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Int J Pharm ; 548(2): 803-811, 2018 Sep 15.
Article in English | MEDLINE | ID: mdl-29031981

ABSTRACT

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.


Subject(s)
Antineoplastic Agents/pharmacokinetics , Bronchial Neoplasms , Drug-Eluting Stents , Gefitinib/pharmacokinetics , Polyurethanes/pharmacokinetics , Tracheal Neoplasms , Antineoplastic Agents/administration & dosage , Antineoplastic Agents/chemistry , Bronchial Neoplasms/drug therapy , Bronchial Neoplasms/metabolism , Drug Liberation , Gefitinib/administration & dosage , Gefitinib/chemistry , Polyurethanes/administration & dosage , Polyurethanes/chemistry , Tracheal Neoplasms/drug therapy , Tracheal Neoplasms/metabolism , X-Ray Diffraction/methods
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