Bioactive Self-Nanoemulsifying Drug Delivery Systems (Bio-SNEDDS) for Combined Oral Delivery of Curcumin and Piperine
Bioactive Self-Nanoemulsifying Drug Delivery Systems (Bio-SNEDDS) for Combined Oral Delivery of Curcumin and Piperine
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DOI：
10.3390/molecules25071703
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发表时间：
2020-04-01
期刊：
影响因子：
4.6
通讯作者：
Alanazi, Fars K.
中科院分区：
文献类型：
--
作者：
Kazi, Mohsin;Shahba, Ahmad A.;Alanazi, Fars K.
背景：天然来源的生物活性油已经引起了医疗保健专业人员和患者的极大兴趣。目的：目的：通过将具有生物活性的天然油脂加入到姜黄素（CUR）和胡椒碱（PP）的制剂中，设计一种具有生物活性的自纳米乳化给药系统（Bio-SNEDDS）。研究方法：在各种SNEDDS制剂中筛选杏、鳄梨、黑籽和花椒籽油的自乳化特性。每种液体SNEDDS制剂均装载有CUR和PP。最佳液体SNEDDS使用Aeroperl（（R））和Neusilin（（R））以1：1 w/w比固化。液体和固体SNEDDS，其特征在于液滴尺寸分析，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。进行体外溶出研究以评价固体Bio-SNEDDS中CUR和PP的释放效率。结果如下：由黑籽油组成的SNEDDS具有优异的自乳化性能，沿着小的液滴尺寸和透明的外观。共溶剂Transcutol P的加入提高了CUR和PP的增溶能力。两种吸附剂均能有效地将液态SNEDDS固化，使药物以无定形状态存在。特别地，由黑籽油/Imwitor 988/Transcutol P/Cremophor RH40（20/20/10/50）组成并且当用Neusilin固化时，SNEDDS显示增强的CUR和PP释放（分别高达60%和77%）。此外，该制剂有效地将高生物活性的黑籽油递送给患者。结论：优化的Bio-SNEDDS包含黑色种子油，显示出优异的自乳化特性，沿着固化时增强的CUR/PP溶解。
Background: Bioactive oils of natural origin have gained huge interests from health care professionals and patients. Objective: 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. Methods: The self-emulsifying properties of apricot, avocado, black seed and Zanthoxylum rhetsa 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((R)) and Neusilin((R)) at 1:1 w/w 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. Results: 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.