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      Going Natural: Using polymers from nature for gastroresistant applications

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          Abstract

          Nutraceuticals provide an additional health or medicinal benefit besides their nutritional value and are therefore marketed for the prevention and treatment of certain conditions. Nutraceuticals contain natural ingredients, usually presented in the form of functional foods or as dietary supplements. Many of the ingredients are susceptible to degradation by gastric acid or can provoke nauseatic feelings or induce vomiting on oral administration. Gastroresistant coatings, widely researched and used in pharmaceuticals, employ enteric polymers which are not regarded as natural ingredients or do not possess GRAS (generally regarded as safe) status by the regulatory bodies, thus cannot be used for nutraceutical products. Consequently, most nutraceuticals are not formulated as gastroresistant and can therefore lack efficacy or are well tolerated. This manuscript provides a critical review of natural substances employed in producing gastroresistant products, their shortcomings, and potential industrial applications. It also identifies current gaps in our knowledge to encourage further research in this area.

          Most cited references101

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          Transit of pharmaceutical dosage forms through the small intestine.

          The gastrointestinal transit of pharmaceutical dosage forms has been measured in 201 studies in normal subjects using gamma scintigraphy. Solutions, small pellets, and single units (matrix tablets and osmotic pumps) were administered with different amounts of food in the stomach, ranging from fasted state to heavy breakfast. Gastric emptying was affected by the nature of the dosage form and the presence of food in the stomach. Solutions and pellets were emptied even when the stomach was in the digestive mode, while single units were retained for long periods of time, depending on the size of the meal. In contrast, measured intestinal transit times were independent of the dosage form and fed state. The small intestinal transit time of about three hours (mean +/- 1 h SEM) has implications for the design of dosage forms for the sustained release of drugs in specific positions in the gastrointestinal tract.
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            Casein-based formulations as promising controlled release drug delivery systems.

            Casein, the major milk protein, forms an integral part of the daily diet in many parts of the world. Casein possesses a number of interesting properties that make it a good candidate for conventional and novel drug delivery systems. This article reviews approaches aimed to associate bioactive molecules to casein and analyze the evidence of their efficacy in modifying the release and/or improving the bioavailability of the associated molecules. The ability of casein to modify drug dissolution from compacts was reported. The high tensile strength of casein films, favors its use as an acceptable film-coating for tablets. Naturally occurring genipin and a natural tissue enzyme, transglutaminase, were used as crosslinkers to prepare novel casein-based hydrogels for the controlled release of bioactives. Casein floating beads were developed to increase the residence time of drugs in the stomach based on its emulsifying and bubble-forming properties. Casein-based microparticles entrapping bioactive molecules were prepared via emulsification-chemical crosslinking with glutaraldehyde, enzymatic crosslinking by transglutaminase, simple coacervation and electrostatic complexation. Casein nano-formulations were also prepared to deliver nutraceuticals and synthetic drugs via enzymatic crosslinking, graft copolymerization, heat-gelation and polyelectrolyte ionic complexation. It can be concluded that casein-based formulations are promising materials for controlled drug delivery. Copyright © 2011 Elsevier B.V. All rights reserved.
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              Casein micelle as a natural nano-capsular vehicle for nutraceuticals

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                Author and article information

                Journal
                BJPharm
                British Journal of Pharmacy
                University of Huddersfield Press
                2058-8356
                10 July 2017
                : 2
                : 1
                : 14-30
                Affiliations
                Department of Pharmacy, School of Applied Sciences, University of Huddersfield, Queensgate, Huddersfield HD1 3DH, United Kingdom
                Author notes
                *Corresponding author. Tel.: +44 (0) 1484 472387 Fax: +44 (0) 1484 472182 E-mail: hamid.merchant@ 123456hud.ac.uk
                Article
                10.5920/bjpharm.2017.01
                bbd0b305-c59b-4c8b-8786-29bc25428447
                © 2017, Joao A.C. Barbosa, Barbara R. Conway, Hamid A. Merchant

                This is an open access article distributed under the terms of the Creative Commons Attribution License (CC BY) 4.0 https://creativecommons.org/licenses/by/4.0/.

                History
                : 17 November 2016
                : 13 February 2017
                : 05 May 2017
                Categories
                Critical Review

                Medicine,Pharmacology & Pharmaceutical medicine,Health & Social care
                Enteric coatings,delayed-release,modified release,nutritional supplements,nutraceuticals

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