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载萘普生的聚(甲基丙烯酸2-羟烷基酯):制备及药物释放动力学

Naproxen-Loaded Poly(2-hydroxyalkyl methacrylates): Preparation and Drug Release Dynamics.

作者信息

Aljubailah Abeer, Alqahtani Saad M S, Al-Garni Tahani Saad, Saeed Waseem Sharaf, Semlali Abdelhabib, Aouak Taieb

机构信息

Chemistry Department, College of Science, King Saud University, Riyadh 11451, Saudi Arabia.

Groupe de Recherche en Écologie Buccale, Faculté de Médecin Dentaire, Université Laval, Quebec City, QC G1V 0A6, Canada.

出版信息

Polymers (Basel). 2022 Jan 23;14(3):450. doi: 10.3390/polym14030450.

Abstract

Poly(2-hydroxyethylmethacrylate)/Naproxen (NPX/pHEMA) and poly (2-hydroxypropyl methacrylate)/Naproxen (NPX/pHPMA) composites with different NPX content were prepared in situ by free radical photopolymerization route. The resulted hybrid materials were characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning Electron microscopy (SEM), and X-ray diffraction (XRD). These composites have been studied as drug carrier systems, in which a comparison of the in vitro release dynamic of NPX between the two drug carrier systems has been conducted. Different factors affecting the performance of the release dynamic of this drug, such as the amount of Naproxen incorporated in the drug carrier system, the pH of the medium and the degree of swelling, have been investigated. The results of the swelling study of pHEMA and pHPMA in different media pHs revealed that the diffusion of water molecules through both polymer samples obeys the Fickian model. The "in vitro" study of the release dynamic of Naproxen from NPX/pHEMA and NPX/pHPMA drug carrier systems revealed that the higher percentage of NPX released was obtained from each polymer carrier in neutral pH medium, and the diffusion of NPX trough these polymer matrices also obeys the Fickian model. It was also found that the less the mass percent of NPX in the composites, the better its release will be. The comparison between the two drug carrier systems revealed that the pHEMA leads to the best performance in the release dynamic of NPX. Regarding Naproxen solubility in water, the results deducted from the "in vitro" study of NPX/pHEMA10 and NPX/pHPMA10 drug carrier systems revealed a very significant improvement in the solubility of NPX in media pH1 (2.33 times, 1.43 times) and 7 (3.32 times, 2.60 times), respectively, compared to those obtained by direct dissolution of Naproxen powder.

摘要

通过自由基光聚合路线原位制备了具有不同萘普生(NPX)含量的聚甲基丙烯酸2-羟乙酯/萘普生(NPX/pHEMA)和聚甲基丙烯酸2-羟丙酯/萘普生(NPX/pHPMA)复合材料。通过傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)、扫描电子显微镜(SEM)和X射线衍射(XRD)对所得杂化材料进行了表征。这些复合材料已作为药物载体系统进行研究,其中对两种药物载体系统之间NPX的体外释放动力学进行了比较。研究了影响该药物释放动力学性能的不同因素,如药物载体系统中萘普生的掺入量、介质的pH值和溶胀程度。pHEMA和pHPMA在不同介质pH值下的溶胀研究结果表明,水分子通过这两种聚合物样品的扩散均符合菲克模型。对NPX/pHEMA和NPX/pHPMA药物载体系统中萘普生释放动力学的“体外”研究表明,在中性pH介质中,从每种聚合物载体中释放出的NPX百分比更高,并且NPX通过这些聚合物基质的扩散也符合菲克模型。还发现复合材料中NPX的质量百分比越低,其释放效果越好。两种药物载体系统之间的比较表明,pHEMA在NPX的释放动力学方面表现最佳。关于萘普生在水中的溶解度,从NPX/pHEMA10和NPX/pHPMA10药物载体系统的“体外”研究得出的结果表明,与直接溶解萘普生粉末相比,NPX在pH1(分别为2.33倍、1.43倍)和pH7(分别为3.32倍、2.60倍)介质中的溶解度有非常显著的提高。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7901/8840337/b1236c04ced9/polymers-14-00450-sch001.jpg

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