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芦丁口服纳米乳的研制及其优化:提高其溶解速率、渗透性和口服生物利用度。

Development and optimization of oral nanoemulsion of rutin for enhancing its dissolution rate, permeability, and oral bioavailability.

机构信息

Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj, Saudi Arabia.

出版信息

Pharm Dev Technol. 2022 Jun;27(5):588-597. doi: 10.1080/10837450.2022.2090957. Epub 2022 Jun 22.

Abstract

Rutin-loaded nanoemulsion (NE-RU) formulation is the core research work in this report. Labrafil M 1944 CS was used as the oil phase, Tween 80 as the surfactant, and Transcutol P as the co-surfactant in the preparation of nanoemulsion. By utilizing a three-level central composite design (CCD), the composition was optimized. The optimized formulation showed a droplet size of 98.53 ± 3.22 nm, zeta potential -46.70 ± 4.78 mV, and drug loading 92.34 ± 3.87%. The results of dissolution, permeability, and oral bioavailability showed about 25.55 folds, 1.98 folds, and 33.68 folds, respectively, in the case of NE-RU as compared to its naïve form. The response of fresh and aged NE was non-significantly different in terms of particle size, zeta potential, and drug loading, indicating that the formulation was stable. The successful development of NE-RU with an improved bioavailability profile suggested that this formulation might be used to examine the pharmacodynamics of oxidative stress-related metabolic disorders.

摘要

载芦丁纳米乳(NE-RU)制剂是本报告的核心研究工作。在制备纳米乳时,Labrafil M 1944 CS 用作油相,吐温 80 用作表面活性剂,Transcutol P 用作助表面活性剂。利用三水平中心组合设计(CCD)对处方进行优化。优化后的制剂粒径为 98.53 ± 3.22nm,Zeta 电位为-46.70 ± 4.78mV,载药量为 92.34 ± 3.87%。与原药相比,溶解、渗透和口服生物利用度的结果分别提高了 25.55 倍、1.98 倍和 33.68 倍。新鲜和老化的 NE 的响应在粒径、Zeta 电位和载药量方面无显著差异,表明该制剂稳定。具有改善的生物利用度特征的 NE-RU 的成功开发表明,该制剂可用于研究与氧化应激相关的代谢紊乱的药效学。

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