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Merck

Formulation, in vitro drug release study and anticancer activity of 5-fluorouracil loaded gellan gum microbeads.

Acta poloniae pharmaceutica (2013-04-25)
S K Sahoo, S K Sahoo, A Behera, S V Patil, S K Panda
RESUMEN

5-Fluorouracil loaded calcium-zinc-gellan and calcium-zinc-gellan-ethyl cellulose microbeads were successfully prepared by simple ionotropic gelation and oil in water ionotropic gelation technique, respectively. Prepared microbeads were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy and evaluated for particle size, drug content, encapsulation efficiency, drug release and cell cytotoxicity study. Microbeads formed were spherical with rough surface. As concentration of gellan and ethyl cellulose has increased encapsulation efficiency, particle size and sustained drug release effect also increased. The release of 5-fluorouracil from microbeads has followed Hixson Crowell model suggesting the mechanism of drug release as dissolution controlled. Cytotoxicity analysis on HT-29 human colon cancer cell lines indicated that 5-FU loaded gellan gum/gellan in combination with ethyl cellulose microbeads leads to sustained releases of drug and thus delayed apoptosis over a long period of time. The formulation with drug:gellan:ethyl cellulose ratio 2.5:7.5:1 was found to be more effectual in terms of sustained drug release activity in addition to anti-cancer activity.

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Sigma-Aldrich
Cloruro de calcio dihydrate, ACS reagent, ≥99%
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Sulfato de cinc heptahidratado, ACS reagent, 99%
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Cloruro de calcio solution, BioUltra, for molecular biology, ~1 M in H2O
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Cloruro de calcio dihydrate, ReagentPlus®, ≥99.0%
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Calcium chloride, anhydrous, BioReagent, suitable for insect cell culture, suitable for plant cell culture, ≥96.0%
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Sulfato de cinc heptahidratado, ReagentPlus®, ≥99.0%
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Cloruro de calcio dihydrate, for molecular biology, ≥99.0%
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Cellulose, microcrystalline, powder, 20 μm
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Cloruro de calcio dihydrate, BioReagent, suitable for cell culture, suitable for insect cell culture, suitable for plant cell culture, ≥99.0%
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Cellulose, microcrystalline, powder
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Sulfato de cinc heptahidratado, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., ≥99.5%
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Cellulose, fibers, (medium)
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Ethyl cellulose, 48.0-49.5% (w/w) ethoxyl basis
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Sulfato de cinc heptahidratado, BioReagent, suitable for cell culture
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Calcium chloride, anhydrous, powder, 99.99% trace metals basis
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Cellulose, Type 20, 20 μm
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Cloruro de calcio dihydrate, BioUltra, for molecular biology, ≥99.5% (KT)
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Ethyl cellulose, 48.0-49.5% (w/w) ethoxyl basis
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Cloruro de calcio dihydrate, puriss. p.a., ACS reagent, reag. Ph. Eur., ≥99%
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α-Cellulose, powder
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Zinc sulfate solution, 0.3 N
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Cloruro de calcio dihydrate, puriss., meets analytical specification of Ph. Eur., USP, FCC, E509, 99-103%, ≤0.0001% Al
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Cellulose, colloidal, microcrystalline
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Sulfato de cinc heptahidratado, BioUltra, for molecular biology, 2.0 M in H2O
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Calcium chloride, AnhydroBeads, −10 mesh, ≥99.9% trace metals basis
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Sulfato de cinc heptahidratado, ≥99.95% trace metals basis
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Ethyl cellulose, viscosity 100 cP, 5 % in toluene/ethanol 80:20(lit.), extent of labeling: 48% ethoxyl
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Ethyl cellulose, viscosity 46 cP, 5 % in toluene/ethanol 80:20(lit.), extent of labeling: 48% ethoxyl
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Cellulose, Type 101, Highly purified, fibers
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Ethyl cellulose, viscosity 4 cP, 5 % in toluene/ethanol 80:20(lit.), extent of labeling: 48% ethoxyl