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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.

DOI:10.3390/polym16081088
PMID:38675007
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11054924/
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/11054924/2dca5041aeb3/polymers-16-01088-g011.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/1e472b00b03e/polymers-16-01088-g006.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/2dca5041aeb3/polymers-16-01088-g011.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/7c0dd31f1224/polymers-16-01088-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/f5190cad6cde/polymers-16-01088-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/181994602ba3/polymers-16-01088-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/0d8ec5d42153/polymers-16-01088-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/71aad4a3eadb/polymers-16-01088-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/ef04b2272d76/polymers-16-01088-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/1e472b00b03e/polymers-16-01088-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/a58242f5b0c7/polymers-16-01088-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/358a47125db5/polymers-16-01088-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/0c9e236750d3/polymers-16-01088-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/2af0092a21a0/polymers-16-01088-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/901f/11054924/2dca5041aeb3/polymers-16-01088-g011.jpg

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The influence of hydrogen bonding between different crystallization tendency drugs and PVPVA on the stability of amorphous solid dispersions.不同结晶倾向药物与聚乙烯吡咯烷酮-醋酸乙烯酯（PVPVA）之间的氢键对无定形固体分散体稳定性的影响。
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Curcumin amorphous solid dispersions benefit from hydroxypropyl methylcellulose E50 to perform enhanced anti-inflammatory effects.
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Int J Biol Macromol. 2023 Dec 1;252:126507. doi: 10.1016/j.ijbiomac.2023.126507. Epub 2023 Aug 24.
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Co-amorphous Drug Delivery Systems: a Review of Physical Stability, In Vitro and In Vivo Performance.共无定形药物递送系统：物理稳定性、体外和体内性能的综述。
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Stable amorphous solid dispersion of flubendazole with high loading via electrospinning.静电纺丝法制备高载量氟苯咪唑稳定无定形固体分散体。
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Continuous Manufacturing and Molecular Modeling of Pharmaceutical Amorphous Solid Dispersions.连续制造和药物无定形固体分散体的分子建模。
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