Chongqing Academy of Chinese Materia Medica, No.34 of Nanshan Road, Nanan District, Chongqing, 400065, China.
Chengdu University of TCM, Chegndu, 611137, China.
BMC Biotechnol. 2022 May 27;22(1):16. doi: 10.1186/s12896-022-00746-6.
The aim of the present study is to increase the solubility of dihydroartemisinin (DHA) using the self-emulsifying drug delivery system (SEDDS).
We first conducted solubility test and ternary phase diagram, then, in order to optimize the formulation of the DHA self-emulsifying agent, the design mixture method was selected in the design expert software. Next, optimal prescription validation and preliminary formulation evaluation were conducted. By comparing the oil-water partition coefficient in vitro, the improvement of the in vivo osmotic absorption of DHA via self-emulsification was evaluated.
The optimal prescription ratio of oleic acid polyethylene glycol glyceride, polyoxyethylene hydrogenated castor oil, and diethylene glycol monoethyl ether in the DHA self-emulsifying preparation = 0.511:0.2:0.289 (w/w/w), with a drug-loading capacity of 26.3634 mg/g, solubility of 2.5448 mg/ml, and self-emulsification time of 230 s. The solubility self-emulsification was approximately 20.52 × higher in DHA than in the crude drug. The self-emulsification could improve DHA permeability and promoting in vivo DHA absorption.
The DHA SEDDS could significantly improve DHA solubility and in vivo absorption.
本研究旨在通过自乳化药物传递系统（SEDDS）来提高二氢青蒿素（DHA）的溶解度。
我们首先进行了溶解度试验和三元相图，然后，为了优化 DHA 自乳化剂的配方，我们在设计专家软件中选择了设计混合方法。接下来，进行了最佳处方验证和初步配方评估。通过比较体外油水分配系数，评估了通过自乳化提高 DHA 体内渗透吸收的效果。
DHA 自乳化制剂中油酸聚乙二醇甘油酯、聚氧乙烯氢化蓖麻油和二乙二醇单乙基醚的最佳处方比例为 0.511:0.2:0.289（w/w/w），载药量为 26.3634 mg/g，溶解度为 2.5448 mg/ml，自乳化时间为 230 s。DHA 的溶解度自乳化约为原料药的 20.52 倍。自乳化可以提高 DHA 的通透性，促进体内 DHA 的吸收。
DHA SEDDS 可以显著提高 DHA 的溶解度和体内吸收。
