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 CaCl2 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.Results: 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.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.
Highlights
Various drug delivery approaches have been explored for successful delivery of drugs to the target site
Colon targeting is naturally of value for the topical treatment of diseases of the colon such as Chron’s diseases, ulcerative colitis, colorectal cancer, and amoebiasis [3]. 5-Aminosalicylic acid (5-ASA), a typical anti-inflammatory agent is the drug of choice for the treatment of ulcerative colitis
To retard the drug release up to 24 h the optimized formulation was coated with Eudragit S-100 in three different concentrations (4 % w/v, 8% w/v, 15% w/v) and the drug release studies were performed
Summary
Various drug delivery approaches have been explored for successful delivery of drugs to the target site. It is necessary to develop a colon-specific delivery system for 5-ASA in the treatment of ulcerative colitis [4]. Considerable attention has been focused on hydrophilic polymers in the design of oral controlled drug delivery systems because of their flexibility to obtain a desirable drug release profile, cost-effectiveness, and broad regulatory acceptance [7]. These polymeric systems have been the potential candidates to deliver bioactive molecules, in controlled release applications [8, 9]. It is dispersible in either hot or cold water, forming a sol having a pH range 5.4–7.0 [10]
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