Poloxamer 407/188 Binary Thermosensitive Gel as a Moxidectin Delivery System: In Vitro Release and In Vivo Evaluation

作者：Xiangchun Ruan, Jidong Hu, LU Lian-shou, Youwei Wang, Chun‐lian Tang, Faquan Liu, Xiuge Gao, Li Zhang, Hao Wu, Huang XianHui, Qing Wei · 发表于：Molecules · 年份：2022 · DOI：10.3390/molecules27103063 · 被引用次数：25 · 研究领域：Helminth infection and control、Drug Solubulity and Delivery Systems、Surgical Sutures and Adhesives

Moxidectin (MXD) is an antiparasitic drug used extensively in veterinary clinics. In this study, to develop a new formulation of MXD, a thermosensitive gel of MXD (MXD-TG) was prepared based on poloxamer 407/188. Furthermore, the gelation temperature, the stability, in vitro release kinetics and in vivo pharmacokinetics of MXD-TG were evaluated. The results showed that the gelation temperature was approximately 27 °C. MXD-TG was physically stable and can be released continuously for more than 96 h in vitro. The Korsmeyer−Peppas model provided the best fit to the release kinetics, and the release mechanism followed a diffusive erosion style. MXD-TG was released persistently for over 70 days in sheep. Part of pharmacokinetic parameters had a difference in female and male sheep (p < 0.05). It was concluded that MXD-TG had a good stability, and its release followed the characteristics of a diffusive erosion style in vitro and a sustained release pattern in vivo.