Development of Polymeric-Based Formulation as Potential Smart Colonic Drug Delivery System

Abstract

Conventional oral formulations are mainly absorbed in the small intestine. This limits their use in the treatment of some diseases associated with the colon, where the drug has to act topically at the inflammation site. This paved the way for the development of a smart colonic drug delivery system, thereby improving the therapeutic efficacy, reducing the dosing frequency and potential side effects, as well as improving patient acceptance, especially in cases where enemas or other topical preparations may not be effective alone in treating the inflammation. In healthy individuals, it takes an oral medication delivery system about 5 to 6 h to reach the colon. A colonic drug delivery system should delay or prohibit the medication release during these five to six hours while permitting its release afterward. The main aim of this study was to develop a smart drug delivery system based on pH-sensitive polymeric formulations, synthesized by a free-radical bulk polymerization method, using different monomer and crosslinker concentrations. The formulations were loaded with 5-amino salicylic acid as a model drug and Capmul MCM C8 as a bioavailability enhancer. The glass transition temperature (Tg), tensile strength, Young’s modulus, and tensile elongation at break were all measured as a part of the dried films’ characterization. In vitro swelling and release studies were performed to assess the behavior of the produced formulations. The in vitro swelling and release evaluation demonstrated the potential ability of the developed system to retard the drug release at conditions mimicking the stomach and small intestine while triggering its release at conditions mimicking the colon, which indicates its promising applicability as a potential smart colonic drug delivery system.

Smart Pellets for Controlled Delivery of 5-Fluorouracil

“…The equilibrium swelling ratios were attained within 72 h for all pellets. The results obtained are in agreement with the data published recently by Bayan et al [4] concerning the polymer used.…”

“…The size of the polymer also affects this behaviour, as it affects the surface area available for fluid penetration. The ability to control this behaviour encourages the use of polymers in many pharmaceutical drug delivery systems [1][2][3][4][5][6][7]. The pellets' swelling was examined in phosphate-buffered saline (PBS).…”

“…Enhanced electrostatic repulsions between the pendant groups are due to the presence of the ionizable anionic pendant group (MA) in these pellets. This ionization is triggered in the simulated intestinal fluid (PBS), where the pH is higher than the pKa of MA, thus contributing to the high swelling ratios of the pellets produced [4]. The equilibrium swelling ratios were attained within 72 h for all pellets.…”

“…Targeted drug delivery to the colon has attracted the attention of many researchers owing to its tremendous advantages over systemic drug administration, including increased drug potency and efficacy and reduced adverse drug reactions [1,2]. Colonic drug delivery systems have been used to treat a plethora of bowel diseases encompassing colorectal carcinoma, ulcerative colitis, diverticulitis, Crohn's disease, and irritable bowel syndrome [3][4][5]. Colon-specific drug delivery has long been used to enhance therapeutic effectiveness by reducing unwanted absorption in other regions of the gastrointestinal tract, guaranteeing that the whole drug dose is specifically delivered to the site of interest in the colon [6,7].…”

Facile Fabrication of Methyl Gallate Encapsulated Folate ZIF-L Nanoframeworks as a pH Responsive Drug Delivery System for Anti-Biofilm and Anticancer Therapy

“…The remarkable physicochemical properties allow for the construction of the biomolecules’ encapsulated drug delivery system. The superior stability in physiological conditions and their acidic decomposition make them highly attractive cargo in pH-responsive drug delivery applications [ 5 , 6 , 7 , 8 , 9 , 10 ]. Recently, encapsulation of plant-derived compounds within ZIFs is an innovative process in human pathogenic disease and cancer treatments.…”