Physiology of the colorectal barrier
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Cited by (39)
Recent advances in colon drug delivery systems
2020, Journal of Controlled ReleaseCitation Excerpt :Mucus is secreted by specialised epithelial cells called goblet cells that line the colon's lamina propia connective layer, to form a single mucus layer. The mucus is composed of mucin glycoprotein that give it its structure and adhesiveness, as well as water, inorganic salts and lipid [33–35]. Colon pH values are different from those of the upper gastrointestinal tract, and they also vary among the different sections of the large intestine.
Development and evaluation of budesonide-based modified-release liquid oral dosage forms
2019, Journal of Drug Delivery Science and TechnologyCoated pellets for oral colon delivery
2015, Journal of Drug Delivery Science and TechnologyCitation Excerpt :Such polymers generally bear glycoside or azo bonds that are susceptible to cleavage by the resident microbiota. The pH of the fluids in the caecum and ascending colon is known to be slightly acidic because of bacterial fermentation activities that cause local accumulation of short-chain fatty acids [22,23]. Moving down to the transverse and descending branches of the colon, a neutral to weakly basic environment is re-established due to the progressive absorption of fermentation products.
Oral drug delivery systems using chemical conjugates or physical complexes
2013, Advanced Drug Delivery ReviewsCitation Excerpt :Among those, mucus layer, polarity and membrane fluidity of different regions were found to contribute to the discrepancies in intestinal drug permeability, as evidenced by the fact that the regional membrane fluidity characteristically decreased from the upper to the lower parts of the gut [102,103]. The microflora and enzymatic activity have a high influence on the stability of a drug in the caecum and ascending colon, where residual tryptic and chymotryptic activities are more challenging than in the distal regions [104]. Another contributing factor is the pH value, which would possibly lie in the optimum range to degrade peptide/protein, in particular, and also to provide additional harshness in the gut [105].
Film coatings for oral colon delivery
2013, International Journal of PharmaceuticsOral colon delivery of insulin with the aid of functional adjuvants
2012, Advanced Drug Delivery ReviewsCitation Excerpt :As previously mentioned, the concentration of such enzymes is indeed subject to a marked and progressive decrease throughout the intestine [4,77,78]. In the caecum and ascending colon, where residual tryptic and chymotryptic activities could be more challenging than in distal regions, the weakly acidic pH values, which would possibly lie outside the optimum range typical of pancreatic endopeptidases, may provide additional protection against extensive insulin proteolysis [8,122]. Furthermore, brush-border membrane-associated enzymes, well-known to be reduced in the colon, were specifically demonstrated to exert a minor impact on insulin integrity [76,77,156].
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