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用于姜黄素和胡椒碱联合口服递送的生物活性自微乳药物传递系统(Bio-SNEDDS)。

Bioactive Self-Nanoemulsifying Drug Delivery Systems (Bio-SNEDDS) for Combined Oral Delivery of Curcumin and Piperine.

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh-11451, Saudi Arabia.

Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

出版信息

Molecules. 2020 Apr 8;25(7):1703. doi: 10.3390/molecules25071703.

Abstract

: Bioactive oils of natural origin have gained huge interests from health care professionals and patients. : To design a bioactive self-nanoemulsifying drug delivery system (Bio-SNEDDS) comprising curcumin (CUR) and piperine (PP) by incorporating bioactive natural oils in the formulation. : The self-emulsifying properties of apricot, avocado, black seed and seed oils were screened within various SNEDDS formulations. Each liquid SNEDDS formulation was loaded with both CUR and PP. The optimal liquid SNEDDS were solidified using Aeroperl and Neusilin at 1:1 / ratio. Liquid and solid SNEDDS were characterized by droplet size analysis, equilibrium solubility, scanning electron microscopy, X-ray powder diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy. In-vitro dissolution studies were performed to evaluate the efficiency of CUR and PP release from solid Bio-SNEDDS. : The liquid SNEDDS comprised of black seed oil exhibited excellent self-emulsification performance, low droplet size along with transparent appearance. The inclusion of the cosolvent Transcutol P improved the solubilization capacity of both CUR and PP. The liquid SNEDDS were efficiently solidified using the two adsorbents and presented the drugs within amorphous state. In particular, SNEDDS comprised of black seed oil/Imwitor988/Transcutol P/Cremophor RH40 (20/20/10/50) and when solidified with Neusilin showed enhanced CUR and PP release (up to 60% and 77%, respectively). In addition, this formulation efficiently delivers the highly bioactive black seed oil to the patient. Conclusions: The optimized Bio-SNEDDS comprising black seed oil showed outstanding self-emulsification characteristics along with enhanced CUR/PP dissolution upon solidification.

摘要

天然生物活性油引起了医疗保健专业人员和患者的极大兴趣。设计一种包含姜黄素(CUR)和胡椒碱(PP)的生物活性自微乳给药系统(Bio-SNEDDS),将生物活性天然油纳入配方中。筛选杏仁、鳄梨、黑种草和芝麻籽油在各种 SNEDDS 配方中的自乳化特性。将每个液体 SNEDDS 配方负载 CUR 和 PP。最佳液体 SNEDDS 使用 Aeroperl 和 Neusilin 以 1:1 的比例固化。液体和固体 SNEDDS 通过粒径分析、平衡溶解度、扫描电子显微镜、X 射线粉末衍射、差示扫描量热法和傅里叶变换红外光谱进行表征。进行体外溶解研究以评估固体 Bio-SNEDDS 中 CUR 和 PP 释放的效率。液体 SNEDDS 由黑种草油组成,表现出优异的自乳化性能、低粒径和透明外观。加入共溶剂 Transcutol P 提高了 CUR 和 PP 的溶解度。两种吸附剂有效地固化了液体 SNEDDS,并将药物呈无定形态呈现。特别是,由黑种草油/Imwitor988/Transcutol P/Cremophor RH40(20/20/10/50)组成的 SNEDDS 并与 Neusilin 固化时,可增强 CUR 和 PP 的释放(分别高达 60%和 77%)。此外,该配方可有效地将高生物活性的黑种草油递送给患者。结论:由黑种草油组成的优化 Bio-SNEDDS 表现出出色的自乳化特性,并在固化时增强 CUR/PP 溶解。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a442/7181043/5332dc5e560d/molecules-25-01703-g001.jpg

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