纤维素和糖基口服可分散薄膜改变了溶解性差的姜黄素的固态和溶解特性。

IF 2.1 Q3 PHARMACOLOGY & PHARMACY Advances in Pharmacological and Pharmaceutical Sciences Pub Date : 2024-05-27 eCollection Date: 2024-01-01 DOI:10.1155/2024/8596712
Helmy Yusuf, Orchidea Meidy Nurintan Savitri, Nadia Natsya Al-Khalifi, Lavinia Gunawan, Brian Karno Chairul, M Agus Syamsur Rijal, Dewi Isadiartuti, Retno Sari
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引用次数: 0

摘要

本研究旨在开发和优化含有植物提取药物姜黄素(CUR)的口服分散薄膜(ODTF)。姜黄素属于生物制药分类系统(BCS)第四类化合物,需要在制剂前提高其水溶性和组织渗透性。为解决此类溶解性和渗透性问题,我们采用 ODTF 生产 CUR 的固体分散基质。研究中使用的成膜聚合物是纤维素基(羟丙基甲基纤维素/HPMC 和羧甲基纤维素/CMC)和糖基麦芽糊精(MDX)。此外,还使用了聚氧乙烯醚(POL)作为表面活性剂和增溶剂。薄膜的生产采用了溶剂浇铸技术。将 CUR 的乙醇溶液与 POL 的水溶液混合,然后在浇铸前加入不同的成膜聚合物中。将 CUR 与 POL 溶液混合处理的目的是帮助药物在聚合物基质中均匀分散,并提高薄膜的润湿性。薄膜的物理状态和特性主要体现在其形态、药物结晶度和混合物的相溶性上。此外,还从溶解速率和溶解效率的角度评估了薄膜的溶解情况。获得的 ODTF 产品表面光滑平整。物理表征还表明,CUR 在 ODTF 中分散均匀,X 射线衍射(XRD)显示其不再是结晶物质。差示扫描量热仪(DSC)也显示,CUR 没有与薄膜发生相分离。这种分散是通过 POL 的增溶作用和紧密的聚合物薄膜基质实现的,这些基质阻止了 CUR 的再结晶。此外,ODTFs 还提高了 CUR 的溶解度,是未加工 CUR 的 3.2 倍。总体而言,纤维素基薄膜的物理性质优于糖基薄膜。
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Cellulose- and Saccharide-Based Orally Dispersible Thin Films Transform the Solid States and Dissolution Characteristics of Poorly Soluble Curcumin.

This study aimed at developing and optimizing the orally dispersible thin film (ODTF) containing a plant-derived drug-curcumin (CUR). CUR belongs to a biopharmaceutical classification system (BCS) class IV compound that requires improving its water solubility and tissue permeability preceding formulation. An ODTF was applied to produce a solid dispersion matrix for CUR to resolve such solubility and permeability problems. The film-forming polymers used in the study were cellulose-based (hydroxypropyl methylcellulose/HPMC and carboxymethylcellulose/CMC) and saccharide-based maltodextrin (MDX). Poloxamer (POL) was also employed as surfactant and solubilizer. The solvent casting technique was applied to produce the films. The ethanolic solution of CUR was mixed with an aqueous solution of POLs and then incorporated into different film-forming polymers prior to casting. The processing of the CUR with POL solution was intended to aid in the even dispersion of the drug in the polymeric matrices and enhance the wettability of the films. The physical state and properties of the films were characterized in terms of their morphology, crystallinity of the drug, and phase miscibility of the mixtures. The dissolution profile of the films was also evaluated in terms of dissolution rate and dissolution efficiency. The obtained ODTF products were smooth and flat-surfaced. Physical characterization also indicated that the CUR was homogeneously dispersed in the ODTFs and no longer existed as crystalline material as revealed by X-ray diffraction (XRD). The CUR was also not phase-separated from the films as disclosed by differential scanning calorimetry (DSC). Such dispersion was achieved through the solubilizing effect of POLs and compact polymeric film matrices that prevented the CUR from recrystallization. Furthermore, the ODTFs also improved the dissolution of CUR by 3.2-fold higher than the raw CUR. Overall, cellulose-based films had favorable physical properties compared with saccharide-based films.

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CiteScore
4.30
自引率
3.60%
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17 weeks
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