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载洛索洛芬钠的 HPMC-g-聚(AMPS)水凝胶的制备及体外表征。

Fabrication and in vitro characterization of HPMC-g-poly(AMPS) hydrogels loaded with loxoprofen sodium.

机构信息

Department of Pharmacy, COMSATS University Islamabad, Abbottabad Campus, 22060, Pakistan.

Department of Pharmacy, COMSATS University Islamabad, Lahore Campus, 60000, Pakistan.

出版信息

Int J Biol Macromol. 2018 Dec;120(Pt B):1624-1631. doi: 10.1016/j.ijbiomac.2018.09.184. Epub 2018 Oct 1.

DOI:10.1016/j.ijbiomac.2018.09.184
PMID:30287359
Abstract

The aim of this study was to prepare hydroxypropyl-methyl cellulose (HPMC)-K15 based hydrogels via free radical polymerization using 2‑acrylamido-2‑methyl propane sulphonic acid (AMPS) as a monomer and N,N'-methylene bisacrylamide (MBAAm) as a crosslinker. Loxoprofen sodium was chosen as a model drug and successfully loaded in hydrogel discs. Sol-gel, porosity, loading efficiency, and the in vitro drug release analysis were carried out to evaluate its drug delivery potential. HMPC-g-poly(AMPS) hydrogels were characterized by using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and scanning electron microscopy (SEM) approaches. Maximum swelling and drug release were observed at pH 7.4. Kinetic modelling suggested that drug release followed first-order kinetics with the non-Fickian mechanism. FTIR and DSC confirmed the formation of new hydrogels. SEM micrographs confirmed uneven, rough, and partially porous type of surface. These results suggested that HMPC-g-poly(AMPS) hydrogels can be a prospective pH-responsive carrier for delivery of water-soluble drugs, such as loxoprofen sodium.

摘要

本研究旨在通过自由基聚合,以 2-丙烯酰胺-2-甲基丙磺酸(AMPS)为单体,N,N'-亚甲基双丙烯酰胺(MBAAm)为交联剂,制备羟丙基甲基纤维素(HPMC)-K15 基水凝胶。将洛索洛芬钠选为模型药物,并成功负载于水凝胶片中。通过溶胶-凝胶法、孔隙率、载药效率和体外药物释放分析来评估其药物传递潜力。采用傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)和扫描电子显微镜(SEM)对 HMPC-g-聚(AMPS)水凝胶进行了表征。在 pH 7.4 时观察到最大的溶胀和药物释放。动力学模型表明药物释放遵循一级动力学和非菲克扩散机制。FTIR 和 DSC 证实了新水凝胶的形成。SEM 显微照片证实了表面不均匀、粗糙和部分多孔的类型。这些结果表明,HMPC-g-聚(AMPS)水凝胶可以作为一种有前景的 pH 响应载体,用于输送洛索洛芬钠等水溶性药物。

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