Fabrication and characterization of gefitinib-releasing polyurethane foam as a coating for drug-eluting stent in the treatment of bronchotracheal cancer

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.

Solid Dispersions of Gefitinib Prepared by Spray Drying with Improved Mucoadhesive and Drug Dissolution Properties

“…Several diffraction peaks are clear in the diffractogram of ZD at 15.1°, 16.1°, 18.6°, 19.2°, 20.6°, 22.5°, 24.2°26.2°and 26.4°. Similar peaks were reported in previous study which were attributed to drug crystallinity (27). PVP, HPMC and Eudragit S100 showed no sharp peaks in their diffractograms which is attributed to their availability in the amorphous form.…”

Biomedical Polyurethanes for Anti-Cancer Drug Delivery Systems: A Brief, Comprehensive Review

“…Drug-release studies showed a sustained highly controlled release of GEF over nine months (with zero-order kinetics). The developed biomaterial is dedicated for the palliative treatment of bronchotracheal cancer [ 70 ]. Another fascinating DDS with very high cytostatic (PACL) release control for 10 days is temperature-responsive PUs (obtained from MDI, PCL, and BDO) [ 71 ].…”

Production of Rigid Polyurethane Foams Using Polyol from Liquefied Oil Palm Biomass: Variation of Isocyanate Indexes

“…In Figure 6a, a broad peak at 3600-3200 cm -1 (stretching vibration of O-H) and peaks at 2920 cm -1 (asymmetric stretching vibration of C-H), 2870 cm -1 (symmetric stretching In Figure 6a, a broad peak at 3600-3200 cm −1 (stretching vibration of O-H) and peaks at 2920 cm −1 (asymmetric stretching vibration of C-H), 2870 cm −1 (symmetric stretching vibration of C-H), and 1100 cm −1 (C-O-C) belong to the EFB polyol. Common peaks that represent functionalities of urethanes and ureas in PU, such as a broad peak at 3300 cm −1 (stretching vibration of amine (N-H) in urethane linkages); peaks at 1720 cm −1 (free C=O of urethanes), 1705 cm −1 (H-bonded C=O of urethanes), 1595 cm −1 (aromatic group of p-MDI), 1510 cm −1 (bending vibration of N-H), 1415 cm −1 (isocyanurate ring), 1360 cm −1 (aromatic amine C−N stretching from p-MDI) [38], 1215 cm −1 (stretching vibration of C-N in urethane linkages) [27], and 1080 cm −1 (C-O-C of urethanes); and a shoulder peak at 1650 cm −1 (N-H of urea) [39] are present in all EFBPUFs spectra.…”