytogenic; D045786:Diterpenes, Kaurane; D004655:Emulsions; D007202:Indicators and Reagents; D009821:Oils; D013501:Surface-Active Agents; C011959:oridonin