Scholarlink

Abstract <p>This study developed and evaluated nanostructured lipid carriers (NLC) made from natural materials loaded with atorvastatin (ATV) to improve its therapeutic effect. ATV is widely used as an antihyperlipidemic drug to lower cholesterol and triglycerides, which are key risk factors for cardiovascular diseases. However, as per the Biopharmaceutical Classification System, ATV belongs to Class II, with low aqueous solubility and extensive hepatic metabolism, which limits its bioavailability and hinder clinical effectiveness.</p> Methods <p>The NLCs were formulated using high-speed homogenization emulsification. The formulation incorporated natural oils such as safflower, sunflower, rice, avocado, and wheat germ oil, recognized for their cholesterol-lowering properties. Lipid matrices included Precirol<sup>®</sup> ATO 5 and Gelucire<sup>®</sup> 50/13, which also functioning as a surfactant due to its amphiphilic properties. Pluronic<sup>®</sup> F-68 was also employed as a surfactant. The formulation was evaluated based on parameters such as lipid and surfactant composition, particle size, polydispersity index (PDI), entrapment efficiency, and drug release profile.</p> Results <p>The NLCs had particle sizes ranging from 163.3 ± 5.8&#xa0;nm to 235.4 ± 6.2&#xa0;nm with PDI values between 0.311 ± 0.023 and 0.396 ± 0.031. Entrapment efficiency reached up to 95.31 ± 4.32%. In-vivo studies demonstrated superior therapeutic efficacy of NLCs, reducing cholesterol levels by 14–37%, outperforming atorvastatin suspension.</p> Conclusions <p>The resulting formulations exhibited particle sizes ranging from 163 to 236&#xa0;nm, with encapsulation efficiencies exceeding 90%. In-vivo studies demonstrated that these lipid nanocarriers significantly enhanced the cholesterol-lowering effect of atorvastatin compared to its conventional suspension form, achieving reductions in cholesterol levels ranging from 14% to 37%.</p> Graphical Abstract <p></p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Evaluation of the Cholesterol-Lowering Effect of Atorvastatin Loaded in Lipid Nanodispersions Based on Natural Materials

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2025年12月20日

查看全文
  • Luis Eduardo Serrano Mora,
  • María de la Luz Zambrano Zaragoza,
  • Lizbeth Martínez Acevedo,
  • Gilberto García Salazar,
  • Jazmin Flores Monroy,
  • David Quintanar Guerrero

摘要

Abstract

This study developed and evaluated nanostructured lipid carriers (NLC) made from natural materials loaded with atorvastatin (ATV) to improve its therapeutic effect. ATV is widely used as an antihyperlipidemic drug to lower cholesterol and triglycerides, which are key risk factors for cardiovascular diseases. However, as per the Biopharmaceutical Classification System, ATV belongs to Class II, with low aqueous solubility and extensive hepatic metabolism, which limits its bioavailability and hinder clinical effectiveness.

Methods

The NLCs were formulated using high-speed homogenization emulsification. The formulation incorporated natural oils such as safflower, sunflower, rice, avocado, and wheat germ oil, recognized for their cholesterol-lowering properties. Lipid matrices included Precirol® ATO 5 and Gelucire® 50/13, which also functioning as a surfactant due to its amphiphilic properties. Pluronic® F-68 was also employed as a surfactant. The formulation was evaluated based on parameters such as lipid and surfactant composition, particle size, polydispersity index (PDI), entrapment efficiency, and drug release profile.

Results

The NLCs had particle sizes ranging from 163.3 ± 5.8 nm to 235.4 ± 6.2 nm with PDI values between 0.311 ± 0.023 and 0.396 ± 0.031. Entrapment efficiency reached up to 95.31 ± 4.32%. In-vivo studies demonstrated superior therapeutic efficacy of NLCs, reducing cholesterol levels by 14–37%, outperforming atorvastatin suspension.

Conclusions

The resulting formulations exhibited particle sizes ranging from 163 to 236 nm, with encapsulation efficiencies exceeding 90%. In-vivo studies demonstrated that these lipid nanocarriers significantly enhanced the cholesterol-lowering effect of atorvastatin compared to its conventional suspension form, achieving reductions in cholesterol levels ranging from 14% to 37%.

Graphical Abstract