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聚(ε-己内酯)/霉酚酸无定形固体分散体的物理化学表征及体外活性

Physicochemical Characterization and In Vitro Activity of Poly(ε-Caprolactone)/Mycophenolic Acid Amorphous Solid Dispersions.

作者信息

Sánchez-Aguinagalde Oroitz, Sanchez-Rexach Eva, Polo Yurena, Larrañaga Aitor, Lejardi Ainhoa, Meaurio Emilio, Sarasua Jose-Ramon

机构信息

Department of Mining-Metallurgy Engineering and Materials Science, POLYMAT, Bilbao School of Engineering, University of the Basque Country (UPV/EHU), Plaza Ingeniero Torres Quevedo 1, 48013 Bilbao, Spain.

Polimerbio SL, Paseo Miramon 170, 20014 Donostia-San Sebastian, Spain.

出版信息

Polymers (Basel). 2024 Apr 13;16(8):1088. doi: 10.3390/polym16081088.

Abstract

The obtention of amorphous solid dispersions (ASDs) of mycophenolic acid (MPA) in poly(ε-caprolactone) (PCL) is reported in this paper. An improvement in the bioavailability of the drug is possible thanks to the favorable specific interactions occurring in this system. Differential scanning calorimetry (DSC) was used to investigate the miscibility of PCL/MPA blends, measuring glass transition temperature (T) and analyzing melting point depression to obtain a negative interaction parameter, which indicates the development of favorable inter-association interactions. Fourier transform infrared spectroscopy (FTIR) was used to analyze the specific interaction occurring in the blends. Drug release measurements showed that at least 70% of the drug was released by the third day in vitro in all compositions. Finally, preliminary in vitro cell culture experiments showed a decreased number of cancerous cells over the scaffolds containing MPA, presumably arising from the anti-cancer activity attributable to MPA.

摘要

本文报道了在聚(ε-己内酯)(PCL)中获得霉酚酸(MPA)的无定形固体分散体(ASD)。由于该体系中发生的有利的特定相互作用,药物的生物利用度有可能得到提高。差示扫描量热法(DSC)用于研究PCL/MPA共混物的混溶性,测量玻璃化转变温度(T)并分析熔点降低以获得负相互作用参数,这表明有利的相互缔合相互作用的发展。傅里叶变换红外光谱(FTIR)用于分析共混物中发生的特定相互作用。药物释放测量表明,在所有组合物中,至少70%的药物在体外第三天前释放。最后,初步的体外细胞培养实验表明,含有MPA的支架上癌细胞数量减少,这可能归因于MPA的抗癌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/7c0dd31f1224/polymers-16-01088-sch001.jpg

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