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Open AccessArticle

Lipid Vesicles Loaded with an HIV-1 Fusion Inhibitor Peptide as a Potential Microbicide

1
Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy, University of Barcelona, 08028 Barcelona, Spain
2
Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08028 Barcelona, Spain
3
Centro de Investigación Biomédica en Red de Enfermedades Neurodegenerativas (CIBERNED), University of Barcelona, 08028 Barcelona, Spain
4
Unit of Synthesis and Biomedical Applications of Peptides, Department of Biological Chemistry, IQAC−CSIC, Jordi Girona 18, 08034 Barcelona, Spain
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(6), 502; https://doi.org/10.3390/pharmaceutics12060502
Received: 17 April 2020 / Revised: 28 May 2020 / Accepted: 29 May 2020 / Published: 31 May 2020
(This article belongs to the Special Issue Controlled Release of Nanostructured Drug Systems)
The effective use of fusion inhibitor peptides against cervical and colorectal infections requires the development of sustained release formulations. In this work we comparatively study two different formulations based on polymeric nanoparticles and lipid vesicles to propose a suitable delivery nanosystem for releasing an HIV-1 fusion inhibitor peptide in vaginal mucosa. Polymeric nanoparticles of poly-d,l-lactic-co-glycolic acid (PLGA) and lipid large unilamellar vesicles loaded with the inhibitor peptide were prepared. Both formulations showed average sizes and polydispersity index values corresponding to monodisperse systems appropriate for vaginal permeation. High entrapment efficiency of the inhibitor peptide was achieved in lipid vesicles, which was probably due to the peptide’s hydrophobic nature. In addition, both nanocarriers remained stable after two weeks stored at 4 °C. While PLGA nanoparticles (NPs) did not show any delay in peptide release, lipid vesicles demonstrated favorably prolonged release of the peptide. Lipid vesicles were shown to improve the retention of the peptide on ex vivo vaginal tissue in a concentration sufficient to exert its pharmacological effect. Thus, the small size of lipid vesicles, their lipid-based composition as well as their ability to enhance peptide penetration on vaginal tissue led us to consider this formulation as a better nanosystem than polymeric nanoparticles for the sustained delivery of the HIV-1 fusion inhibitor peptide in vaginal tissues. View Full-Text
Keywords: microbicides; drug delivery system; nanoparticle; fusion inhibitor peptide; vaginal mucosa microbicides; drug delivery system; nanoparticle; fusion inhibitor peptide; vaginal mucosa
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MDPI and ACS Style

Sánchez-López, E.; Paús, A.; Pérez-Pomeda, I.; Calpena, A.; Haro, I.; Gómara, M.J. Lipid Vesicles Loaded with an HIV-1 Fusion Inhibitor Peptide as a Potential Microbicide. Pharmaceutics 2020, 12, 502.

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