Eudragit-coated pectin microspheres of 5-fluorouracil for colon targeting.

作者: Amol Paharia , Awesh K Yadav , Gopal Rai , Sunil K Jain , Shyam S Pancholi

DOI: 10.1208/PT0801012

关键词: EmulsionChromatographyPectinParticle sizeDehydrationPolymer ratioChemistryMicrosphereControlled releaseFluorouracil

摘要: An objective of the present investigation was to prepare and evaluate Eudragit-coated pectin microspheres for colon targeting 5-fluorouracil (FU). Pectin were prepared by emulsion dehydration method using different ratios FU (1:3 1:6), stirring speeds (500–2000 rpm) emulsifier concentrations (0.75%–1.5% wt/vol). The yield preparation encapsulation efficiencies high all microspheres. Microspheres drug:polymer ratio 1:4, speed 1000 rpm, 1.25% wt/vol concentration emulsifying agent selected as an optimized formulation. Eudragit-coating performed oil-in-oil solvent evaporation coat: core (5:1). evaluated surface morphology, particle size distribution, swellability, percentage drug entrapment, in vitro release simulated gastrointestinal fluids (SGF). study formulation also colonic fluid presence 2% rat cecal content. Organ distribution albino rats establish potential colon. profile from pH dependent. In acidic medium, rate much slower; however, released quickly at 7.4. It is concluded that are promising controlled carriers colon-targeted delivery FU.

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