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使用不同共价交联剂制备用于延迟和延长药物释放的载萘普生丝胶蛋白/海藻酸盐珠粒并进行评估。

Development and evaluation of naproxen-loaded sericin/alginate beads for delayed and extended drug release using different covalent crosslinking agents.

作者信息

Freitas Emanuelle D, Freitas Vitória M S, Rosa Paulo C P, da Silva Meuris G C, Vieira Melissa G A

机构信息

School of Chemical Engineering, University of Campinas - UNICAMP, Albert Einstein Avenue, 500, 13083-852 Campinas, SP, Brazil.

Faculty of Pharmaceutical Sciences, University of Campinas - UNICAMP, Cândido Portinari Street, 13083-871 Campinas, SP, Brazil.

出版信息

Mater Sci Eng C Mater Biol Appl. 2021 Jan;118:111412. doi: 10.1016/j.msec.2020.111412. Epub 2020 Aug 22.

Abstract

Different polymer matrix compositions based on sericin and alginate blend (using or not the covalent crosslinking agents dibasic sodium phosphate, polyvinyl alcohol and polyethylene glycol) were evaluated to entrap naproxen. Sericin has been shown to be essential for improving incorporation efficiency. Comparing the formulations with and without crosslinking agent, the best results were obtained for that composed only of sericin and alginate, with satisfactory values of entrapment efficiency (>80%) and drug loading capacity (>20%). In this case, delayed release (<10% in acid medium) and prolonged release (~360 min) were achieved, with a complex release mechanism involving swelling and polymer chain relaxation. The incorporation of the drug could be confirmed by the techniques of characterization of X-ray diffraction (XRD), scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR), as well as drug compatibility with the polymer matrix. In addition, particles of suitable size for multiparticulate systems were obtained and with higher thermal stability when compared to the pure drug.

摘要

评估了基于丝胶蛋白和海藻酸盐共混物(使用或不使用共价交联剂磷酸氢二钠、聚乙烯醇和聚乙二醇)的不同聚合物基质组合物对萘普生的包封情况。已证明丝胶蛋白对于提高包封效率至关重要。比较有无交联剂的制剂,仅由丝胶蛋白和海藻酸盐组成的制剂取得了最佳结果,其包封效率(>80%)和载药量(>20%)令人满意。在这种情况下,实现了延迟释放(在酸性介质中<10%)和延长释放(约360分钟),其复杂的释放机制涉及溶胀和聚合物链松弛。药物的包封可通过X射线衍射(XRD)、扫描电子显微镜(SEM)和傅里叶变换红外光谱(FTIR)等表征技术以及药物与聚合物基质的相容性来证实。此外,获得了适用于多颗粒系统的合适尺寸颗粒,并且与纯药物相比具有更高的热稳定性。

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