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胡椒碱纳米乳剂的制备:体外表征、离体评价及细胞活力评估

Formulation of Piperine-Loaded Nanoemulsion: In Vitro Characterization, Ex Vivo Evaluation, and Cell Viability Assessment.

作者信息

Alshehri Sultan, Bukhari Sarah I, Imam Syed Sarim, Hussain Afzal, Alghaith Adel F, Altamimi Mohammad A, AlAbdulkarim Abdullah S, Almurshedi Alanood

机构信息

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

出版信息

ACS Omega. 2023 Jun 15;8(25):22406-22413. doi: 10.1021/acsomega.2c08187. eCollection 2023 Jun 27.

Abstract

Piperine is an alkaloid, but its therapeutic efficacy is limited due to poor aqueous solubility. In this study, piperine nanoemulsions were prepared using oleic acid (oil), Cremophore EL (surfactant), and Tween 80 (co-surfactant) using the high-energy ultrasonication approach. The optimal nanoemulsion (N2) was further evaluated using transmission electron microscopy, release, permeation, antibacterial, and cell viability studies based on minimal droplet size and maximum encapsulation efficiency. The prepared nanoemulsions (N1-N6) showed a transmittance of more than 95%, a mean droplet size between 105 ± 4.11 and 250 ± 7.4 nm, a polydispersity index of 0.19 to 0.36, and a ζ potential of -19 to -39 mV. The optimized nanoemulsion (N2) showed significantly improved drug release and permeation compared with pure piperine dispersion. The nanoemulsions were stable in the tested media. The transmission electron microscopy image showed a spherical and dispersed nanoemulsion droplet. The antibacterial and cell line results of piperine nanoemulsions were significantly better than the pure piperine dispersion. The findings suggested that piperine nanoemulsions may be a more advanced nanodrug delivery system than conventional ones.

摘要

胡椒碱是一种生物碱,但由于其水溶性差,治疗效果有限。在本研究中,采用高能超声法,以油酸(油相)、聚氧乙烯蓖麻油(表面活性剂)和吐温80(助表面活性剂)制备了胡椒碱纳米乳。基于最小液滴尺寸和最大包封率,使用透射电子显微镜、释放、渗透、抗菌和细胞活力研究对最佳纳米乳(N2)进行了进一步评估。制备的纳米乳(N1-N6)的透光率超过95%,平均液滴尺寸在105±4.11至250±7.4nm之间,多分散指数为0.19至0.36,ζ电位为-19至-39mV。与纯胡椒碱分散体相比,优化后的纳米乳(N2)的药物释放和渗透显著改善。纳米乳在测试介质中稳定。透射电子显微镜图像显示纳米乳滴呈球形且分散。胡椒碱纳米乳的抗菌和细胞系结果明显优于纯胡椒碱分散体。研究结果表明,胡椒碱纳米乳可能是一种比传统纳米药物递送系统更先进的纳米药物递送系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6f1e/10308402/1be2d635c4d4/ao2c08187_0002.jpg

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