Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt, End of 90th street, Fifth settlement, New Cairo, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Kasr El-Aini Street, Cairo, Egypt.
AAPS PharmSciTech. 2018 Apr;19(3):1001-1010. doi: 10.1208/s12249-017-0897-8. Epub 2017 Nov 6.
Non-ionic surfactant (NIS) based in situ forming vesicles (ISVs) present an affordable alternative to the traditional systems for the parenteral control of drug release. In this work, NIS based ISVs encapsulating tenoxicam were prepared using the emulsion method. Tenoxicam-loaded ISVs were prepared using a 2.3 full factorial experimental design, where three factors were evaluated as independent variables; type of NIS (A), molar ratio of NIS to Tween®80 (B), and phase ratio of the internal ethyl acetate to the external Captex® oil phase (C). Percentage drug released after 1 h, particle size of the obtained vesicles and mean dissolution time were chosen as the dependent variables. Selected formulation was subjected to morphological investigation, injectability, viscosity measurements, and solid state characterization. Optimum formulation showed spherical nano-vesicles in the size of 379.08 nm with an initial drug release of 37.32% in the first hour followed by a sustained drug release pattern for 6 days. DSC analysis of the optimized formulation confirmed the presence of the drug in an amorphous form with the nano-vesicles. Biological evaluation of the selected formulation was performed on New Zealand rabbits by IM injection. The prepared ISVs exhibited a 45- and 28-fold larger AUC and MRT values, respectively, compared to those of the drug suspension. The obtained findings boost the use of ISVs for the treatment of many chronic inflammatory conditions.
基于非离子表面活性剂(NIS)的原位形成囊泡(ISVs)为控制药物释放的传统系统提供了一种经济实惠的替代方案。在这项工作中,使用乳化法制备了包载双氯芬酸钠的 NIS 原位形成囊泡。使用 2.3 全因子实验设计制备了载双氯芬酸钠的 ISVs,其中三个因素被评估为独立变量;NIS 的类型(A)、NIS 与吐温®80 的摩尔比(B)和内部乙酸乙酯与外部 Captex®油相的相比例(C)。选择的制剂进行了形态学研究、可注射性、粘度测量和固态特性研究。优化的制剂表现出尺寸为 379.08nm 的球形纳米囊泡,在最初的 1 小时内药物释放 37.32%,随后持续释放药物 6 天。优化制剂的 DSC 分析证实了药物以无定形形式存在于纳米囊泡中。通过肌内注射在新西兰兔上进行了选定制剂的生物学评价。与药物混悬剂相比,所制备的 ISVs 的 AUC 和 MRT 值分别增加了 45 倍和 28 倍。这些发现为治疗许多慢性炎症疾病中使用 ISVs 提供了支持。