Development and characterization of a nanoemulsion containing propranolol for topical delivery.

Autor:	Zanela da Silva Marques T; Department of Drugs and Medicines, Faculty of Pharmacy., Santos-Oliveira R; Institute of Nuclear Energy., Betzler de Oliveira de Siqueira L; Department of Drugs and Medicines, Faculty of Pharmacy., Cardoso VDS; Unit of Biocatalysis, Bioproducts and Bioenergy (Bioinivar), Institute of Microbiology Paulo de Góes, Federal University of Rio de Janeiro, Rio de Janeiro, RJ, Brazil., de Freitas ZMF; Department of Drugs and Medicines, Faculty of Pharmacy., Barros RCDSA; Department of Drugs and Medicines, Faculty of Pharmacy., Villa ALV; Department of Drugs and Medicines, Faculty of Pharmacy., Monteiro MSSB; Department of Drugs and Medicines, Faculty of Pharmacy., Dos Santos EP; Department of Drugs and Medicines, Faculty of Pharmacy., Ricci-Junior E; Department of Drugs and Medicines, Faculty of Pharmacy.
Jazyk:	angličtina
Zdroj:	International journal of nanomedicine [Int J Nanomedicine] 2018 May 14; Vol. 13, pp. 2827-2837. Date of Electronic Publication: 2018 May 14 (Print Publication: 2018).
DOI:	10.2147/IJN.S164404
Abstrakt:	Background: Propranolol (PPN) is a therapeutic option for the treatment of infantile hemangiomas. This study aimed at the development of nanoemulsion (NE) containing 1% PPN, characterization of the system, and safety studies based on ex vivo permeation, cytotoxicity, and biodistribution in vivo. Methods: The formulation was developed and characterized in relation to the droplet size, polydispersity index (PDI), pH, zeta potential, and electronic microscopy. Ex vivo permeation studies were used to evaluate the cutaneous retention of PPN in the epidermis and dermis. Cytotoxicity studies were performed in fibroblasts, macrophages, and keratinocytes. In vivo biodistribution assay of the formulations was performed by means of labeling with technetium-99m. Results: NE1 exhibited droplet size of 26 nm, PDI <0.4, pH compatible with the skin, and zeta potential of -20 mV, which possibly contributes to the stability. Electron microscopy showed that the NE presented droplets of nanometric size and spherical shape. NE1 provided excellent stability for PPN. In the ex vivo cutaneous permeation assay, the NE provided satisfactory PPN retention particularly in the dermis, which is the site of drug action. In addition, NE1 promoted cutaneous permeation of the PPN in small amount. In vivo biodistribution showed that the radiolabeled formulation remained in the skin and a small amount reached the bloodstream. NE1 presented low cytotoxicity to fibroblasts, macrophages, and keratinocytes in the concentrations evaluated in the cytotoxicity assay. Conclusion: We concluded that the formulation is safe for skin administration; however, cutaneous irritation studies should be performed to confirm the safety of the formulation before clinical studies in patients with infantile hemangiomas. Competing Interests: Disclosure The authors report no conflicts of interest in this work.
Databáze:	MEDLINE
Externí odkaz:	Zobrazit plný text záznamu