Penetration of polymeric nanoparticles loaded with an HIV-1 inhibitor peptide derived from GB virus C in a vaginal mucosa model

[Display omitted] Despite the great effort to decrease the HIV infectivity rate, current antiretroviral therapy has several weaknesses; poor bioavailability, development of drug resistance and poor ability to access tissues. However, molecules such as peptides have emerged asa new expectative to HIV...

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Bibliographic Details
Published in:European journal of pharmaceutics and biopharmaceutics 2017-11, Vol.120, p.98-106
Main Authors: Ariza-Sáenz, Martha, Espina, Marta, Bolaños, Nuria, Calpena, Ana Cristina, Gomara, María José, Haro, Isabel, García, María Luisa
Format: Article
Language:English
Subjects:
Animals
Anti-HIV Agents - administration & dosage
Anti-HIV Agents - chemistry
Biological Availability
Chitosan - chemistry
Drug Carriers - chemistry
Drug delivery systems
Drug Delivery Systems - methods
Female
Fusion inhibitor peptide
GB virus C - metabolism
HIV Infections - drug therapy
HIV-1
HIV-1 - drug effects
In vitro peptide release
In vivo and ex vivo permeation studies
Membrana mucosa
Mucous membrane
Mucous Membrane - metabolism
Nanoparticles
Nanoparticles - administration & dosage
Nanoparticles - chemistry
Nanopartícules
Peptides
Peptides - administration & dosage
Peptides - chemistry
Polymeric nanoparticles
Polymers - chemistry
Pèptids
Sistemes d'alliberament de medicaments
Swine
Tandem Mass Spectrometry - methods
Vagina
Vagina - metabolism
Vaginal mucosa
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Summary:[Display omitted] Despite the great effort to decrease the HIV infectivity rate, current antiretroviral therapy has several weaknesses; poor bioavailability, development of drug resistance and poor ability to access tissues. However, molecules such as peptides have emerged asa new expectative to HIV eradication. The vaginal mucosa is the main spreading point of HIV. There are natural barriers such as the vaginal fluid which protects the vaginal epithelium from any foreign agents reaching it. This work has developed and characterized Nanoparticles (NPs) coated with glycol chitosan (GC), loaded with an HIV-1 inhibitor peptide (E2). In vitro release and ex vivo studies were carried out using the vaginal mucosa of swine and the peptide was determined by HPLC MS/MS validated method. Moreover, the peptide was labeled with 5(6)-carboxyfluoresceine and entrapped into the NPs to carried out in vivo studies and to evaluate the NPs penetration and toxicity in the vaginal mucosa of the swine. The mean size of the NPs, ξ and the loading percentage were fundamental features for to reach the vaginal tissue and to release the peptide within intercellular space. The obtained results suggesting that the fusion inhibitor peptides loaded into the NPs coated with GC might be a new way to fight the HIV-1, due to the formulation might reach the human epithelial mucosa and release peptide without any side effects.
ISSN:0939-6411
1873-3441
DOI:10.1016/j.ejpb.2017.08.008