Colon delivery of anti-inflammatory drugs accelerates healing of TNBS induced-colitis in rats.

The in vivo fate of nanoparticles and nanoparticle-loaded microcapsules after oral administration in mice: Evaluation of their potential for colon-specific delivery

“…Overall, the encapsulation of NPs in MCs resulted in a higher colonic NP intensity 42 from 8 h to 24 h post-administration compared to the free NPs, due to a NP 'guarding' effect of MCs dur- 43 ing their transit along mouse gastrointestinal tract which decreased NP excretion in faeces. These imag- 44 ing data revealed that this widely-utilised colon-targeting MC formulation lacked site-precision for 45 releasing its NP load in the colon, but the increased residence time of the NPs in the lower gastrointestinal 46 tract suggests that it is still useful for localised release of chemotherapeutics, compared to NP adminis- 47 tration alone. In addition, both formulations resided in the stomach of mice at considerable concentra- 48 tions over 24 h. Thus, adhesion of NP-or MC-based oral delivery systems to gastric mucosa may be 49 problematic for colon-specific delivery of the cargo to the colon and should be carefully investigated 50 for a full evaluation of particulate delivery systems.…”

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

“…Simulation curves were calculated by use of the pharmacokinetic model to be reported elsewhere. Experimental data are cited fromTozaki et al (1998a). Results are expressed as means AE s.e.m.…”

Colon-specific Delivery of Budesonide with Azopolymer-coated Pellets: Therapeutic Effects of Budesonide with a Novel Dosage Form against 2,4,6-Trinitrobenzenesulphonic Acid-induced Colitis in Rats

“…MPO activity, CaB ratio and damage score increased for 10 days after intracolonic administration of TNBS, and recovered to the control levels after 14 days. Maximal MPO activity, CaB ratio and damage score were observed on day 5 after intracolonic administration of TNBS (Tozaki et al 1998(Tozaki et al , 1999. We therefore evaluated the therapeutic effects of budesonide for treatment of colitis on day 5 after intracolonic administration of TNBS in the following experiments.…”

“…The azopolymer-coated pellets containing budesonide ( $ 3Á3 mg budesonideacapsule) were prepared by Ono Pharmaceutical Co. Ltd, (Osaka, Japan). The mean diameter and weight of the pellet were 1Á0± 1Á2 mm and 1Á0 mg, respectively (Tozaki et al 1998). The surface of the capsule was coated with Eudragit L-100 (10Á7% waw) as an enteric coating material and further coated with a straight-chain azopolymer (9Á09% waw) developed by Kimura et al (1992).…”