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Artigo Produção Nacional
BIBTEX RIS

Monitoring structural features, biocompatibility and biological efficacy of gamma-irradiated methotrexate-loaded spray-dried microparticles

2017; Elsevier BV; Volume: 80; Linguagem: Inglês

10.1016/j.msec.2017.06.013

ISSN

1873-0191

Autores

Alice Rodrigues de Oliveira, Philippe C. Mesquita, Paula Renata Lima Machado, Kléber Juvenal Silva Farias, Yêda Medeiros Bastos de Almeida, Matheus de Freitas Fernandes‐Pedrosa, Alianda Maira Cornélio, Eryvaldo Sócrates Tabosa do Egito, Arnóbio Antônio da Silva-Júnior,

Tópico(s)

Nanoparticle-Based Drug Delivery

Resumo

In this study, biodegradable and biocompatible gamma irradiated poly-(dl-lactide-co-glycolide) (PLGA) spray-dried microparticles were prepared aiming to improve the efficacy of methotrexate (MTX). The experimental design included three formulations of microparticles containing distinct drug amount (9%, 18%, and 27% w/w) and three distinct gamma irradiation dose (15 kGy, 25 kGy, and 30 kGy). The physicochemical and drug release properties of the microparticles supported their biocompatibility and biological efficacy studies in different cell lines. The irradiation induced slight changes in the spherical shape of the microparticles and the formation of free radicals was dependent on the drug loading. However, the amorphous character, particle size, drug loading, and drug release rate of the microparticles were preserved. The drug release data from all microparticles formulation were evaluated by using four drug kinetic models and by comparison of their similarity factor (f2). The gamma irradiation did not induce changes in the biocompatibility of PLGA microparticles and in the biological activity of the MTX-loaded microparticles. Finally, the spray-dried MTX-loaded PLGA microparticles enhanced the efficacy of the drug in the human cervical cancer cells (SiHa cell line). This study demonstrated the feasibility of the gamma irradiated spray dried PLGA microparticles for prolonged release of MTX, supporting a promising antitumor-drug delivery system for parenteral (subcutaneous) or pulmonary use.

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