Nanostructured lipid carriers for hair follicle-targeted delivery of clindamycin and rifampicin to hidradenitis suppurativa treatment.

Autor: Pereira MN; Laboratory of Food, Drugs, and Cosmetics (LTMAC), School of Health Sciences, University of Brasília, 70910-900, Brasília, DF, Brazil., Tolentino S; Laboratory of Food, Drugs, and Cosmetics (LTMAC), School of Health Sciences, University of Brasília, 70910-900, Brasília, DF, Brazil., Pires FQ; Laboratory of Food, Drugs, and Cosmetics (LTMAC), School of Health Sciences, University of Brasília, 70910-900, Brasília, DF, Brazil., Anjos JLV; Institute of Physics, Federal University of Goiás - UFCat, 75704-020, Catalão, GO, Brazil., Alonso A; Institute of Mathematics and Physics, Federal University of Goiás, 74690-900, Goiânia, GO, Brazil., Gratieri T; Laboratory of Food, Drugs, and Cosmetics (LTMAC), School of Health Sciences, University of Brasília, 70910-900, Brasília, DF, Brazil., Cunha-Filho M; Laboratory of Food, Drugs, and Cosmetics (LTMAC), School of Health Sciences, University of Brasília, 70910-900, Brasília, DF, Brazil., Gelfuso GM; Laboratory of Food, Drugs, and Cosmetics (LTMAC), School of Health Sciences, University of Brasília, 70910-900, Brasília, DF, Brazil. Electronic address: gmgelfuso@unb.br.
Jazyk: angličtina
Zdroj: Colloids and surfaces. B, Biointerfaces [Colloids Surf B Biointerfaces] 2021 Jan; Vol. 197, pp. 111448. Date of Electronic Publication: 2020 Nov 07.
DOI: 10.1016/j.colsurfb.2020.111448
Abstrakt: Hidradenitis suppurativa is a chronic and debilitating inflammatory condition related to a permanent obstruction of the pilosebaceous units. Until nowadays, therapeutic options are unsatisfactory. Here, we propose nanostructured lipid carriers (NLC) entrapping an association of clindamycin phosphate (CDM) and rifampicin (RIF) as a topical alternative for the treatment of the disease. Chemical compatibility between the drugs was demonstrated using thermal analysis combined with ATR-FTIR and X-ray powder diffraction assays. Nanocarriers' diameter was narrowly distributed (polydispersity index = 0.2) around 400 ± 14 nm, they possess a negative surface charge (-48.9 ± 0.7 mV) and high drug entrapment efficiencies (80.2 ± 0.4 % and 93.4 ± 0.7 % for CDM and RIF, respectively). The formulation proved to be safe for the topical application, as it was non-irritant on both HET-CAM and reconstructed human epidermis (RHE) assays. Spin-label EPR indicated an NLC affinity for the lipidic domains of stratum corneum, which could benefit the targeting of the sebaceous units. Indeed, when applied on the skin in vitro, even when mimicking the sebaceous condition, NLC accumulated into the hair follicles openings, not altering the amount of accumulated CDM and significantly increasing by 12-fold the uptake of RIF in these structures. In conclusion, developed NLC formulation incorporating the antibiotics CDM and RIF is a promising strategy for the topical treatment of hidradenitis suppurativa or other infections that may affect the pilosebaceous units.
(Copyright © 2020 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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