Abstract
Biologics have changed the management of inflammatory bowel disease (IBD), but there are concerns with unexpected systemic toxicity and loss of therapeutic response following administration by injection. Rectal administration of biologics offers potentially reduced therapy costs, as well as safer and more effective local delivery to inflammation sites. Hydrogels are potentially useful carriers of biologics for improved delivery to the inflamed intestinal mucosa. Here, we prepared a hydrogel system based on ascorbyl palmitate (AP) and incorporated a model macromolecular drug (fluorescently-labelled dextran) into the system. Characterization of gel properties included rheology, drug loading and release, cytotoxicity, and drug delivery in an in vitro intestinal model. We report that this hydrogel can be formed under a moderate environment that is amenable to incorporation of some biologics. The system showed a shear-thinning behavior. AP hydrogel released approximately 60% of the drug within 5 h and showed reasonable a cytotoxicity profile. The study therefore provides evidence that AP hydrogel has potential for local delivery of macromolecules to the intestinal mucosa in IBD.
Highlights
Crohn’s Disease (CD) and Ulcerative Colitis (UC) are two main forms of inflammatory bowel disease (IBD) affecting an estimated 2.5–3 million people in Europe [1] and with an increasing prevalence in newly industrialized countries
An ‘inflammation-targeting’ hydrogel based on ascorbyl palmitate (AP), an amphiphile that is generally recognized as safe (GRAS) by the United States (U.S.) Food and Drug Administration, was developed by Zhang et al [9]
We report here that the AP hydrogel can be formed under a moderate environment that is amenable to incorporation of some biologics, such as antibodies, in the system and displays behaviors suitable for rectal delivery of biologics
Summary
Crohn’s Disease (CD) and Ulcerative Colitis (UC) are two main forms of inflammatory bowel disease (IBD) affecting an estimated 2.5–3 million people in Europe [1] and with an increasing prevalence in newly industrialized countries. Rectal hydrogel-mediated sulfasalazine delivery was more therapeutic and induced a lower plasma concentration of a potentially toxic drug by-product In another recent study, a thermo-sensitive system based on a non-ionic surfactant copolymer consisting of hydrophilic polyethylene glycol and hydrophobic polypropylene glycol blocks was developed for rectal budesonide delivery. An ‘inflammation-targeting’ hydrogel based on ascorbyl palmitate (AP), an amphiphile that is generally recognized as safe (GRAS) by the United States (U.S.) Food and Drug Administration, was developed by Zhang et al [9] This system delivered the anti-inflammatory corticosteroid dexamethasone in a targeted manner to the site of inflammation owing to its negative charge interacting with the positively charged proteins accumulated selectively to the sites of inflammation in the colonic mucosa [10,11].
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