Characterization of calcium alginate beads of 5-fluorouracil for colon delivery

Hetal K Patel, Amrita Nagle, R S R Murthy

Abstract


Amultiparticulate system combining pH-sensitive property and specific biodegradability for colon targeted delivery of 5-fluorouracil (5-FU) was examined. The purpose of this study was to prepare and evaluate the colon-specific alginate beads of 5-FU for the treatment of colon cancer. Calcium alginate beads were prepared by extruding 5-FU loaded alginate solution to calcium chloride solution, and gelled spheres were formed instantaneously by ionotropic gelation reaction using different ratios of FU and alginate, alginate and calcium chloride, stirring speeds (500-1500 rpm), and reaction time. The
core beads were coated with Eudragit S-100 to prevent drug release in the stomach and provide controlled dissolution of enteric coat in the small intestine and maximum drug release in the colon. Morphology and surface characteristics of the formulation were determined by scanning electron microscopy. In vitro drug release studies were performed in conditions simulating stomach to colon transit. No significant release was observed at acidic pH, however, when it reached the pH
where Eudragit S-100 starts to dissolve, drug release was observed. Also, release of drug was found to be higher in presence of rat caecal content.


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References


Rang HP, Dale MM. Pharmacology. 1st ed. UK; 1988. p. 609.

Laueence DR, Bennet PN. Clinical pharmacology. 6th ed. UK: ELBS;

p. 719-30.

Controlled drug delivery. In: Bruck SD, editor. Vol. 2. CRC Press; 1982.

p. 190.

Uekama M, Horikawa T, Yamanaka M, Hiramaya F. Peracylated

b-cyclodextrins as novel sustained release carries for a water soluble

drug, molsidomine. J Pharm Pharmacol 1994;46:714-7.

Krishnaiah YS, Veer Raju P, Dinesh Kumar B, Bhaskar P, Satyanarayana V. Development of colon targeted drug delivery systems for mebendazole.

J Control Rel 2001;77:87-95.

Krishnaiah YS, Satyanarayana V, Kumar DB, Karthikeyan RS, Bhaskar

P. In vivo pharmacokinetics in human volunteers: Oral administered

guar gum-based colon-targeted 5-fluorouracil tablets. Eur J Pharm Sci

;19:355-62.

Atyab F, Inanloo K, Dinarvand. Bovin serum albumin-loaded pectinate

beads as colonic peptide delivery system: Preparation and invitro

characterization. Drug Deliv 2005;12:367-75.

Paharia A, Yadav AK, Rai G, Jain SK, Pancholi SS, Agrawal GP. Eudragit-

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

PharmSciTech 2007;8:12.

Atyab F, Inanloo K, Dinarvand. Bovin serum albumin-loaded pectinate

beads as colonic peptide delivery system: Preparation and invitro

characterization. Drug Deliv 2005;12:367-75.

Tozaki M, Emi Y, Horisaka E, Fujita T, Yamamoto A, Muranishi S.

Degradation of insulin and calcitonin and their protection by various

protease inhibitors in rat caecal contents: Implications in peptide

delivery to the colon. J Pharm Pharmacol 1997;49:164-8.

Vandelli MA, Leo E, Forni F, Bernatei MT. In vitro evaluation of a potential colonic drug delivery system that releases drug after a controllable lag-time. Eur J Pharm Biopharm 1996;43:148-51.

Barar FS. Essentials of pharmacotneraperitics. 2nd ed. New Delhi: S.

Chand and Company Ltd; 1992. p. 778.




DOI: http://dx.doi.org/10.22377/ajp.v2i4.196

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