Jouf University.
Acta Chim Slov. 2022 Jun 14;69(2):483-488. doi: 10.17344/acsi.2022.7370.
The poor aqueous solubility of candidate drugs has presented a great challenge to formulation scientists for their effective oral delivery. Poor solubility is often associated with poor dissolution behavior and, subsequently, poor bioavailability for those drugs when intestinal absorption is dissolution rate limited. In the present study electrospun polymeric nanofibers were developed to address the poor aqueous solubility of ibuprofen, a Biopharmaceutic Classification System (BCS) class-II drug. Hydrophilic spinnable polymers like polyvinyl pyrrolidone were deployed as a carrier system for the fabrication of nanofibers. The electrospinning parameters like flow rate, voltage, and spinneret to collector distance were optimized. The fabricated ibuprofen-loaded nanofibers were characterized using scanning electron microscopy and differential scanning calorimetry. Drug release studies and ex vivo intestinal absorption studies were also carried out. The nanofiber-based platform significantly improved in vitro absorption of ibuprofen compared to pure ibuprofen crystals.
候选药物的水溶性差，这给制剂科学家们带来了巨大的挑战，难以实现其有效的口服递送。当肠道吸收受溶解速率限制时，水溶性差通常与较差的溶解行为相关，进而导致这些药物的生物利用度较差。在本研究中，开发了电纺聚合物纳米纤维来解决布洛芬（一种生物药剂学分类系统（BCS）II 类药物）的水溶性差的问题。亲水性可纺聚合物，如聚乙烯吡咯烷酮，被用作制造纳米纤维的载体系统。对电纺参数（如流速、电压和喷丝头到收集器的距离）进行了优化。使用扫描电子显微镜和差示扫描量热法对制备的载药纳米纤维进行了表征。还进行了药物释放研究和离体肠道吸收研究。与纯布洛芬晶体相比，基于纳米纤维的平台显著提高了布洛芬的体外吸收。
