Statistical optimization of alginate-based oral dosage form of 5-aminosalicylic acid aimed to colonic delivery: in vitro and in vivo evaluation

Kaffash, Ehsan, Saremnejad, Farinaz, Abbaspour, Mohammadreza, Mohajeri, Seyed Ahmad, Garekani, Hadi Afrasiabi, Jafarian, Amir Hossein, Sardo, Hossein Shahdadi, Akhgari, Abbas and Nokhodchi, Ali (2019) Statistical optimization of alginate-based oral dosage form of 5-aminosalicylic acid aimed to colonic delivery: in vitro and in vivo evaluation. Journal of Drug Delivery Science and Technology. ISSN 1773-2247

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Abstract

Although different colon-targeting methods such as pH and time-dependent as well as bacterially degradable systems have been developed, due to variations in physiological conditions of patients, one system alone cannot produce a reliable drug delivery system. Therefore, in this study, an attempt was made to formulate 5-ASA pellets based on a combination of pH and time-dependent systems. A 32 full-factorial design was used to evaluate the effect of sodium alginate (SA) concentration and the polymer ratio (Eudragit® RS: Eudragit® S100) on morphology, mechanical features and release behaviour of 5-ASA pellet formulations. Fourier transform infrared spectroscopy, and differential scanning calorimetry analysis ruled out any interactions between the formulations components. The optimized formulation released 35, 55 and 89% of the drug within 15 h, at pHs 1.2, 6.8 and 7.4, respectively. In vivo studies demonstrated that the administration of sodium alginate-based matrix pellets containing 5-ASA coated with ES100 was effective in alleviating the damaged tissues and also decreased the inflammatory score and the rate of weight loss in colitis rats. The results indicated the remarkable anti-inflammatory efficacy of the designed colonic delivery system and the proposed formulations can be further developed in the pharmaceutical industry for patient use.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: R Medicine > RS Pharmacy and materia medica > RS0153 Materia medica
R Medicine > RS Pharmacy and materia medica > RS0153 Materia medica > RS0192 Pharmaceutical technology
R Medicine > RS Pharmacy and materia medica > RS0153 Materia medica > RS0200 Pharmaceutical dosage forms
Depositing User: Ali Nokhodchi
Date Deposited: 16 Apr 2019 08:36
Last Modified: 01 Jul 2019 16:16
URI: http://sro.sussex.ac.uk/id/eprint/83275

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