Chitosan capsules for colon-specific drug delivery: Improvement of insulin absorption from the rat colon.

Tozaki, Hideyuki; Yamamoto, A.; Muranishi, Shozo

doi:10.2745/dds.12.311

Cited by 51 publications

(58 citation statements)

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“…There are a number of reports that chitosan can be used as an absorption enhancer of drugs. [39][40][41][42] Sugimoto et al 43) reported that ampicillin absorption by poly(vinyl alcohol)-gel spheres was enhanced by the chitosan combination, and that poly(vinyl alcohol)-gel spheres prepared with chitosan prolonged the small intestinal transit time more than poly(vinyl alcohol)-gel spheres. Singh and Udupa 44) reported that the antitumor activity in Ehrlich ascites tumor-bearing mice given methotrexate-loaded chitosan microspheres was better when compared with plain methotrexate on oral administration, and the plasma methotrexate levels were more sustained.…”

Section: Discussionmentioning

confidence: 99%

Prevention by Chitosan of Myelotoxicity, Gastrointestinal Toxicity and Immunocompetent Organic Toxicity Induced by 5‐Fluorouracil without Loss of Antitumor Activity in Mice

Kimura

Okuda

1999

Japanese Journal of Cancer Research

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Section: Discussionmentioning

confidence: 99%

Prevention by Chitosan of Myelotoxicity, Gastrointestinal Toxicity and Immunocompetent Organic Toxicity Induced by 5‐Fluorouracil without Loss of Antitumor Activity in Mice

Kimura

Okuda

1999

Japanese Journal of Cancer Research

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“…In addition, chitosan has been widely applied as a potential formulation excipient in conventional pharmaceutical devices. This polymer also has been investigated as a potential adjuvant for orally controlled release systems [30] and colon targeting [4][5][6][7] . In addition, it was reported that chitosan had mucoadhesive properties, which probably was mediated through ionic interactions with negative charges in mucus or on cell surfaces.…”

Section: Discussionmentioning

confidence: 99%

“…Therefore, we hope to find some absorption enhancers to augment permeability of rebamipide across the colonic tissues, and in this case, this drug should be specifically localized in the large intestine by its colon-specific delivery to improve its therapeutic effect on colitis and to decrease its side-effects, as well. There are many investigations on absorption enhancers; meanwhile, it has been demonstrated previously that chitosan capsule could act as useful carriers for colon-specific delivery of peptide and anti-inflammatory drugs including insulin, calcitonin, 5-aminosalicylic acid and ridog rel [6][7][8][9] . However, the effects of absorption enhancers increasing the distribution on colon and chitosan capsule on the colonspecific delivery of rebamipide ought to be established.…”

Section: Introductionmentioning

confidence: 99%

Permeabilities of rebamipide via rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier

Huang¹,

Li²,

Luo³

et al. 2008

WJG

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AIM:To investigate the permeability characteristics of rebamipide across intestinal mucosa, and examine the effects of some absorption enhancers on the permeability across the colonic tissue. Another purpose is to demonstrate the colon-specific delivery of rebamipide with or without absorption enhancers using chitosan capsule as a carrier. METHODS: The permeability of rebamipide was evaluated using an in vitro diffusion chamber system, and the effects of some absorption enhancers on the permeability via colon were further investigated. The release of rebamipide from chitosan or gelatin capsule was studied by Japan Pharmacopoeia rotating basket method. The colonic and plasma concentrations were analyzed by high performance liquid chromatography (HPLC) to evaluate colon-targeting action after oral administration of various dosage forms, and rebamipide with absorption enhancers in chitosan dosage forms. RESULTS: The permeability of rebamipide across the jejunal or ileal membranes was higher than the colonic membranes. Both sodium laurate (C12) and labrasol significantly increased permeability across the colon membranes. On the other hand, the release of rebamipide from chitosan capsule was less than 10% totally within 6 h. The area under concentration-time profile of drug in the colon mucosa using chitosan capsules (AUCLI, 1 6011.2 ng · h/g) was 2.5 times and 4.4 times greater than using gelatin capsules and CMC suspension, respectively. Meanwhile, the area under concentration-time profile of drug in the plasma (AUCPL) was 1016.0 ng · h/mL for chitosan capsule, 1887.9 ng · h/mL for CMC suspension p and 2163.5 ng·h/mL for gelatin capsule. Overall, both AUCLI and AUCPL were increased when C12 was coadministrated, but the increase of AUCLI was much greater; the drug delivery index (DDI) was more than 1 compared with simple chitosan capsule group. CONCLUSION: There was a regional difference in the permeability of Rebamipide across the jejunum, ileum and the colon, and passive diffusion seems to be one of the major transport mechanisms of rebamipide. Absorption enhancers can increase the permeability of rebamipide across the colon tissue significantly. In addition, chitosan capsule may be a useful carrier to deliver rebamipide to the colon specifically and the coadministration of C12 with rebamipide may also be very useful in local treatment.© 2008 The WJG Press. All rights reserved.Key words: Rebamipide; Diffusion chamber; Permeability; Sodium laurate; Chitosan capsule; Colon-specific delivery Peer reviewer: Atsushi Nakajima, Professor, Yokohama City University Hospital, 3-9 Fukuura Kanazawaku, Yokohama 236, Japan Huang BB, Li GF, Luo JH, Duan L, Nobuaki K, Akira Y. Permeabilities of rebamipide via the rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier.

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“…78%) and batches A5, A1 and A2 released 77.35, 69.55 and 78.12% of insulin respectively at 8 h. There was insignificant difference (p>0.05) in the release profiles of the various batches of the microspheres. The drug concentration and the polymeric carrier are some of the main factors affecting drug release (Tozaki et al, 1997). Expectedly, this manner of release is related to the pH responsiveness of Eudragit RL100 (Pignatello et al, 2000;Philip et al, 2010).…”

Section: Release Studymentioning

confidence: 99%

Microspheres of insulin-Eudragit complex: Formulation, characterization and in vivo studies

Momoh¹,

Jackson²,

Musiliu³

et al. 2017

Afr. J. Pharm. Pharmacol.

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Insulin, a hormonal drug for the management of diabetes mellitus has continued to attract attention of many researchers and pharmaceutical formulators for more than a decade. However, its low oral bioavailability due to the activities of intestinal enzymes restricts its route of administration to only the parenteral route. This study was designed to evaluate the capacity of mucoadhesive microspheres formulated with varying blends of Eudragit ® RL 100 and Eudragit ® RS 100 to protect insulin for oral administration. Microspheres containing varying blends of Eudragit ® RL 100/RS100 loaded insulin was prepared by solvent evaporation method and were characterized in vitro and in vivo. Results showed that stable formulation with high encapsulation efficiency, positive zeta potential and high bioadhesion were obtained in all the formulations. In vitro release showed a maximum release of 9 and 87% release in pH 1.2 and 7.2, respectively. Single oral studies showed a decreased in blood glucose level comparably equal to that of subcutaneous (sc) administration. The results of this study indicate that insulin-loaded Eudragit RL100/RS100 microspheres could be a promising drug delivery system to improve oral absorption of insulin.

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Chitosan capsules for colon-specific drug delivery: Improvement of insulin absorption from the rat colon.

Cited by 51 publications

References 0 publications

Prevention by Chitosan of Myelotoxicity, Gastrointestinal Toxicity and Immunocompetent Organic Toxicity Induced by 5‐Fluorouracil without Loss of Antitumor Activity in Mice

Prevention by Chitosan of Myelotoxicity, Gastrointestinal Toxicity and Immunocompetent Organic Toxicity Induced by 5‐Fluorouracil without Loss of Antitumor Activity in Mice

Permeabilities of rebamipide via rat intestinal membranes and its colon specific delivery using chitosan capsule as a carrier

Microspheres of insulin-Eudragit complex: Formulation, characterization and in vivo studies

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