Celebioglu Asli, Dash Kareena, Aboelkheir Mahmoud, Kilic Mehmet E, Durgun Engin, Uyar Tamer
Fiber Science Program, Department of Human Centered Design, College of Human Ecology, Cornell University Ithaca NY 14853 USA
Biological Sciences, College of Arts and Sciences, Cornell University Ithaca NY 14853 USA.
RSC Med Chem. 2023 Dec 21;15(2):595-606. doi: 10.1039/d3md00557g. eCollection 2024 Feb 21.
Naproxen is a well-known non-steroidal anti-inflammatory drug (NSAID) that suffers from limited water solubility. The inclusion complexation with cyclodextrin (CD) can eliminate this drawback and the free-standing nanofibrous film (NF) generated from these inclusion complexes (ICs) can be a promising alternative formula as an orally disintegrating drug delivery system. For this, naproxen/CD IC NFs were generated using the highly water soluble hydroxypropylated derivative of βCD (HPβCD) with two different molar ratios of 1/1 and 1/2 (drug/CD). The complexation energy calculated by the modeling study demonstrated a more favorable interaction between HPβCD and naproxen for the 1/2 molar ratio than 1/1. HPβCD/naproxen IC NFs were generated with loading concentrations of ∼7-11% and without using toxic chemicals. HPβCD/naproxen IC NFs indicated a faster and enhanced release profile in aqueous medium compared to pure naproxen owing to inclusion complexation. Moreover, rapid disintegration in less than a second was achieved in an artificial saliva environment.
萘普生是一种著名的非甾体抗炎药（NSAID），但其水溶性有限。与环糊精（CD）形成包合物可以消除这一缺点，由这些包合物（ICs）生成的独立纳米纤维膜（NF）作为口腔崩解药物递送系统可能是一种有前途的替代配方。为此，使用β-CD的高水溶性羟丙基化衍生物（HPβCD）以1/1和1/2两种不同摩尔比（药物/CD）生成了萘普生/CD IC NF。建模研究计算的络合能表明，对于1/2摩尔比，HPβCD与萘普生之间的相互作用比1/1摩尔比更有利。以约7-11%的负载浓度生成了HPβCD/萘普生IC NF，且未使用有毒化学品。由于形成了包合物，与纯萘普生相比，HPβCD/萘普生IC NF在水性介质中显示出更快且增强的释放曲线。此外，在人工唾液环境中不到一秒钟就实现了快速崩解。
