title: Properties of PLA/PCL particles as vehicles for oral delivery of the androgen hormone 17α-methyltestosterone.
abstract: 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.
authors.affiliation: Department of Engineering of Materials and of Bioprocesses, School of Chemical Engineering, University of Campinas, Av. Albert Einstein 500, 13083-852 Campinas, Brazil. Electronic address: prisacchetin@gmail.com.
authors.forename: Priscila Soares Costa
authors.initials: PS
authors.lastname: Sacchetin
authors.affiliation: Department of Physical Chemistry, Institute of Chemistry, University of Campinas, Rua Josué de Castro 6154, 13083-970 Campinas, Brazil. Electronic address: rafashe@gmail.com.
authors.forename: Rafaela Ferreira
authors.initials: RF
authors.lastname: Setti
authors.affiliation: Department of Physical Chemistry, Institute of Chemistry, University of Campinas, Rua Josué de Castro 6154, 13083-970 Campinas, Brazil. Electronic address: paulorosa@iq.unicamp.br.
authors.forename: Paulo de Tarso
authors.initials: Pde T
authors.lastname: Vieira e Rosa
authors.affiliation: Department of Engineering of Materials and of Bioprocesses, School of Chemical Engineering, University of Campinas, Av. Albert Einstein 500, 13083-852 Campinas, Brazil. Electronic address: ammoraes@feq.unicamp.br.
authors.forename: Ângela Maria
authors.initials: ÂM
authors.lastname: Moraes
mesh_terms: D000284:Administration, Oral; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D005260:Female; D006863:Hydrogen-Ion Concentration; D007700:Kinetics; D019344:Lactic Acid / Q000737:chemistry*; D008297:Male; D008777:Methyltestosterone / Q000008:administration & dosage / Q000737:chemistry* / Q000378:metabolism; D008962:Models, Theoretical; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry*; D012727:Sex Characteristics; D017210:Tilapia
chemical_list: D004337:Drug Carriers; D011091:Polyesters; D011108:Polymers; C016240:polycaprolactone; D019344:Lactic Acid; C033616:poly(lactide); D008777:Methyltestosterone
keywords: 17α-Methyltestosterone; PCL; PLA; Particles; Supercritical fluid