Starch hydrogels as targeted colonic drug delivery vehicles

Koev, Todor; Harris, Hannah; Kiamehr, Sara; Khimyak, Yaroslav Z.; Warren, Frederick J.

doi:10.1016/j.carbpol.2022.119413

Cited by 27 publications

(11 citation statements)

References 55 publications

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“…The development of a colon-specific oral formulation is challenging as it must pass through the upper alimentary canal intact, avoiding any potential metabolism or drug release in the gastrointestinal tract (GIT) prior to releasing the drug in the proximal colon. Various colonic delivery systems have been developed to overcome these challenges, including the use of time-dependent formulation, pH-sensitive and bacterial degrading coating materials, hydrogels, biodegradable polymers, and prodrugs [ 10 , 11 , 12 , 13 , 14 ]. Each of these approaches comes with its own particular advantages and limitations [ 2 ].…”

Section: Introductionmentioning

confidence: 99%

Design, Development, and Optimisation of Smart Linker Chemistry for Targeted Colonic Delivery—In Vitro Evaluation

Abd-Ellah

Mudududdla²,

Carter

et al. 2023

Pharmaceutics

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Drug targeting is necessary to deliver drugs to a specific site of action at a rate dictated by therapeutic requirements. The pharmacological action of a drug can thereby be optimised while minimising adverse effects. Numerous colonic drug delivery systems have been developed to avoid such undesirable side effects; however, these systems lack site specificity, leaving room for further improvement. The objective of the present study was to explore the potential of amino-alkoxycarbonyloxymethyl (amino-AOCOM) ether prodrugs as a general approach for future colonic delivery. To circumvent inter- and intra-subject variabilities in enzyme activities, these prodrugs do not rely on enzymes but rather are activated via a pH-triggered intramolecular cyclisation–elimination reaction. As proof of concept, model compounds were synthesised and evaluated under various pH conditions, simulating various regions of the gastrointestinal tract (GIT). Probe 15 demonstrated excellent stability under simulated stomach- and duodenum-like conditions and protected 60% of the payload in a small intestine-like environment. Moreover, 15 displayed sustained release at colonic pH, delivering >90% of the payload over 38 h. Mesalamine (Msl) prodrugs 21 and 22 were also synthesised and showed better stability than probe 15 in the simulated upper GIT but relatively slower release at colonic pH (61–68% of Msl over 48 h). For both prodrugs, the extent of release was comparable to that of the commercial product Asacol. This study provides initial proof of concept regarding the use of a cyclisation-activated prodrug for colon delivery and suggests that release characteristics still vary on a case-by-case basis.

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Section: Introductionmentioning

confidence: 99%

Design, Development, and Optimisation of Smart Linker Chemistry for Targeted Colonic Delivery—In Vitro Evaluation

Abd-Ellah

Mudududdla²,

Carter

et al. 2023

Pharmaceutics

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“…The type of starch presented in tablets can influence the drug release, mostly regarding the crystallinity aspect, which has proportional resistance to enzymatic systems; another aspect observed was a faster disintegration and drug release for starch with a higher crosslinking degree [ 152 ]. A slowly digestible starch, which is also resistant, is ideal for oral colon-specific drug delivery, as it passes intact through the digestive system to disintegrate in the intestine [ 153 , 154 ].…”

Section: Plant-derived Polymersmentioning

confidence: 99%

Plant Polysaccharides in Engineered Pharmaceutical Gels

et al. 2022

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Hydrogels are a great ally in the pharmaceutical and biomedical areas. They have a three-dimensional polymeric structure that allows the swelling of aqueous fluids, acting as an absorbent, or encapsulating bioactive agents for controlled drug release. Interestingly, plants are a source of biogels, specifically polysaccharides, composed of sugar monomers. The crosslinking of these polymeric chains forms an architecture similar to the extracellular matrix, enhancing the biocompatibility of such materials. Moreover, the rich hydroxyl monomers promote a hydrophilic behavior for these plant-derived polysaccharide gels, enabling their biodegradability and antimicrobial effects. From an economic point of view, such biogels help the circular economy, as a green material can be obtained with a low cost of production. As regards the bio aspect, it is astonishingly attractive since the raw materials (polysaccharides from plants-cellulose, hemicelluloses, lignin, inulin, pectin, starch, guar, and cashew gums, etc.) might be produced sustainably. Such properties make viable the applications of these biogels in contact with the human body, especially incorporating drugs for controlled release. In this context, this review describes some sources of plant-derived polysaccharide gels, their biological function, main methods for extraction, remarkable applications, and properties in the health field.

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“…After being modified, NPs can be utilized as drug carriers, combining with other medications to regulate drug release in the colon, increase drug targeting and affinity, and provide targeted therapeutic effects. For example, starch hydrogels (10%, w/v) can be used as targeted colonic drug delivery vehicles in UC ( Koev et al, 2022 ).…”

Section: Modified Polysaccharide Used In the Treatment Of Ulcerative ...mentioning

confidence: 99%

The Function of Natural Polysaccharides in the Treatment of Ulcerative Colitis

Guo

Cao

et al. 2022

Front. Pharmacol.

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Ulcerative colitis (UC) is an inflammatory bowel disease that is persistent and nonspecific. There are several medications available for the treatment of UC. However, conventional UC medications have substantial adverse effects, low clinical effectiveness, and a high recurrence rate. Therefore, it is critical to discover new medicines that are both safe and effective for UC patients. Natural polysaccharides offer a wide range of pharmacological benefits, including anti-inflammatory, anti-virus, anti-tumor, anti-aging, immune enhancement, and gut flora regulation. In the therapy of UC, natural polysaccharides can modulate inflammatory factors, the immune system, and intestinal flora, and preserve the intestinal mucosa. It demonstrates a good curative effect and is of safety to use, thereby being a potential treatment for UC patients. This paper covers the structure, the pharmacological effects on UC, and the mechanisms of natural polysaccharides. Finally, limitations, challenges, and perspectives are discussed. It is hoped that the findings of this publication will inspire more natural polysaccharides research and provide a theoretical foundation for the creation of new UC medications.

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Starch hydrogels as targeted colonic drug delivery vehicles

Cited by 27 publications

References 55 publications

Design, Development, and Optimisation of Smart Linker Chemistry for Targeted Colonic Delivery—In Vitro Evaluation

Design, Development, and Optimisation of Smart Linker Chemistry for Targeted Colonic Delivery—In Vitro Evaluation

Plant Polysaccharides in Engineered Pharmaceutical Gels

The Function of Natural Polysaccharides in the Treatment of Ulcerative Colitis

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