Preparation, in vitro and in vivo Evaluation of Isoliquiritigenin-loaded TPGS modified proliposomes

Publication date: Available online 16 March 2019Source: International Journal of PharmaceuticsAuthor(s): Jian Liu, Qilong Wang, Michael Adu-Frimpong, Qiuyu Wei, Yujiao Xie, Kangyi Zhang, Chunmei Wei, Wen Weng, Hao Ji, Elmurat Toreniyazov, Ximing Xu, Jiangnan YuAbstractIsoliquiritigenin (ISL) has a great variety of pharmacological effects especially liver cancer therapy, but its poor solubility, bioavailability and liver targeting have limited its clinical use. In order to solve the aforementioned shortcomings, the TPGS-modified proliposomes loaded with ISL (ISL-TPGS-PLP) was prepared in this study. ISL-TPGS-PLP was fabricated via thin-film dispersion method and was characterized by the appearance, particle size, zeta potential and morphology. HPLC was used to evaluate entrapment efficiency (EE), in vitro release and stability of ISL-TPGS-PLP single or combined while appropriate physicochemical parameters were measured with DLS. Meanwhile, the pharmacokinetics and tissue distribution were also studied after oral administration. The results demonstrated that ISL-TPGS-PLP had a mean size of 23.8±0.9 nm, high EE of 97.33±0.40%. More importantly, nearly 90% ISL was released from ISL-TPGS-PLP within 24 hours while only 50% was released from ISL suspension. In the pharmacokinetics study, the area under the curve (AUC0-24h) of ISL-TPGS-PLP was 1.53 times higher than that of ISL suspension. The Tissue distribution study showed that the ISL released from ISL-TPGS-PLP was ...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research

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