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• W2119196996 endingPage "1908" @default.
• W2119196996 startingPage "1896" @default.
• W2119196996 abstract "Gelatin-methotrexate microspheres for intra-tumor administration have possibilities for minimizing systemic toxicities of methotrexate (MTX) and overcoming its resistance. Gelatin-MTX conjugates prepared by a carbodiimide reaction were crosslinked with glutaraldehyde to form microspheres (MTX:gelatin molar ratios of 2:1, 15:1, and 21:1). Microspheres were evaluated under in vitro tumor conditions at pH 6.5 and 37 degrees C with and without Cathepsin B (Cat B). Some microspheres were capped with an ethanolamine/cyanoborohydride procedure. SEM of broken microspheres revealed a hollow shell structure. Superficial Cat B degradation influenced some free MTX release but produced no conjugate fragment release. HPLC measured release of fragments (<10 kDa) was very little and release of free MTX was small. However, higher drug load microspheres released less free MTX than lower drug load, a substantial lag phase of free MTX release from capped microspheres changed to an initial rapid release in uncapped microspheres, and fragments were only released from uncapped microspheres. Opened unstable Schiff base crosslinks in uncapped microspheres may allow enzyme to produce conjugate fragments not observed in capped microspheres. Free MTX release may occur from dissolved uncrosslinked conjugate within the hollow microspheres. Important relationships and observations are described that will be useful for gelatin and perhaps other proteinaceous microspheres." @default.
• W2119196996 created "2016-06-24" @default.
• W2119196996 creator A5045779971 @default.
• W2119196996 creator A5072068799 @default.
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• W2119196996 date "2006-09-01" @default.
• W2119196996 modified "2023-09-23" @default.
• W2119196996 title "Gelatin-Methotrexate Conjugate Microspheres as a Potential Drug Delivery System" @default.
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• W2119196996 doi "https://doi.org/10.1002/jps.20572" @default.
• W2119196996 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16850436" @default.
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