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Design, Development, and Optimization of Sterculia Gum-Based Tablet Coated with Chitosan/Eudragit RLPO Mixed Blend Polymers for Possible Colonic Drug Delivery.

Nath B, Nath LK - J Pharm (Cairo) (2012)

Bottom Line: Chitosan in the mixed film coat was found to be degraded by enzymatic action of the microflora in the colon.Release kinetic data revealed that the optimized MCDDS was fitted well into first-order model, and apparent lag time was found to be 6 hours, followed by Higuchi release kinetics.In vivo study in rabbits shows delayed T max, prolonged absorption time, decreased C max, and absorption rate constant (Ka), indicating a reduced systemic toxicity of the drug as compared to other dosage forms.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Sciences, Girijananda Chowdhury Institute of Pharmaceutical Sciences (GIPS), Azara, Assam, Guwahati 781001, India ; Girijananda Chowdhury Institute of Pharmaceutical Sciences (GIPS) Affiliated to Gauhati University, Azara, Assam, Guwahati 781017, India.

ABSTRACT
The purpose of this study is to explore the possible applicability of Sterculia urens gum as a novel carrier for colonic delivery system of a sparingly soluble drug, azathioprine. The study involves designing a microflora triggered colon-targeted drug delivery system (MCDDS) which consists of a central polysaccharide core and is coated to different film thicknesses with blends of chitosan/Eudragit RLPO, and is overcoated with Eudragit L00 to provide acid and intestinal resistance. The microflora degradation property of gum was investigated in rat caecal medium. Drug release study in simulated colonic fluid revealed that swelling force of the gum could concurrently drive the drug out of the polysaccharide core due to the rupture of the chitosan/Eudargit coating in microflora-activated environment. Chitosan in the mixed film coat was found to be degraded by enzymatic action of the microflora in the colon. Release kinetic data revealed that the optimized MCDDS was fitted well into first-order model, and apparent lag time was found to be 6 hours, followed by Higuchi release kinetics. In vivo study in rabbits shows delayed T max, prolonged absorption time, decreased C max, and absorption rate constant (Ka), indicating a reduced systemic toxicity of the drug as compared to other dosage forms.

No MeSH data available.


Related in: MedlinePlus

Effect of increasing coating thickness of eudragit RLPO (FC1-10% w/w), (FC2-12% w/w) and (FC3-14% w/w) on in vitro drug release in SCF. Each point represents the mean ± SD.
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fig3: Effect of increasing coating thickness of eudragit RLPO (FC1-10% w/w), (FC2-12% w/w) and (FC3-14% w/w) on in vitro drug release in SCF. Each point represents the mean ± SD.

Mentions: It was observed that increased in the level of weight gain from 10%, 12%, and 14% in the batches of FC1, FC2, and FC3 and keeping the concentration of chitosan constant at 15% w/w made chitosan particles less susceptible to bacterial attack, resulting in longer lag time and lesser percentage of drug released in 18 h owing to less accessibility of the chitosan particles across the eudragit coat by the colonic bacteria. Figure 3 shows that as the coating thickness was increased, drug release was decreased, as evidenced by the difference factor f1 value which was lower than 15. For the calculation of f1 and f2 (similarity factor) values, only one data point at which more than 85% of the drug release had been released was taken into consideration. Drug release decreased.


Design, Development, and Optimization of Sterculia Gum-Based Tablet Coated with Chitosan/Eudragit RLPO Mixed Blend Polymers for Possible Colonic Drug Delivery.

Nath B, Nath LK - J Pharm (Cairo) (2012)

Effect of increasing coating thickness of eudragit RLPO (FC1-10% w/w), (FC2-12% w/w) and (FC3-14% w/w) on in vitro drug release in SCF. Each point represents the mean ± SD.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC4595939&req=5

fig3: Effect of increasing coating thickness of eudragit RLPO (FC1-10% w/w), (FC2-12% w/w) and (FC3-14% w/w) on in vitro drug release in SCF. Each point represents the mean ± SD.
Mentions: It was observed that increased in the level of weight gain from 10%, 12%, and 14% in the batches of FC1, FC2, and FC3 and keeping the concentration of chitosan constant at 15% w/w made chitosan particles less susceptible to bacterial attack, resulting in longer lag time and lesser percentage of drug released in 18 h owing to less accessibility of the chitosan particles across the eudragit coat by the colonic bacteria. Figure 3 shows that as the coating thickness was increased, drug release was decreased, as evidenced by the difference factor f1 value which was lower than 15. For the calculation of f1 and f2 (similarity factor) values, only one data point at which more than 85% of the drug release had been released was taken into consideration. Drug release decreased.

Bottom Line: Chitosan in the mixed film coat was found to be degraded by enzymatic action of the microflora in the colon.Release kinetic data revealed that the optimized MCDDS was fitted well into first-order model, and apparent lag time was found to be 6 hours, followed by Higuchi release kinetics.In vivo study in rabbits shows delayed T max, prolonged absorption time, decreased C max, and absorption rate constant (Ka), indicating a reduced systemic toxicity of the drug as compared to other dosage forms.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmaceutical Sciences, Girijananda Chowdhury Institute of Pharmaceutical Sciences (GIPS), Azara, Assam, Guwahati 781001, India ; Girijananda Chowdhury Institute of Pharmaceutical Sciences (GIPS) Affiliated to Gauhati University, Azara, Assam, Guwahati 781017, India.

ABSTRACT
The purpose of this study is to explore the possible applicability of Sterculia urens gum as a novel carrier for colonic delivery system of a sparingly soluble drug, azathioprine. The study involves designing a microflora triggered colon-targeted drug delivery system (MCDDS) which consists of a central polysaccharide core and is coated to different film thicknesses with blends of chitosan/Eudragit RLPO, and is overcoated with Eudragit L00 to provide acid and intestinal resistance. The microflora degradation property of gum was investigated in rat caecal medium. Drug release study in simulated colonic fluid revealed that swelling force of the gum could concurrently drive the drug out of the polysaccharide core due to the rupture of the chitosan/Eudargit coating in microflora-activated environment. Chitosan in the mixed film coat was found to be degraded by enzymatic action of the microflora in the colon. Release kinetic data revealed that the optimized MCDDS was fitted well into first-order model, and apparent lag time was found to be 6 hours, followed by Higuchi release kinetics. In vivo study in rabbits shows delayed T max, prolonged absorption time, decreased C max, and absorption rate constant (Ka), indicating a reduced systemic toxicity of the drug as compared to other dosage forms.

No MeSH data available.


Related in: MedlinePlus