泊洛沙姆 407/188 二元温敏凝胶作为莫昔克丁传递系统：体外释放和体内评价。
Poloxamer 407/188 Binary Thermosensitive Gel as a Moxidectin Delivery System: In Vitro Release and In Vivo Evaluation.
机构信息
Laboratory of Veterinary Pharmacology and Toxicology, College of Animal Science and Technology, Anhui Agricultural University, Hefei 230036, China.
China Institute of Veterinary Drug Control, Beijing 100081, China.
出版信息
Molecules. 2022 May 10;27(10):3063. doi: 10.3390/molecules27103063.
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.
莫昔克丁（MXD）是一种广泛用于兽医诊所的抗寄生虫药物。在这项研究中，为了开发 MXD 的新制剂，基于泊洛沙姆 407/188 制备了 MXD 的温敏凝胶（MXD-TG）。此外，还评估了 MXD-TG 的胶凝温度、稳定性、体外释放动力学和体内药代动力学。结果表明，胶凝温度约为 27°C。MXD-TG 在物理上是稳定的，可以在体外持续释放超过 96 小时。Korsmeyer-Peppas 模型最适合描述释放动力学，释放机制遵循扩散侵蚀模式。在绵羊中，MXD-TG 持续释放超过 70 天。部分药代动力学参数在雌性和雄性绵羊中存在差异（p<0.05）。结论是，MXD-TG 具有良好的稳定性，其体外释放遵循扩散侵蚀模式的特征，体内呈现持续释放模式。
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