کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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2502143 | 1557374 | 2013 | 14 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: A novel pH-sensitive interferon-β (INF-β) oral delivery system for application in multiple sclerosis A novel pH-sensitive interferon-β (INF-β) oral delivery system for application in multiple sclerosis](/preview/png/2502143.png)
pH-sensitive microparticles were prepared using trimethyl-chitosan (TMC), poly(ethylene glycol)dimethacrylate (PEGDMA) and methacrylic acid (MAA) by free radical suspension polymerization, for the oral delivery of interferon-β (INF-β). The microparticles were subsequently compressed into a suitable oral tablet formulation. A Box–Behnken experimental design was employed for generating a series of formulations with varying concentrations of TMC (0.05–0.5 g/100 mL) and percentage crosslinker (polyethylene glycol diacrylate) (3–8%, w/w of monomers), for establishment of an optimized TMC-PEGDMA-MAA copolymeric microparticles. For pragmatism, insulin was initially employed as the model peptide for undertaking the preliminary experimentation and the optimized formulation was subsequently evaluated using INF-β. The prepared copolymeric microparticulate system was characterized for its morphological, porositometric and mucoadhesive properties. The optimized microparticles with 0.5 g/100 mL TMC and 3% crosslinker had an INF-β loading efficiency of 53.25%. The in vitro release of INF-β was recorded at 74% and 3% in intestinal (pH 6.8) and gastric (pH 1.2) pH from the oral tablet formulation, respectively. The tablet was further evaluated for plasma concentration of INF-β in the New Zealand White rabbit, and compared to a known subcutaneous formulation. The system showed an astounding effective release profile over 24 h with higher INF-β plasma concentrations compared with the subcutaneous injection formulation.
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Journal: International Journal of Pharmaceutics - Volume 456, Issue 2, 18 November 2013, Pages 459–472