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通过热熔挤出法制备的用于姜黄素和胡椒碱共递送的无定形聚合物-磷脂固体分散体

Amorphous Polymer-Phospholipid Solid Dispersions for the Co-Delivery of Curcumin and Piperine Prepared via Hot-Melt Extrusion.

作者信息

Wdowiak Kamil, Miklaszewski Andrzej, Cielecka-Piontek Judyta

机构信息

Department of Pharmacognosy and Biomaterials, Poznan University of Medical Sciences, 3 Rokietnicka St., 60-806 Poznan, Poland.

Institute of Materials Science and Engineering, Poznan University of Technology, Jana Pawla II 24, 61-138 Poznan, Poland.

出版信息

Pharmaceutics. 2024 Jul 28;16(8):999. doi: 10.3390/pharmaceutics16080999.

DOI:10.3390/pharmaceutics16080999
PMID:39204344
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11359794/
Abstract

Curcumin and piperine are plant compounds known for their health-promoting properties, but their use in the prevention or treatment of various diseases is limited by their poor solubility. To overcome this drawback, the curcumin-piperine amorphous polymer-phospholipid dispersions were prepared by hot melt extrusion technology. X-ray powder diffraction indicated the formation of amorphous systems. Differential scanning calorimetry confirmed amorphization and provided information on the good miscibility of the active compound-polymer-phospholipid dispersions. Owing to Fourier-transform infrared spectroscopy, the intermolecular interactions in systems were investigated. In the biopharmaceutical properties assessment, the improvement in solubility as well as the maintenance of the supersaturation state were confirmed. Moreover, PAMPA models simulating the gastrointestinal tract and blood-brain barrier showed enhanced permeability of active compounds presented in dispersions compared to the crystalline form of individual compounds. The presented paper suggests that polymer-phospholipid dispersions advantageously impact the bioaccessibility of poorly soluble active compounds.

摘要

姜黄素和胡椒碱是具有促进健康特性的植物化合物，但它们在预防或治疗各种疾病中的应用受到其低溶解度的限制。为克服这一缺点，采用热熔挤出技术制备了姜黄素 - 胡椒碱无定形聚合物 - 磷脂分散体。X射线粉末衍射表明形成了无定形体系。差示扫描量热法证实了非晶化，并提供了有关活性化合物 - 聚合物 - 磷脂分散体良好混溶性的信息。借助傅里叶变换红外光谱法，研究了体系中的分子间相互作用。在生物药剂学性质评估中，证实了溶解度的提高以及过饱和状态的维持。此外，模拟胃肠道和血脑屏障的PAMPA模型显示，与单个化合物的结晶形式相比，分散体中活性化合物的渗透性增强。本文表明，聚合物 - 磷脂分散体对难溶性活性化合物的生物可及性具有有利影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/4a59896aea36/pharmaceutics-16-00999-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/612de2814b02/pharmaceutics-16-00999-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/9a4e4f443fe7/pharmaceutics-16-00999-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/da06365169bf/pharmaceutics-16-00999-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/86aafad5135a/pharmaceutics-16-00999-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/fc2925f75b8b/pharmaceutics-16-00999-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/d38cd9ead1ed/pharmaceutics-16-00999-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/4a59896aea36/pharmaceutics-16-00999-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/612de2814b02/pharmaceutics-16-00999-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/9a4e4f443fe7/pharmaceutics-16-00999-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/da06365169bf/pharmaceutics-16-00999-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/86aafad5135a/pharmaceutics-16-00999-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/fc2925f75b8b/pharmaceutics-16-00999-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/d38cd9ead1ed/pharmaceutics-16-00999-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f4da/11359794/4a59896aea36/pharmaceutics-16-00999-g007.jpg

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