Laboratory of Nanosystems and Drug Delivery Devices (NanoSYS), School of Pharmacy, Universidade Federal de Goiás (UFG), Goiânia, Brazil.
J Microencapsul. 2021 Mar;38(2):124-133. doi: 10.1080/02652048.2020.1857862. Epub 2020 Dec 17.
The study aimed to develop lipid nanoparticles using excipients compatible with carvedilol (CARV) for enhanced transdermal drug delivery. Nanostructured lipid carriers (NLC) were successfully obtained and fully characterised. Franz diffusion cells were used for release and permeation studies in the porcine epidermis (EP) and full-thickness rat skin. NLC4 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/cm compared to 3.06 ± 0.79 µg/cm. NLC4 increased CARV permeation by 2.5-fold compared to the unloaded drug in rat skin studies (13.73 ± 4.12 5.31 ± 1.56 µg/cm). NLC4 seems to be a promising carrier for the transdermal delivery of CARV.
本研究旨在开发与卡维地洛（CARV）兼容的赋形剂的脂质纳米粒，以增强经皮药物传递。成功获得并充分表征了纳米结构脂质载体（NLC）。Franz 扩散池用于在猪表皮（EP）和全厚大鼠皮中进行释放和渗透研究。NLC4 和 NLC5（CARV 浓度为 0.5mg/mL）的粒径较小（分别为 80.58±1.70nm 和 116.80±12.23nm），包封效率分别为 98.14±0.79%和 98.27±0.99%。载有 CARV 的 NLC4 和 NLC5 可控制药物释放。NLC4 允许 CAR 通过猪 EP 以更大的量渗透，即 11.83±4.71µg/cm 与 3.06±0.79µg/cm 相比。与未载药的药物相比，NLC4 在大鼠皮肤研究中使 CARV 的渗透增加了 2.5 倍（13.73±4.12 5.31±1.56µg/cm）。NLC4 似乎是 CARV 经皮传递的有前途的载体。
