Allopurinol encapsulated in polycyanoacrylate nanoparticles as potential lysosomatropic carrier

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dc.contributor.authorGonzález-Martín, G
dc.contributor.authorFigueroa, C
dc.contributor.authorMerino, I
dc.contributor.authorOsuna, A
dc.date.accessioned2025-01-21T01:31:31Z
dc.date.available2025-01-21T01:31:31Z
dc.date.issued2000
dc.description.abstractThe activity of allopurinol-loaded polyethylcyanoacrylate nanoparticles against Trypanosoma cruzi was compared to that of free allopurinol using in vitro cultures of epimastigotes. Ethylcyanoacrylate nanoparticles were prepared by an emulsion polymerization process, and formulations containing different concentrations of allopurinol, polyethylcyanoacrylate and surfactants were investigated and analyzed in size and amount of drug entrapped. The nanoparticles obtained were less than 200 nm in size, as measured by electron microscopy and cytometry. The peak amount of allopurinol entrapped in the nanoparticles was 62.8 +/- 1.9 mu g mg(-1) of nanoparticles using 400 mu l of polyethylcyanoacrylate, 200 mu l of surfactant (Tween 20) and 20 mg of allopurinol in 50 mi of polymerization medium and the association efficiency was 100.7%. After 6 h of incubation at pH 7.4 the release of allopurinol from the nanoparticles was 7.4%, while at pH 1.2 only 3.1% was released after 4-6 h (t = 42.8, P < 0.0001). The in vitro studies, using cultures of T. cruzi epimastigotes, demonstrated considerable increases in the trypanocidal activity of the allopurinol-loaded nanoparticles in comparison with a standard solution of allopurinol (91.5 vs. 45.9%) at an allopurinol concentration of 16.7 mu g ml(-1). In addition, it was shown that the unloaded nanoparticles, by mechanisms not completely elucidated, had a trypanocidal activity similar to that of standard solutions of allopurinol. To study cytotoxicity, increasing concentrations of unloaded nanoparticles were incubated on vero-line cell cultures. The concentration that killed 50% cells was 200 mu g ml(-1), four times higher than that necessary to kill 50% of T. cruzi. It is concluded that the polyethylcyanoacrylate nanoparticles constitute a good carrier of drugs against the T. cruzi. The allopurinol loaded-nanoparticles significantly increased the trypanocidal activity in comparison to the free drug. (C) 2000 Elsevier Science B.V. All rights reserved.
dc.fuente.origenWOS
dc.identifier.issn0939-6411
dc.identifier.urihttps://repositorio.uc.cl/handle/11534/97084
dc.identifier.wosidWOS:000087462800006
dc.issue.numero2
dc.language.isoen
dc.pagina.final142
dc.pagina.inicio137
dc.revistaEuropean journal of pharmaceutics and biopharmaceutics
dc.rightsacceso restringido
dc.subjectallopurinol
dc.subjectdrug carrier
dc.subjectnanoparticles
dc.subjectpolycyanoacrylates
dc.subjectTrypanosoma cruzi
dc.subject.ods03 Good Health and Well-being
dc.subject.odspa03 Salud y bienestar
dc.titleAllopurinol encapsulated in polycyanoacrylate nanoparticles as potential lysosomatropic carrier
dc.typeartículo
dc.volumen49
sipa.indexWOS
sipa.trazabilidadWOS;2025-01-12
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