4.8 Article

Emerging technologies to increase gastrointestinal transit times of drug delivery systems

Journal

JOURNAL OF CONTROLLED RELEASE
Volume 346, Issue -, Pages 289-299

Publisher

ELSEVIER
DOI: 10.1016/j.jconrel.2022.04.016

Keywords

Oral drug delivery; Gastrointestinal transit times; Mucus permeation; Mucoinert; Charge conversion; Thiolated nanocarriers; Thiolated cyclodextrins

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In addition to established technologies, such as devices and formulations, there are new emerging technologies that have the potential to significantly impact gastrointestinal transit times. These include nanocarriers that can penetrate deeply into the mucus gel layer and remain there for a prolonged period, nanocarriers that can form strong ionic bonds with mucus glycoproteins, and nanocarriers that can form covalent bonds with cysteine-rich sub domains of mucus glycoproteins. This review provides an overview of these technologies and critically discusses their potential and shortcomings.
Apart from already established technologies to increase gastrointestinal transit times, including devices rapidly increasing in size once they have reached the stomach in order to retard the passage through the pylorus, formulations that float on gastric fluids and mucoadhesive drug delivery systems adhering to the gastrointestinal mucosa, there are new technologies emerging that might be game changing. They include mucus permeating nanocarriers that are able to diffuse deeply into the mucus gel layer of the gastric and intestinal mucosa remaining there for a prolonged time period (i), charge-converting nanocarriers that shift their zeta potential from negative to positive within the mucus gel layer providing strong ionic bonds with anionic mucus glycoproteins (ii) and thiolated nanocarriers and cyclodextrins form even covalent bonds with cysteine-rich sub domains of mucus glycoproteins (iii). Within this review we will provide an overview about these emerging new technologies and will critically discuss their potential and shortcomings.

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