Permeability and in vivo distribution of poly(epsilon-caprolactone) nanoparticles loaded with zidovudine

Autor(es)

Magalhaes, Milena C. R. S. ^{[1, 2]} ; Castro, Brenda F. M. ^[1] ; de Castro, Whocely V. ^[3] ; Barros, Andre L. B. ^[1] ; Fernandes, Renata S. ^[1] ; Silva-Cunha, Armando ^[1] ; Fialho, Silvia L. ^[2]

Afiliação do(s) autor(es)

^[1] Univ Fed Minas Gerais, Fac Pharm, Ave Presidente Antonio Carlos 6627, BR-31270901 Belo Horizonte, MG - Brazil

^[2] Ezequiel Dias Fdn, Pharmaceut Res & Dev, Rua Conde Pereira Carneiro 80, BR-30510010 Belo Horizonte, MG - Brazil

^[3] Univ Fed Sao Joao del Rei, Fac Pharm, Rua Sebastiao Goncalves Coelho 400, BR-35501296 Divinopolis, MG - Brazil

• Tipo de documento: Artigo Científico
• Fonte: JOURNAL OF NANOPARTICLE RESEARCH; v. 20, n. 7 JUN 27 2018.
• Citações Web of Science: 0

Resumo

Zidovudine (AZT) is one of first choice drugs for the treatment of acquired immunodeficiency syndrome (AIDS). Despite its efficacy to control virus replication, the extent of adverse effects and the therapeutic regimen are directly related to patients' non-compliance. In this work, we evaluated the permeability and in vivo distribution of AZT incorporated into poly(-caprolactone), PCL, nanoparticles (AZT-NP) aiming to reduce the normally observed side effects and increase the drug bioavailability. AZT-NP were obtained by interfacial deposition of preformed polymer. The mean diameter of the nanoparticles was 283.4 nm +/- 17.0 with a polydispersity index of 0.232 +/- 0.073. The nanoparticles presented a zeta potential of -32.4 mV +/- 3.3, en-trapment rate of 53.11% +/- 9.25, and were stable for at least 7 days. The drug and the polymer showed no incompatibility in thermal analysis. The permeability of AZT across Caco-2 cells was 22-fold higher for AZT-NP compared to the drug solution. The nanoparticles were able to release AZT in vivo after oral administration in mice, and the plasma levels of labeled AZT-NP were higher and more constant when compared to free labeled AZT. Thus, AZT-NP demonstrated superior performance compared to the drug solution in vivo and in vitro, showing the potential of this system for the treatment of AIDS. (AU)

• Processo FAPESP: 14/50928-2 - INCT 2014: Nanotecnologia Farmacêutica: uma abordagem transdisciplinar
• Beneficiário: Maria Vitória Lopes Badra Bentley
• Modalidade de apoio: Auxílio à Pesquisa - Temático