Abstract
The aim of our work is to prepare mucoadhesive particles with biopolymers and 5-Aminosalicylic acid (5ASA) using the ionotropic gelation technique to ensure a controlled drug release at the colon level with potential applications in the treatment of intestinal bowel disease (IBD). The preparation of particles through the crosslinking of Chitosan (CS) with sodium tripolyphosphate (TPP) using different mass ratios and the influence of the k-Carrageenan (kCG) layer were studied. UV–VIS spectrometry was employed to assess encapsulation efficiency and drug release profile of 5ASA. The particles were investigated using FT-IR spectrometry for chemical characterization and the DLS results highlighted a monodisperse particle size distribution. The morphology of the polymeric beads was investigated using micro-computer tomography (µCT) and Scanning Electron Microscopy (SEM). Particles based on Chitosan and k-Carrageenan were able to incorporate and preserve 5ASA in an acidic and alkaline medium. The 5ASA loaded polymeric particles obtained after immersion for 1 h in kCG solution exhibited the lowest release rate in pH = 1.2. Biocompatibility studies performed on all of the particles displayed a good viability for the CCD 841 CoN cells and low cytotoxicity. All of the results have shown that these new biomaterials could be a versatile platform of targeted carriers with potential applications in inflammatory bowel disease treatment.
Highlights
Inflammatory bowel disease (IBD) is a chronic and nonspecific inflammatory disorder mainly affecting the large and small bowel
The two major types of IBD are Crohn’s disease (CD) and ulcerative colitis (UC). 5-Aminosalicylic acid (5ASA), alongside with methotrexate, corticosteroids, and sulfasalazine, is one of the current drugs used in a conventional treatment plan for IBD as a result of its anti-inflammatory and antioxidant effects on the swelled intestine [1,2,3]
Even though it is commonly used in IBD treatment, high doses of 5ASA are necessary, which leads in time to side effects because it is rapidly and extensively absorbed by the mucosa of the upper gastrointestinal tract, which hinder the therapeutic action in the proximal colon
Summary
Inflammatory bowel disease (IBD) is a chronic and nonspecific inflammatory disorder mainly affecting the large and small bowel. 5-Aminosalicylic acid (5ASA), alongside with methotrexate, corticosteroids, and sulfasalazine, is one of the current drugs used in a conventional treatment plan for IBD as a result of its anti-inflammatory and antioxidant effects on the swelled intestine [1,2,3]. For a drug delivery system that is able to target the colon, the pharmaceutical compound has to cross the abdominal region and the small intestine to the required destination in a manner that keeps it more or less intact [8,9] Biopolymers, such as polysaccharides, have been used as possible encapsulation materials due to their biocompatibility, non-toxicity, mucoadhesive properties, plentifulness in nature, and low price. Natural hydrophilic ionic biopolymers such as alginate, pectin, chitosan, and k-carrageenan are widely used in pharmaceuticals, in the food industry, and in medicine because of their biocompatibility and biodegradability properties [10,11,12]
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