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Optimized copolymeric microstructured platforms for smart controlled delivery of an anticoagulant drug: Preparation, in vitro assessment and crossover study in healthy adult human volunteers
International Journal of Pharmaceutics ( IF 5.8 ) Pub Date : 2021-09-08 , DOI: 10.1016/j.ijpharm.2021.121084
Alaa H Salama 1 , Samar M Abouelatta 2
Affiliation  

In the present study, novel micro-structured copolymeric carriers were developed based on the grafting technology where acrylamide was chemically crosslinked with different types of Eudragits® (NE30D, L100, RL30D, or RS30D) based on a 41*21 factorial design. The designed systems efficiently engulfed the anticoagulant drug dipyridamole (DIP), within their formed entangled mesh of crosslinked polymeric network. An optimized formulation, ECOP4 with a desirability-value of 0.706, (in which DIP is engulfed within a copolymeric network of acrylamide and Eudragit® RS30D) showed high engulfment capacity (97.13 ± 1.34%) and controlled DIP release over 8 h. FTIR studies revealed absence of interactions between DIP and the formed copolymer. ECOP4 was further inserted within an easily-administered safe raft forming system composed of a mixture of LM-pectin and gellan gum. A pharmacokinetic study was performed using human volunteers to determine DIP concentration in their plasma after administering the designed formulation using the high-performance liquid chromatography (HPLC) method. A crossover design was adopted comparing the designed formulation with Persantin® 25 mg tablets as a reference standard. Superior results were obtained for the optimized formulation regarding the measured pharmacokinetic parameters (AUC0-24h, Cmax, and Tmax) with a 2.31 fold increase in relative bioavailability, which reveals the usefulness of the designed grafted dipyridamole formulation in site-specific delivery system.



中文翻译:

用于抗凝药物智能控制递送的优化共聚微结构平台:健康成人志愿者的制备、体外评估和交叉研究

在本研究中,基于 4 1 *2 1的丙烯酰胺与不同类型的 Eudragits®(NE30D、L100、RL30D 或 RS30D)化学交联的接枝技术开发了新型微结构共聚载体。因子设计。设计的系统在其形成的交联聚合物网络的缠结网中有效地吞噬了抗凝药物双嘧达莫 (DIP)。优化配方 ECOP4 的合意性值为 0.706(其中 DIP 被丙烯酰胺和 Eudragit® RS30D 的共聚网络吞噬)显示出高吞噬能力 (97.13 ± 1.34%) 并在 8 小时内控制 DIP 释放。FTIR 研究表明 DIP 和形成的共聚物之间不存在相互作用。ECOP4 被进一步插入由LM-果胶和结冷胶混合物组成的易于管理的安全筏形成系统中。在使用高效液相色谱 (HPLC) 方法管理设计的制剂后,使用人类志愿者进行了一项药代动力学研究,以确定他们血浆中的 DIP 浓度。采用交叉设计,将设计的配方与作为参考标准的 Persantin® 25 mg 片剂进行比较。关于测量的药代动力学参数(AUC)的优化配方获得了优异的结果0-24h、 C max和 T max ),相对生物利用度增加 2.31 倍,这揭示了所设计的接枝双嘧达莫制剂在位点特异性递送系统中的有用性。

更新日期:2021-09-17
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