Eudragit-coated pectin microspheres of 5-fluorouracil for colon targeting |
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Authors: | Amol Paharia Awesh K Yadav Gopal Rai Sunil K Jain Shyam S Pancholi Govind P Agrawal |
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Institution: | (1) Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, 470 003 Sagar, (M.P.), India;(2) SLT Institute of Pharmaceutical Sciences, Guru Ghasidas University, 495 009 Bilaspur, (C.G.), India;(3) Shree Dhanvantary Pharmacy College, Kim, District Surat, 94110 Gujrat, India |
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Abstract: | An objective of the present investigation was to prepare and evaluate Eudragit-coated pectin microspheres for colon targeting
of 5-fluorouracil (FU). Pectin microspheres were prepared by emulsion dehydration method using different ratios of FU and
pectin (1:3 to 1:6), stirring speeds (500–2000 rpm) and emulsifier concentrations (0.75%–1.5% wt/vol). The yield of preparation
and the encapsulation efficiencies were high for all pectin microspheres. Microspheres prepared by using drug:polymer ratio
1:4, stirring speed 1000 rpm, and 1.25% wt/vol concentration of emulsifying agent were selected as an optimized formulation.
Eudragit-coating of pectin microspheres was performed by oil-in-oil solvent evaporation method using coat: core ratio (5:1).
Pectin microspheres and Eudragit-coated pectin microspheres were evaluated for surface morphology, particle size and size
distribution, swellability, percentage drug entrapment, and in vitro drug release in simulated gastrointestinal fluids (SGF).
The in vitro drug release study of optimized formulation was also performed in simulated colonic fluid in the presence of
2% rat cecal content. Organ distribution study in albino rats was performed to establish the targeting potential of optimized
formulation in the colon. The release profile of FU from Eudragit-coated pectin microspheres was pH dependent. In acidic medium,
the release rate was much slower; however, the drug was released quickly at pH 7.4. It is concluded from the present investigation
that Eudragit-coated pectin microspheres are promising controlled release carriers for colon-targeted delivery of FU.
Published: February 16, 2007 |
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Keywords: | 5-Fluorouracil pectin microspheres Eudragit coating colon targeting |
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