Validation of a Pharmacokinetic Model of Colon-specific Drug Delivery and the Therapeutic Effects of Chitosan Capsules Containing 5-Aminosalicylic Acid on 2,4,6-Trinitrobenzenesulphonic Acid-induced Colitis in Rats

Tozaki, Hideyuki; Fujita, Takuya; Odoriba, Tomokazu; Terabe, Akira; Okabe, Susumu; Muranishi, Shozo; Yamamoto, Akira

doi:10.1211/0022357991776796

Cited by 39 publications

(20 citation statements)

References 11 publications

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“…Determination of pharmacokinetic parameters: Animal studies procedure [34,35]. Eighteen young, male albino rats divided into three groups (body weight 150-180 g) were obtained from the central animal house, and the experimental protocol for the animal studies was approved by the institutional animal ethical committee.…”

Section: Stability Studiesmentioning

confidence: 99%

Formulation and evaluation of chitosan microspheres of aceclofenac for colon‐targeted drug delivery

Umadevi

Thiruganesh

Suresh

et al. 2010

Biopharm & Drug Disp

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The objective of this investigation was to develop novel colon specific drug delivery. Aceclofenac, a NSAID, was successfully encapsulated into chitosan microspheres. Various formulations were prepared by varying the ratio of chitosan, span-85 and stirring speed and the amount of glutaraldehyde. The SEM study showed that microspheres have smooth surfaces. Microspheres were characterised by Fourier transform infrared (FTIR) spectroscopy and differential scanning calorimetry (DSC) to confirm the absence of chemical interactions between drug and polymer and to know the formation of microspheres structure. The microspheres were evaluated for particle size, encapsulation efficiency, drug loading capacity, mucoadhesion studies, stability studies, in vitro and in vivo drug release studies. Particle sizes, as measured by the laser light scattering technique, were of an average size in the range 41-80 µm. The swelling index was in the range 0.37-0.82 and the entrapment efficiency range was 51-75% for all the formulations. The optimised batch ACM(13) released 83.6% at 8 h and 104% at 24 h in SCF containing rat caecal content. Eudragit coated chitosan microspheres prevented the release of the aceclofenac in the physiological environment of the stomach and small intestine and released 95.9±0.34% in the colon. With regard to release kinetics, the data were best fitted with the Higuchi model and showed zero order release with non-Fickian diffusion mechanism. The in vivo findings suggest that aceclofenac microspheres exhibit a prolonged effect of aceclofenac in rats and produce a significant anti-inflammatory effect. The findings of the present study conclusively state that chitosan microspheres are promising for colon targeting of aceclofenac to synchronise with chronobiological symptoms of rheumatoid arthritis.

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Section: Stability Studiesmentioning

confidence: 99%

Formulation and evaluation of chitosan microspheres of aceclofenac for colon‐targeted drug delivery

Umadevi

Thiruganesh

Suresh

et al. 2010

Biopharm & Drug Disp

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“…In a study by Tozaki et al (1999a), 5-amino salicylic acid (5-ASA) containing chitosan capsules were also observed to be more effective than other 5-ASA formulations for the treatment of 2,4,6-trinitrobenzene sulfonic acid sodium salt induced colitis in rats. Similar results were obtained with the colon specific delivery of R68070, a new thromboxane inhibitor (Tozaki et al 1999b).…”

Section: Colon Targetingmentioning

confidence: 99%

Chitosan: some pharmaceutical and biological aspects - an update

Singla

Chawla

2001

Journal of Pharmacy and Pharmacology

705

363

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Chitosan, a natural polysaccharide, is being widely used as a pharmaceutical excipient. It is obtained by the partial deacetylation of chitin, the second most abundant natural polymer.Chitosan comprises a series of polymers varying in their degree of deacetylation, molecular weight, viscosity, pKa etc. The presence of a number of amino groups permit chitosan to chemically react with anionic systems, thereby resulting in alteration of physicochemical characteristics of such combinations.Chitosan has found wide applicability in conventional pharmaceutical devices as a potential formulation excipient, some of which include binding, disintegrating and tablet coating properties. The polymer has also been investigated as a potential adjuvant for swellable controlled drug delivery systems. Use of chitosan in novel drug delivery as mucoadhesive, gene and peptide drug administration via the oral route as well as its absorption enhancing effects have been explored by a number of researchers.Chitosan exhibits myriad biological actions, namely hypocholesterolemic, antimicrobial and wound healing properties. Low toxicity coupled with wide applicability makes it a promising candidate not only for the purpose of drug delivery for a host of drug moieties (antiinflammatories, peptides etc.) but also as a biologically active agent.It is the endeavour of the present review to provide an insight into the biological and pharmaceutical profile of chitosan. Various investigations carried out recently are reported, although references to research performed on chitosan prior to the recent reviews have also been included, where appropriate.

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“…This technique is more useful for evaluating efficacy of drugs as well as site-specific dosage forms in animal models of inflammation (21,22).…”

Section: Introductionmentioning

confidence: 99%

I n Vivo Evaluation of 5-ASA Colon-Specific Tablets Using Experimental-Induced Colitis Rat Animal Model

et al. 2015

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Abstract. Colonic drug delivery is intended not only for local treatment in inflammatory bowel disease (IBD) but also for systemic delivery of therapeutics. Intestinal myeloperoxidase (MPO) determination could be used to estimate the average level of inflammation in colon as well as to determine the efficacy of drugs to be used in the treatment of inflammatory bowel diseases or study the specificity of dosage forms to be used for colonic targeting of anti-inflammatory drugs. Colonic prodrug sulfasalazine (SASP) gets metabolized to give 5-aminosalicylic acid (5-ASA), which is the active portion of SASP. However, when given orally, 5-ASA is absorbed in upper part of gastrointestinal tract (GIT) and not made available in colon. In the present study, colon-targeted delivery of 5-ASA was achieved by formulating tablets with two natural polymers namely guar gum and pectin using compression coating method. Colonic specificity of 5-ASA tablets (prepared using guar gum and pectin as polymers) was evaluated in vitro using simulated fluids mimicking in vivo environment as well as in vivo method using chemically (2,4,6-trinitrobenzenesulfonic acid and acetic acid)-induced colitis rat model. Both colon-specific formulations of 5-ASA (guar gum and pectin) were observed to be more effective in reducing inflammation in chemically induced colitis rat models when compared to colon-specific prodrug sulfasalazine as well as conventional 5-ASA administered orally.

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Validation of a Pharmacokinetic Model of Colon-specific Drug Delivery and the Therapeutic Effects of Chitosan Capsules Containing 5-Aminosalicylic Acid on 2,4,6-Trinitrobenzenesulphonic Acid-induced Colitis in Rats

Cited by 39 publications

References 11 publications

Formulation and evaluation of chitosan microspheres of aceclofenac for colon‐targeted drug delivery

Formulation and evaluation of chitosan microspheres of aceclofenac for colon‐targeted drug delivery

Chitosan: some pharmaceutical and biological aspects - an update

I n Vivo Evaluation of 5-ASA Colon-Specific Tablets Using Experimental-Induced Colitis Rat Animal Model

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