Development of carvedilol-loaded lipid nanoparticles with compatible lipids and enhanced skin permeation in different skin models

Abstract

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 in vitro 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/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). NLC4 seems to be a promising carrier for the transdermal delivery of CARV.

Keywords:

• Carvedilol
• nanostructured lipid carriers
• skin permeation
• skin retention
• skin models
• transdermal delivery

Compliance with ethical standards

Animal care were performed according to the ethical standards of the Normative Resolutions of the National Council for the Control of Animal Experimentation – CONCEA. Approval in June 2017 by the Ethics Committee on the Use of Animals/CEUA-PRPI-UFG was granted under number 053/17.

Disclosure statement

The authors declare that they have no conflict of interest.

Additional information

Funding

Conselho Nacional de Desenvolvimento Científico e Tecnológico - CNPq (project number 454377/2016-9), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior – CAPES, and Fundação de Amparo à Pesquisa do Estado de Goiás - FAPEG.