脂质纳米胶囊增强柚皮素在大鼠小肠非外翻囊中的溶解度和渗透性。

Enhanced Solubility and Permeability of Naringenin Across Non-Everted Sacs of Rat Small Intestine by Lipid Nanocapsules.

机构信息

Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.

出版信息

Recent Pat Nanotechnol. 2021;15(1):55-69. doi: 10.2174/1872210514666200731181130.

DOI:10.2174/1872210514666200731181130

PMID:32735533

Abstract

BACKGROUND

Naringenin (NRG) has many health benefits, including; anti-atherogenic, antiinflammatory, antitumor, and anticancer activity, as well as improvement of lipid metabolism. However, its use is limited due to its low solubility and bioavailability.

OBJECTIVES

The aim of the present patent study was the preparation and optimization of NRG loaded Novel Lipid Nanocapsules (LNCs) for the improvement of NRG solubility and gut permeability.

METHODS

Studied variables included; Solutol® HS15 and NRG concentration and the ratio of cold diluent water to primary emulsion. The storage stability of the LNCs was evaluated for 32 days and thermal analyses were conducted by Differential Scanning Calorimetry (DSC). The antioxidant properties of the NRG in LNCs were studied by measuring the 2,2-Diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging activity. The enhancement of permeation of NRG by the LNCs from the intestine was evaluated by the non-everted gut sac method.

RESULTS

The optimized NRG-LNCs had a hydrodynamic diameter of 29.41±1.25 nm, a low polydispersity index, and high entrapment efficiency of 99.25±2.31%. The LNCs could retain NRG radical scavenging activity, showed good storage stability, and significantly improved NRG solubility (69 fold) and permeation through non-everted rat intestinal sac (4.33 fold).

CONCLUSION

LNCs of NGR enhance solubility and intestinal permeability of this flavonoid and may be useful in the improvement of its bioavailability.

摘要

背景

柚皮素（NRG）具有许多健康益处，包括抗动脉粥样硬化、抗炎、抗肿瘤和抗癌活性，以及改善脂质代谢。然而，由于其低溶解度和生物利用度，其应用受到限制。

目的

本专利研究的目的是制备和优化 NRG 负载新型脂质纳米胶囊（LNC），以提高 NRG 的溶解度和肠道通透性。

方法

研究变量包括 Solutol® HS15 和 NRG 浓度以及冷稀释水与初级乳液的比例。通过差示扫描量热法（DSC）对 LNC 的储存稳定性进行了 32 天的评估，并进行了热分析。通过测量 2,2-二苯基-1-苦基肼（DPPH）自由基清除活性来研究 NRG 在 LNC 中的抗氧化性质。通过非翻转肠囊法评价 LNC 对 NRG 从肠道渗透的增强作用。