当前位置: X-MOL 学术J. Microencapsul. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Development of carvedilol-loaded lipid nanoparticles with compatible lipids and enhanced skin permeation in different skin models
Journal of Microencapsulation ( IF 3.9 ) Pub Date : 2020-12-11
Najla Locatelli Santos Esteves, Lígia Marquez Andrade, Anna Paula Krawczyk-Santos, Bruno Santos Souza, Ricardo Neves Marreto, Stephânia Fleury Taveira

Abstract

Aim

The study aimed to develop lipid nanoparticles using excipients compatible with carvedilol (CARV) for enhanced transdermal drug delivery

Methods

Nanostructured lipid carriers (NLC) were successfully obtained and fully characterized. Franz diffusion cells were used for release and in vitro permeation studies in the porcine epidermis (EP) and full-thickness rat skin

Results

NLC 4 and NLC5 (0.5 mg/mL of CARV) presented small size (80.58 ± 1.70 and 116.80 ± 12.23 nm, respectively) and entrapment efficiency of 98.14 ± 0.79 and 98.27 ± 0.99%, respectively. CARV-loaded NLC4 and NLC5 controlled drug release. NLC4 allowed CAR permeation through porcine EP in greater amounts than NLC5, i.e., 11.83 ± 4.71 µg/cm2 compared to 3.06 ± 0.79 µg/cm2. NLC4 increased CARV permeation by 2.5-fold compared to the unloaded drug in rat skin studies (13.73 ± 4.12 versus 5.31 ± 1.56 µg/cm2).

Conclusions

NLC4 seems to be a promising carrier for the transdermal delivery of CARV.



中文翻译:

开发出具有卡维地洛的脂质纳米颗粒,具有相容的脂质并在不同的皮肤模型中增强了皮肤的渗透

摘要

目标

这项研究旨在使用与卡维地洛(CARV)相容的赋形剂开发脂质纳米颗粒,以增强透皮药物传递

方法

纳米结构脂质载体(NLC)已成功获得并进行了充分表征。Franz扩散细胞用于猪表皮(EP)和全厚度大鼠皮肤的释放和体外渗透研究

结果

NLC 4和NLC5(0.5 mg / mL CARV)体积小(分别为80.58±1.70和116.80±12.23 nm),包封率分别为98.14±0.79和98.27±0.99%。载有CARV的NLC4和NLC5控制药物释放。与NLC5相比,NLC4允许CAR通过猪EP的渗透量更大,即11.83±4.71 µg / cm 2,而3.06±0.79 µg / cm 2。与大鼠皮肤研究中未加载的药物相比,NLC4使CARV渗透增加了2.5倍(13.73±4.125.31±1.56 µg / cm 2)。

结论

NLC4似乎是CARV透皮递送的有希望的载体。

更新日期:2020-12-11
down
wechat
bug