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Int J Pharm ; 548(2): 803-811, 2018 Sep 15.
Artigo em Inglês | MEDLINE | ID: mdl-29031981

RESUMO

The purpose of the present study was to develop gefitinib-loaded polymeric foams that can be used as coating of drug-eluting stents for palliative treatment of bronchotracheal cancer. Release of such an anticancer drug from such stent coating can retard tumor regrowth into the bronchial lumen. Gefitinib-loaded polyurethane (PU) foams were prepared by embedding either gefitinib micronized crystals or gefitinib-loaded poly(lactic-co-glycolic acid) microspheres in water-blown films, with up to 10% w/w loading for gefitinib microcrystals and 15% w/w for gefitinib microspheres (corresponding to 1.0% w/w drug loading). Drug-release studies showed sustained release of gefitinib over a period of nine months, with higher absolute release rates at higher drug loading content. By the end of the studied nine month release periods, 60-100% of the loaded gefitinib had been released. Foams loaded with gefitinib-PLGA microspheres at 15% w/w showed accelerated drug release after 4 months, coinciding with the degradation of PLGA microparticles in the PU foam as demonstrated by scanning electron microscopy (SEM). When applied on a nitinol braided bronchotrachial stent, PU coatings with gefitinib microspheres showed similar mechanical properties as the drug-free PU coating, which indicated that the loading of microspheres did not affect the mechnical properties of the PU foams. In conclusion, we have fabricated drug-loaded PU foams that are suitable for bronchotracheal stent coating.


Assuntos
Antineoplásicos/farmacocinética , Neoplasias Brônquicas , Stents Farmacológicos , Gefitinibe/farmacocinética , Poliuretanos/farmacocinética , Neoplasias da Traqueia , Antineoplásicos/administração & dosagem , Antineoplásicos/química , Neoplasias Brônquicas/tratamento farmacológico , Neoplasias Brônquicas/metabolismo , Liberação Controlada de Fármacos , Gefitinibe/administração & dosagem , Gefitinibe/química , Poliuretanos/administração & dosagem , Poliuretanos/química , Neoplasias da Traqueia/tratamento farmacológico , Neoplasias da Traqueia/metabolismo , Difração de Raios X/métodos
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