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.
journal_name
Curr Drug Delivjournal_title
Current drug deliveryauthors
De Marco Almeida F,Silva CN,de Araujo Lopes SC,Santos DM,Torres FS,Cardoso FL,Martinelli PM,da Silva ER,de Lima ME,Miranda LAF,Oliveira MCdoi
10.2174/1567201815666180108170206subject
Has Abstractpub_date
2018-01-01 00:00:00pages
1064-1071issue
7eissn
1567-2018issn
1875-5704pii
CDD-EPUB-87779journal_volume
15pub_type
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