Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Colloids Surf B Biointerfaces. 2021 Mar;199:111534. doi: 10.1016/j.colsurfb.2020.111534. Epub 2020 Dec 15.
The present study is concerned with the suitability of using Myrj 59, out-performing the commonly used stabilizer i.e., poloxamer, for preparation of cubosomes on one hand and gives an insight into the need for distinctive choice of delivery system and administration route towards better diabetes pharmacotherapy on the other hand. In light, repaglinide (REP) cubosomal dispersion and in-situ gel forms were prepared and physicochemically characterized. The selected cubosomal forms were tested for in-vitro drug release and administered via intranasal (IN) and intraperitoneal (IP) routes and compared with Intravenous (IV) REP solution regarding in-vivo antidiabetic efficacy. The results confirmed the formation of cubic nanostructures (170-233 nm), entrapping high REP amounts (93.2-95.66 %). Sustained REP release from selected cubosomal forms was realized with no burst release. Upon in-vivo assessment, IN and IP REP cubosomes and cubosomal gel exhibited superior long-acting in-vivo traits over IV REP solution, respecting percentages of maximum reduction, total decrease in BG levels, and the pharmacological availability. Moreover, IP REP cubosomes and cubosomal gel revealed higher values of the aforementioned parameters than IN counterparts. In conclusion, IN and IP administration of the newly developed cubosomal forms could proffer feasible options for an optimal control of BG levels.
本研究关注的是使用 Myrj 59 作为制备立方纳米载体的稳定剂（优于常用的稳定剂即泊洛沙姆）的适用性，一方面提供了对选择独特的给药系统和给药途径以改善糖尿病治疗的必要性的深入了解。在这项研究中，制备并物理化学表征了瑞格列奈（REP）立方纳米载体分散体和原位凝胶形式。对所选立方纳米载体形式进行了体外药物释放测试，并通过鼻内（IN）和腹腔内（IP）途径给药，并与静脉内（IV）REP 溶液进行了体内抗糖尿病功效比较。结果证实了立方纳米结构（170-233nm）的形成，其包封了高浓度的 REP（93.2-95.66%）。从所选立方纳米载体形式中实现了 REP 的持续释放，没有突释。在体内评估中，IN 和 IP 的 REP 立方纳米载体和立方纳米载体凝胶在体内表现出优于 IV REP 溶液的长效作用，这体现在最大降低百分比、血糖水平的总降低以及药物的有效性方面。此外，IP 给药的 REP 立方纳米载体和立方纳米载体凝胶在上述参数方面显示出更高的值。总之，新开发的立方纳米载体形式的 IN 和 IP 给药可以提供控制血糖水平的优化选择。
