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用安全的甲基-β-环糊精包合物提高酮洛芬的溶解度和抗炎疗效。

Enhancing ketoprofen's solubility and anti-inflammatory efficacy with safe methyl-β-cyclodextrin complexation.

机构信息

School of Chemical Engineering, Yeungnam University, Gyeongsan, 38541, Republic of Korea.

PG & Research Department of Chemistry, Government Arts College, Chidambaram, 608 102, Tamil Nadu, India.

出版信息

Sci Rep. 2024 Sep 14;14(1):21516. doi: 10.1038/s41598-024-71615-9.

DOI:10.1038/s41598-024-71615-9
PMID:39277667
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11401905/
Abstract

Improved solubility and anti-inflammatory (AI) properties are imperative for enhancing the effectiveness of poorly water-soluble drugs, particularly non-steroidal anti-inflammatory drugs (NSAIDs). To address these critical issues, our focus is on obtaining NSAID materials in the form of inclusion complexes (IC) with methyl-beta-cyclodextrin (MCD). Ketoprofen (KTP) is selected as the NSAID for this study due to its potency in treating various types of pain, inflammation, and arthritis. Our objective is to tackle the solubility challenge followed by enhancing the AI activity. Confirmation of complexation is achieved through observing changes in the absorbance and fluorescence intensities of KTP upon the addition of MCD, indicating a 1:1 stoichiometric ratio. Phase solubility studies demonstrated improved dissolution rates after the formation of ICs. Further analysis of the optimized IC is conducted using FT-IR, NMR, FE-SEM, and TG/DTA techniques. Notable shifts in chemical shift values and morphological alterations on the surface of the ICs are observed compared to their free form. Most significantly, the IC exhibited superior AI and anti-arthritic (AA) activity compared to KTP alone. These findings highlight the potential of ICs in expanding the application of KTP, particularly in pharmaceuticals, where enhanced stability and efficacy of natural AIs and AAs are paramount.

摘要

提高溶解度和抗炎（AI）性质对于增强水溶性差的药物的疗效至关重要，尤其是非甾体抗炎药（NSAIDs）。为了解决这些关键问题，我们专注于获得 NSAID 材料与甲基-β-环糊精（MCD）的包合复合物（IC）的形式。酮洛芬（KTP）被选为该研究的 NSAID，因为它具有治疗各种类型疼痛、炎症和关节炎的功效。我们的目标是解决溶解度问题，然后提高 AI 活性。通过观察 MCD 加入后 KTP 的吸光度和荧光强度的变化来确认络合，表明存在 1:1 的化学计量比。相溶解度研究表明，形成 IC 后溶解速率得到提高。使用 FT-IR、NMR、FE-SEM 和 TG/DTA 技术对优化的 IC 进行进一步分析。与游离形式相比，观察到化学位移值的显著变化和 IC 表面的形态变化。最重要的是，IC 表现出比 KTP 单独使用更好的 AI 和抗关节炎（AA）活性。这些发现强调了 IC 在扩展 KTP 的应用方面的潜力，特别是在药物方面，其中天然 AI 和 AA 的稳定性和疗效的提高至关重要。

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