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巴西蘑菇多糖稳定的五环三萜负载乳液:析因设计与细胞保护研究。

Pentacyclic triterpene-loaded emulsion stabilized by Agaricus blazei Murill polysaccharides: Factorial design and cytoprotection study.

作者信息

Campelo Matheus da Silva, Aragão Cecília Brilhante, Teixeira Izabell Maria Martins, de Siqueira Erlânia Alves, da Silva-Filho Carlos José Alves, Ricardo Nágila Maria Pontes Silva, Soares Sandra de Aguiar, de Oliveira Cristiani Lopes Capistrano Gonçalves, Muniz Celli Rodrigues, Barbosa Francisco Geraldo, Mafezoli Jair, Sampaio Tiago Lima, Ribeiro Maria Elenir Nobre Pinho

机构信息

Organic and Inorganic Chemistry Department, Science Center, Federal University of Ceará, Fortaleza, CE 60440-900, Brazil; Department of Pharmacy, Faculty of Pharmacy, Dentistry and Nursing, Federal University of Ceará, Fortaleza, CE 60430-370, Brazil.

Organic and Inorganic Chemistry Department, Science Center, Federal University of Ceará, Fortaleza, CE 60440-900, Brazil.

出版信息

Int J Biol Macromol. 2023 Apr 15;234:123731. doi: 10.1016/j.ijbiomac.2023.123731. Epub 2023 Feb 16.

Abstract

In this study, pentacyclic triterpene-loaded emulsions were stabilized by polysaccharides from Agaricus blazei Murill mushroom (PAb). The drug-excipient compatibility results by Fourier Transform Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) showed the absence of physicochemical incompatibilities. The use of these biopolymers at 0.75 % led to obtaining emulsions with droplets smaller than 300 nm, moderate polydispersity, and ζ-potential >30 mV in modulus. The emulsions presented high encapsulation efficiency, suitable pH for topical application, and absence of macroscopic signs of instability during 45 days. Morphological analysis suggested the deposition of thin layers of PAb around the droplets. The encapsulation of pentacyclic triterpene in emulsions, stabilized by PAb, improved the cytocompatibility of this drug against PC12 and murine astrocyte cells. There was a reduction in cytotoxicity, which resulted in a lower accumulation of intracellular reactive oxygen species and maintenance of the mitochondrial transmembrane potential. Based on these results, it is estimated that PAb are promising biopolymers for the emulsions' stabilization by improving their physicochemical and biological properties.

摘要

在本研究中,来自姬松茸的多糖(PAb)稳定了负载五环三萜的乳液。傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)的药物-辅料相容性结果表明不存在物理化学不相容性。使用0.75%的这些生物聚合物可得到液滴小于300nm、多分散性适中且ζ电位模量>30mV的乳液。这些乳液具有高包封率、适合局部应用的pH值,并且在45天内没有宏观不稳定迹象。形态分析表明PAb薄层沉积在液滴周围。由PAb稳定的乳液中五环三萜的包封提高了该药物对PC12和小鼠星形胶质细胞的细胞相容性。细胞毒性降低,导致细胞内活性氧积累减少和线粒体跨膜电位维持。基于这些结果,估计PAb是通过改善其物理化学和生物学性质来稳定乳液的有前景的生物聚合物。

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