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Mater Sci Eng C Mater Biol Appl ; 58: 870-81, 2016 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-26478382

RESUMEN

The aim of this study was to produce PLA (poly(lactic acid)) and PCL (polycaprolactone) oral carriers through the precipitation of the polymer solutions using supercritical CO2 as an antisolvent for the controlled release of the hydrophobic model drug 17α-methyltestosterone (MT). Such drug is a steroidal hormone used orally to develop and sustain primary and secondary male sex characteristics, e.g. for female Nile tilapia sex reversal in aquaculture. The influence of hormone, PLA and PCL concentrations on particle formation was analyzed, showing that high PCL concentrations produced particles with rougher surfaces and greater mean diameters. The incorporation efficiency of MT ranged from 20 to 51%, and its addition resulted in increases in particle mean diameter from 23 to 54 µm. Aggregation was observed for particles incorporating or not MT and high concentrations of MT led to the formation of more amorphous structures, changing the thermal behavior of the particles. The exposure of the PLA/PCL particles to pH conditions simulating gastrointestinal fish conditions showed that hormone release fraction at acidic pH ranged from 8 to 63% (over 2h), while in the basic pH the proportion released varied from 23 to 60% (over 10h), reaching levels adequate for the desired in vivo activity.


Asunto(s)
Portadores de Fármacos/química , Ácido Láctico/química , Metiltestosterona/química , Poliésteres/química , Polímeros/química , Administración Oral , Animales , Liberación de Fármacos , Femenino , Concentración de Iones de Hidrógeno , Cinética , Masculino , Metiltestosterona/administración & dosificación , Metiltestosterona/metabolismo , Modelos Teóricos , Tamaño de la Partícula , Caracteres Sexuales , Tilapia
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