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使用白蛋白纳米载体口服递送鳄梨皮提取物以调节胆固醇吸收。

Oral Delivery of Avocado Peel Extract Using Albumin Nanocarriers to Modulate Cholesterol Absorption.

作者信息

Teixeira Laura M, Viana Ana S, Reis Catarina P, Pacheco Rita

机构信息

Centro de Química Estrutural, Institute of Molecular Sciences, Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, Portugal.

Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade de Lisboa, 1749-016 Lisboa, Portugal.

出版信息

Pharmaceutics. 2025 Aug 15;17(8):1061. doi: 10.3390/pharmaceutics17081061.

Abstract

Hypercholesterolemia, a metabolic disorder and major risk factor for cardiovascular disease, remains a global health concern. Although current pharmacological interventions effectively reduce cholesterol levels, their use is often associated with adverse side effects. These limitations have driven interest in alternative or complementary approaches based on natural products; however, the poor solubility, stability, and bioavailability of many natural compounds emphasize the need for innovative drug delivery systems to enhance their health-promoting potential. The extract obtained from peels, a sustainable and underutilized by-product, has previously been reported to have cholesterol-lowering properties. : The extract was encapsulated in bovine serum albumin nanoparticles. The nanoformulation was characterized for physicochemical properties and for extract stability under acid-simulated gastric digestion. Safety and biocompatibility were evaluated by in vitro cytotoxicity assays using intestinal Caco-2 and liver HepG2 cells, and in vivo toxicity using . The bioavailability of the extract and the nanoformulation's capacity to reduce cholesterol absorption in a differentiated Caco-2 cell model were additionally assessed. : Encapsulation enhanced extract stability and bioavailability, protecting it from degradation in acid simulated gastric digestion. The nanoparticles showed favorable physicochemical properties, including a small size of less than 100 nm, and demonstrated safety and biocompatibility. In the Caco-2 model, the encapsulation of the extract resulted in reduced cholesterol permeation compared to the free extract These findings suggest that the nanoformulation developed may offer a safe and effective strategy for the oral delivery of peel extract, reinforcing its potential for application in hypercholesterolemia management.

摘要

高胆固醇血症是一种代谢紊乱疾病,也是心血管疾病的主要危险因素,仍是全球关注的健康问题。尽管目前的药物干预措施能有效降低胆固醇水平,但其使用往往伴随着不良副作用。这些局限性促使人们对基于天然产物的替代或补充方法产生兴趣;然而,许多天然化合物的溶解性、稳定性和生物利用度较差,这凸显了创新药物递送系统以增强其促进健康潜力的必要性。从果皮中提取的提取物是一种可持续利用但未充分利用的副产品,此前已有报道称其具有降胆固醇特性。该提取物被包裹在牛血清白蛋白纳米颗粒中。对该纳米制剂的理化性质以及在模拟胃酸消化条件下提取物的稳定性进行了表征。通过使用肠道Caco-2细胞和肝脏HepG2细胞的体外细胞毒性试验以及使用……进行的体内毒性试验来评估安全性和生物相容性。此外,还评估了提取物的生物利用度以及该纳米制剂在分化的Caco-2细胞模型中降低胆固醇吸收的能力。包裹提高了提取物的稳定性和生物利用度,保护其在模拟胃酸消化中不被降解。纳米颗粒表现出良好的理化性质,包括小于100nm的小尺寸,并显示出安全性和生物相容性。在Caco-2模型中,与游离提取物相比,提取物的包裹导致胆固醇渗透降低。这些发现表明,所开发的纳米制剂可能为果皮提取物的口服递送提供一种安全有效的策略,增强其在高胆固醇血症管理中的应用潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/95df/12389412/b1b07d324f27/pharmaceutics-17-01061-g001.jpg

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