Petchsomrit Arpa, Sermkaew Namfa, Wiwattanapatapee Ruedeekorn
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.
Phytomedicine and Pharmaceutical Biotechnology Excellence Research Center, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla 90112, Thailand.
Sci Pharm. 2017 Mar 15;85(1):11. doi: 10.3390/scipharm85010011.
Alginate-based composite sponges were developed as carriers to prolong the gastric retention time and controlled release of curcumin-loaded self-microemulsifying drug delivery systems (Cur-SMEDDS). Liquid Cur-SMEDDS was incorporated into a solution made up of a mixture of polymers and converted into a solid form by freeze-drying. The ratio of alginate as the main polymer, adsorbent (colloidal silicon dioxide), and additional polymers-sodium carboxymethyl cellulose (SCMC), hydroxypropyl methylcellulose (HPMC)-was varied systematically to adjust the drug loading and entrapment efficiency, sponge buoyancy, and the release profile of Cur-SMEDDS. The optimum composite sponge was fabricated from a 4% alginate and 2% HPMC mixed solution. It immediately floated on simulated gastric fluid (SGF, pH 1.2) and remained buoyant over an 8 h period. The formulation exhibited an emulsion droplet size of approximately 30 nm and provided sustained release of Cur-SMEDDS in SGF, reaching 71% within 8 h compared with only 10% release from curcumin powder. This study demonstrates the potential of alginate-based composite sponges combined with self-microemulsifying formulations for gastroretention applications involving poorly soluble compounds.
基于海藻酸盐的复合海绵被开发为载体，以延长载有姜黄素的自微乳化药物递送系统（Cur-SMEDDS）的胃滞留时间并实现其控释。将液态Cur-SMEDDS加入由聚合物混合物制成的溶液中，并通过冷冻干燥转化为固体形式。作为主要聚合物的海藻酸盐、吸附剂（胶体二氧化硅）和其他聚合物——羧甲基纤维素钠（SCMC）、羟丙基甲基纤维素（HPMC）的比例被系统地改变，以调节药物负载量和包封效率、海绵浮力以及Cur-SMEDDS的释放曲线。最佳复合海绵由4%海藻酸盐和2% HPMC的混合溶液制成。它立即漂浮在模拟胃液（SGF，pH 1.2）上，并在8小时内保持漂浮。该制剂的乳液滴尺寸约为30 nm，并在SGF中实现了Cur-SMEDDS的缓释，8小时内释放率达到71%，而姜黄素粉末的释放率仅为10%。本研究证明了基于海藻酸盐的复合海绵与自微乳化制剂相结合在涉及难溶性化合物的胃滞留应用中的潜力。
