水凝胶型载姜黄素O/W悬浮液的制备

Timo Bodmer, Steffen F. Hartmann, C. Keck, Martina Kleiner, K. Köhler
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引用次数: 0

摘要

姜黄素是生物医药分类系统(BCS) IV类物质,具有多种潜在的治疗作用。然而,像许多其他BCS IV活性药物成分一样,需要复杂的配方来保证足够高的生物利用度。一种不太为人所知的递送系统是悬浮乳剂(SE)。se是具有连续相或分散相结晶API的乳剂。本研究旨在制备姜黄素负载的o/w悬浮液,其颗粒处于油相,用于包封或触发释放等效果。为了在油相中获得较高的包封效率(EE),颗粒需要小于乳状液滴的尺寸。测试了超声破碎和球磨在不同分散介质中制备这些纳米晶体的能力。研究发现,以米甘醇为原料的生产最适合该晶体在SEs中的应用。珠磨产生的颗粒中约85%(按体积计)小于约5 μ m的液滴尺寸。相比之下,只有23%的超声碎片颗粒小于这些液滴的直径。随后,该油悬浮液被成功用于生产水凝胶型o/w悬浮液乳剂。在本研究的第二部分,我们研究了不同的测定包封效率的方法,但没有一种方法能准确、满意地测定包封效率。最后,两种悬浮液在宏观上无法区分,并且具有物理稳定性。综上所述,我们证明了可以制备稳定的基于水凝胶的负载姜黄素的o/w悬浮液。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Production of Hydrogel-Based Curcumin-Loaded O/W Suspoemulsions
Curcumin is a biopharmaceutical classification system (BCS) class IV substance with many potential therapeutic effects. However, like many other BCS IV active pharmaceutical ingredients, complex formulations are needed to guarantee a sufficiently high bioavailability. A not-so-well-known delivery system is a suspoemulsion (SE). SEs are emulsions with a crystalline API in continuous or dispersed phases. This study aimed to produce curcumin-loaded o/w suspoemulsions with the particle in the oil phase for, e.g., encapsulation or triggered release effects. The particles need to be smaller than the emulsion droplet size to attain high encapsulation efficiencies (EE) in the oil phase. Sonofragmentation and bead milling were tested for their ability to produce these nanocrystals in different dispersion media. It was discovered that production in miglyol was the best fit for the needed application of the crystals in SEs. Around 85% (by volume) of the particles produced with bead milling were smaller than the droplet size of about 5 µm. In contrast, only 23% of the sonofragmentated particles were below the diameter of those droplets. This oily suspension was then used to successfully produce hydrogel-based o/w suspoemulsions. In the second part of this study, we investigated different methods for determining encapsulation efficiency, but none of the methods accurately and satisfactorily resolved the encapsulation efficiency. Finally, the suspoemulsions could not be macroscopically distinguished from one another and were physically stable. In summary, we showed that stable hydrogel-based curcumin-loaded o/w suspoemulsions could be produced.
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