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Swelling/floating capability and drug release characterizations of gastroretentive drug delivery system based on a combination of hydroxyethyl cellulose and sodium carboxymethyl cellulose.

Chen YC, Ho HO, Liu DZ, Siow WS, Sheu MT - PLoS ONE (2015)

Bottom Line: Of note, floating duration was enhanced when in simulated gastric solution compared to DIW.Further, the hydration of tablets was found to be retarded as the NaCl concentration in the medium increased resulting in smaller gel layers and swelling sizes.The release mechanism of the freely water-soluble drug, metformin, was mainly diffusion-controlled, while those of the water-soluble drug, ciprofloxacin, and the slightly water-soluble drug, esomeprazole, were mainly anomalous diffusion.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan.

ABSTRACT
The aim of this study was to characterize the swelling and floating behaviors of gastroretentive drug delivery system (GRDDS) composed of hydroxyethyl cellulose (HEC) and sodium carboxymethyl cellulose (NaCMC) and to optimize HEC/NaCMC GRDDS to incorporate three model drugs with different solubilities (metformin, ciprofloxacin, and esomeprazole). Various ratios of NaCMC to HEC were formulated, and their swelling and floating behaviors were characterized. Influences of media containing various NaCl concentrations on the swelling and floating behaviors and drug solubility were also characterized. Finally, release profiles of the three model drugs from GRDDS formulation (F1-4) and formulation (F1-1) were examined. Results demonstrated when the GRDDS tablets were tested in simulated gastric solution, the degree of swelling at 6 h was decreased for each formulation that contained NaCMC in comparison to those in de-ionized water (DIW). Of note, floating duration was enhanced when in simulated gastric solution compared to DIW. Further, the hydration of tablets was found to be retarded as the NaCl concentration in the medium increased resulting in smaller gel layers and swelling sizes. Dissolution profiles of the three model drugs in media containing various concentrations of NaCl showed that the addition of NaCl to the media affected the solubility of the drugs, and also their gelling behaviors, resulting in different mechanisms for controlling a drug's release. The release mechanism of the freely water-soluble drug, metformin, was mainly diffusion-controlled, while those of the water-soluble drug, ciprofloxacin, and the slightly water-soluble drug, esomeprazole, were mainly anomalous diffusion. Overall results showed that the developed GRDDS composed of HEC 250HHX and NaCMC of 450 cps possessed proper swelling extents and desired floating periods with sustained-release characteristics.

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Swelling indexes of the combination of PEO 8000K and NaCMC with different ratios in deionized water.
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pone.0116914.g002: Swelling indexes of the combination of PEO 8000K and NaCMC with different ratios in deionized water.

Mentions: To confirm that the swelling ability was related to the repulsive effect of negative charges of carboxylate groups carried by NaCMC, up to 40% of NaCMC of 450 cps was incorporated with another neutral hydrophilic polymer of PEO 8000K, as shown in Table 1 (G-0~G-4). Similar results were obtained; for example, the swelling index soared when the amount of NaCMC increased (Fig. 2). However, the swelling size obtained from F1–4 formulation was larger than those of PEO formulations. This reinforced the notion that incorporation of swellable ionic polymers of an appropriate viscosity, such as NaCMC of 450 cps, synergistically promoted the swelling ability. Unlike incorporation of the HEC 250HHX matrix, sinking was observed with the PEO 8000K formulations regardless of the amount of NaCMC of 450 cps added, as demonstrated by the results listed in Table 1.


Swelling/floating capability and drug release characterizations of gastroretentive drug delivery system based on a combination of hydroxyethyl cellulose and sodium carboxymethyl cellulose.

Chen YC, Ho HO, Liu DZ, Siow WS, Sheu MT - PLoS ONE (2015)

Swelling indexes of the combination of PEO 8000K and NaCMC with different ratios in deionized water.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4305323&req=5

pone.0116914.g002: Swelling indexes of the combination of PEO 8000K and NaCMC with different ratios in deionized water.
Mentions: To confirm that the swelling ability was related to the repulsive effect of negative charges of carboxylate groups carried by NaCMC, up to 40% of NaCMC of 450 cps was incorporated with another neutral hydrophilic polymer of PEO 8000K, as shown in Table 1 (G-0~G-4). Similar results were obtained; for example, the swelling index soared when the amount of NaCMC increased (Fig. 2). However, the swelling size obtained from F1–4 formulation was larger than those of PEO formulations. This reinforced the notion that incorporation of swellable ionic polymers of an appropriate viscosity, such as NaCMC of 450 cps, synergistically promoted the swelling ability. Unlike incorporation of the HEC 250HHX matrix, sinking was observed with the PEO 8000K formulations regardless of the amount of NaCMC of 450 cps added, as demonstrated by the results listed in Table 1.

Bottom Line: Of note, floating duration was enhanced when in simulated gastric solution compared to DIW.Further, the hydration of tablets was found to be retarded as the NaCl concentration in the medium increased resulting in smaller gel layers and swelling sizes.The release mechanism of the freely water-soluble drug, metformin, was mainly diffusion-controlled, while those of the water-soluble drug, ciprofloxacin, and the slightly water-soluble drug, esomeprazole, were mainly anomalous diffusion.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei, Taiwan.

ABSTRACT
The aim of this study was to characterize the swelling and floating behaviors of gastroretentive drug delivery system (GRDDS) composed of hydroxyethyl cellulose (HEC) and sodium carboxymethyl cellulose (NaCMC) and to optimize HEC/NaCMC GRDDS to incorporate three model drugs with different solubilities (metformin, ciprofloxacin, and esomeprazole). Various ratios of NaCMC to HEC were formulated, and their swelling and floating behaviors were characterized. Influences of media containing various NaCl concentrations on the swelling and floating behaviors and drug solubility were also characterized. Finally, release profiles of the three model drugs from GRDDS formulation (F1-4) and formulation (F1-1) were examined. Results demonstrated when the GRDDS tablets were tested in simulated gastric solution, the degree of swelling at 6 h was decreased for each formulation that contained NaCMC in comparison to those in de-ionized water (DIW). Of note, floating duration was enhanced when in simulated gastric solution compared to DIW. Further, the hydration of tablets was found to be retarded as the NaCl concentration in the medium increased resulting in smaller gel layers and swelling sizes. Dissolution profiles of the three model drugs in media containing various concentrations of NaCl showed that the addition of NaCl to the media affected the solubility of the drugs, and also their gelling behaviors, resulting in different mechanisms for controlling a drug's release. The release mechanism of the freely water-soluble drug, metformin, was mainly diffusion-controlled, while those of the water-soluble drug, ciprofloxacin, and the slightly water-soluble drug, esomeprazole, were mainly anomalous diffusion. Overall results showed that the developed GRDDS composed of HEC 250HHX and NaCMC of 450 cps possessed proper swelling extents and desired floating periods with sustained-release characteristics.

Show MeSH
Related in: MedlinePlus