Improved tacrolimus skin permeation by co-encapsulation with clobetasol in lipid nanoparticles: study of drug effects in lipid matrix by electron paramagnetic resonance

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dc.creatorAndrade, Lígia Marquez
dc.creatorSilva, Luis Antônio Dantas
dc.creatorSantos, Anna Paula Krawczyk
dc.creatorAmorim, Isabella Cristina de Sousa Marques
dc.creatorGonçalves, Priscila Bianca Rodrigues da Rocha
dc.creatorLima, Eliana Martins
dc.creatorAnjos, Jorge Luiz Vieira dos
dc.creatorAlonso, Antonio
dc.creatorMarreto, Ricardo Neves
dc.creatorTaveira, Stephânia Fleury
dc.date.accessioned2023-11-24T15:49:06Z
dc.date.available2023-11-24T15:49:06Z
dc.date.issued2017
dc.description.abstractCombined therapy with corticosteroids and immunosuppressant-loaded nanostructured lipid carriers (NLC) could be useful in the treatment of skin diseases. To circumvent NLC loading capacity problems, loaded drugs should have different physicochemical characteristics, such as tacrolimus (TAC) and clobetasol (CLO). Therefore, in the present study, TAC and CLO were encapsulated in NLC (TAC-NLC, CLO-NLC and TAC+CLO-NLC), coated or otherwise with chitosan. Electron paramagnetic resonance (EPR) spectroscopy of different spin labels was used to investigate the impact of drug and oil incorporation on the lipid dynamic behavior of the lipid matrices. In addition, the impact of co-encapsulation on drug release and skin permeation was evaluated. Entrapment efficiency was greater than 90% for both drugs, even when the maximum drug loading achieved for TAC-NLC and CLO-NLC was kept at TAC+CLO-NLC, because TAC is more soluble in the solid lipid and CLO in the liquid lipid. EPR data indicated that both drugs reduced the lipid fluidity near the polar surface of the lipid matrix, which suggests their presence in this region. In addition, EPR data showed that liquid lipid is also present in more superficial regions of the nanoparticle matrix. CLO was released faster than TAC from TAC+CLO-NLC, probably because it is more soluble in the liquid lipid. TAC skin penetration was affected by CLO. A 5-fold increase in TAC penetration was observed from TAC+CLO-NLC when compared to TAC-NLC formulations. Coating also increased TAC and CLO permeation to deeper skin layers (1.8-fold and 1.6-fold, respectively). TAC+CLO-NLC seems to be an effective strategy for topical delivery of TAC and CLO, and thus constitutes promising formulations for the treatment of skin diseases.
dc.identifier.citationANDRADE, Lígia Marque et al. Improved tacrolimus skin permeation by co-encapsulation with clobetasol in lipid nanoparticles: study of drug effects in lipid matrix by electron paramagnetic resonance. European Journal of Pharmaceutics and Biopharmaceutics, Stuttgart, v. 119, p. 142-149, 2017. DOI: 10.1016/j.ejpb.2017.06.014. Disponível em: https://www.sciencedirect.com/science/article/pii/S0939641116309006?via%3Dihub. Acesso em: 12 set. 2023.
dc.identifier.doi10.1016/j.ejpb.2017.06.014
dc.identifier.issn0939-6411
dc.identifier.issne- 1873-3441
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0939641116309006?via%3Dihub
dc.language.isoeng
dc.publisher.countryHolanda
dc.publisher.departmentInstituto de Física - IF (RMG)
dc.rightsAcesso Restrito
dc.subjectClobetasol
dc.subjectTacrolimus
dc.subjectNanostructured lipid carriers
dc.subjectSkin permeation
dc.subjectChitosan coating
dc.subjectCo-encapsulation
dc.titleImproved tacrolimus skin permeation by co-encapsulation with clobetasol in lipid nanoparticles: study of drug effects in lipid matrix by electron paramagnetic resonance
dc.typeArtigo

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