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Physicochemical Characterization and Skin Permeation of Cationic Transfersomes Containing the Synthetic Peptide PnPP-19

[ Vol. 15 , Issue. 7 ]

Author(s):

Flavia De Marco Almeida*, Carolina Nunes Silva, Savia Caldeira de Araujo Lopes, Daniel Moreira Santos, Fernanda Silva Torres, Felipe Lima Cardoso, Patricia Massara Martinelli, Elizabeth Ribeiro da Silva, Maria Elena de Lima, Lucas Antonio Ferreira Miranda and Monica Cristina Oliveira   Pages 1064 - 1071 ( 8 )

Abstract:


Background: PnPP-19 is a 19-amino-acid synthetic peptide previously described as a novel drug for the treatment of erectile dysfunction.

Objective: The aim of this work was to evaluate the physicochemical properties of cationic transfersomes containing PnPP-19 and the skin permeation of free PnPP-19 and PnPP-19-loaded transfersomes.

Methods: Three different liposomal preparation methods were evaluated. Cationic transfersomes contained egg phosphatidyl choline: stearylamine (9:1 w/w) and Tween 20 (84.6:15.4 lipid:Tween, w/w). Lipid concentration varied from 20 to 40 mM. We evaluated the entrapment percentage, mean diameter, zeta potential and stability at 4 °C of the formulations. The skin permeation assays were performed with abdominal human skin using Franz diffusion cell with 3 cm2 diffusion area at 32 °C and a fluorescent derivative of the peptide, containing 5-TAMRA, bound to PnPP-19 C-terminal region, where an extra lysine was inserted.

Results: Our results showed variable entrapment efficiencies, from 6% to 30%, depending on the preparation method and the lipid concentration used. The reverse phase evaporation method using a total lipid concentration equal to 40 mM led to the best entrapment percentage (30.2 + 4.5%). Free PnPP-19 was able to permeate skin at a rate of 10.8 ng/cm2/h. However, PnPP-19 was specifically hydrolyzed by skin proteases, generating a fragment of 15 amino acid residues. Encapsulated PnPP-19 permeated the skin at a rate of 19.8 ng/cm2/h.

Conclusion: The encapsulation of PnPP-19 in cationic transfersomes protected the peptide from degradation, favoring its topical administration.

Keywords:

Cationic transfersomes, peptide, PnPP-19, skin permeation, topical delivery system, nanotechnology.

Affiliation:

Laboratorio de Tecnologia Farmaceutica, Departamento de Produtos Farmaceuticos, Faculdade de Farmacia, Universidade Federal de Minas Gerais, Belo Horizonte, Laboratorio de Venenos e Toxinas Animais, Departamento de Bioquimica e Imunologia, Instituto de Ciencias Biologicas, Universidade Federal de Minas Gerais, Belo Horizonte, Laboratorio de Tecnologia Farmaceutica, Departamento de Produtos Farmaceuticos, Faculdade de Farmacia, Universidade Federal de Minas Gerais, Belo Horizonte, Laboratorio de Venenos e Toxinas Animais, Departamento de Bioquimica e Imunologia, Instituto de Ciencias Biologicas, Universidade Federal de Minas Gerais, Belo Horizonte, Laboratorio de Venenos e Toxinas Animais, Departamento de Bioquimica e Imunologia, Instituto de Ciencias Biologicas, Universidade Federal de Minas Gerais, Belo Horizonte, Cirurgia Plastica Sebastiao Nelson, Belo Horizonte, Laboratorio de Neurobiologia, Departamento de Morfologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, Laboratorio de Neurobiologia, Departamento de Morfologia, Instituto de Ciências Biológicas, Universidade Federal de Minas Gerais, Belo Horizonte, Laboratorio de Venenos e Toxinas Animais, Departamento de Bioquimica e Imunologia, Instituto de Ciencias Biologicas, Universidade Federal de Minas Gerais, Belo Horizonte, Laboratorio de Tecnologia Farmaceutica, Departamento de Produtos Farmaceuticos, Faculdade de Farmacia, Universidade Federal de Minas Gerais, Belo Horizonte, Laboratorio de Tecnologia Farmaceutica, Departamento de Produtos Farmaceuticos, Faculdade de Farmacia, Universidade Federal de Minas Gerais, Belo Horizonte

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