A Novel Approach of Locust Bean Gum Microspheres for Colonic Delivery of Mesalamine

Abstract

Objective: The objective of the present study was to formulate site-specific drug delivery of mesalamine using Locust bean gum. Methods:The core microspheres were prepared by ionic gelation method using CaCl2Results: The SEM images revealed the surface morphology was rough and smooth for core and coated microspheres, respectively. The optimized batch (ILBG6) of core microspheres(for 7hr), coated microspheres and coated microspheres in presence of rat caecal contents (8%w/v) for 24hr exhibited 98.44±2.48, 73.58±3.49 % and 98.28±4.42 drug release, respectively. The drug release from all locust bean gum microsphere formulations followed higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the korsmeyer-peppas equation with an fickian kinetics mechanism. Finally, stability studies suggested the change in entrapment efficiency and in vitro drug release of microspheres was minimal, indicating good stability of the formulation.solution and cross-linked with glutaraldehyde and were further coated with pH-sensitive polymer eudragit S-100(1.5-4.5 ml) to retard the drug release in the upper gastrointestinal environment (Stomach and small intestine). Microspheres were characterized by ftir spectroscopy, differential scanning calorimetry and evaluated by scanning electron microscopy (SEM), particle size analysis, entrapment efficiency and in vitro drug release studies in different simulated gastric fluids. Stability studies were carried out for one month at 40±2 °C/75±5% RH. Conclusion:The microspheres formed using natural polysaccharide locust beangum by ionic gelation method are capable of colon targeting the anti-inflammatory drug, mesalamine for the treatment of ulcerative colitis.

In Vitro Methods to Study Colon Release: State of the Art and An Outlook on New Strategies for Better In-Vitro Biorelevant Release Media

“…Several groups have based their method on the work done by Prasad et al [ 127 ], who used a USP bath with 4% of rat caecum in phosphate buffer pH 6.8, and to keep the system semi-anaerobic, the solution was bubbled through with CO 2 . There are slight variations to this method, for example, by using different pHs, 6.5 [ 128 ]–7.5 [ 129 ], using nitrogen in some steps of the method instead of CO 2 [ 128 ], using variations in caecum content, 2%–10% [ 129 , 130 ], and varying the type of USP setup [ 128 ] or using sealed bottles [ 131 ]. In systems based on azo-structures, the intact or sonicated caecum (to release intracellular enzymes) have been mixed with co-factors such as benzyl viologen, NADP, glucose-6-phosphate dehydrogenase, and glucose-6-phosphate [ 122 , 132 , 133 ].…”

Formulation and in Vitro Evaluation of Ramelteon Tablets for Colon Drug Delivery System by Compression Coating

“…The prepared core tablets were subjected to compression coating by using various compositions of polymers such as Ethylcellulose, Eudragit L 100 and Eudragit S 100 as coating materials [8,9]. The composition of coating layer is given in below table 2.…”

Gastrointestinal Variables and Drug Absorption

“…Several groups have based their method on the work done by Prasad et al [127], who used a USP bath with 4% of rat caecum in phosphate buffer pH 6.8, and to keep the system semi-anaerobic, the solution was bubbled through with CO 2 . There are slight variations to this method, for example, by using different pHs, 6.5 [128]-7.5 [129], using nitrogen in some steps of the method instead of CO 2 [128], using variations in caecum content, 2%-10% [129,130], and varying the type of USP setup [128] or using sealed bottles [131]. In systems based on azo-structures, the intact or sonicated caecum (to release intracellular enzymes) have been mixed with co-factors such as benzyl viologen, NADP, glucose-6-phosphate dehydrogenase, and glucose-6-phosphate [122,132,133].…”