A novel natural GRAS-grade enteric coating for pharmaceutical and nutraceutical products

Khoder, Mouhamad; Schropp, Verena; Zeitler, Susanne; Pereira, Beatriz C.; Habashy, Rober; Royall, Paul G.; Wang, Julie; Alhnan, Mohamed Albed

doi:10.1016/j.ijpharm.2020.119392

Cited by 17 publications

(13 citation statements)

References 31 publications

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“…At low pH it is insoluble, while at higher pH, it dissolves forming pores in the ethylcellulose coating which promote disintegration and drug release. An enteric coating based on an alginate and pectin blend has also been reported [102]. Oral thin films are used in lingual (for enteral), sublingual, and buccal drug delivery.…”

Section: Film Coatings and Oral Filmsmentioning

confidence: 99%

Applications of polymer blends in drug delivery

Nyamweya¹

2021

Futur J Pharm Sci

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Background Polymers are essential components of many drug delivery systems and biomedical products. Despite the utility of many currently available polymers, there exists a demand for materials with improved characteristics and functionality. Due to the extensive safety testing required for new excipient approval, the introduction and use of new polymers is considerably limited. The blending of currently approved polymers provides a valuable solution by which the limitations of individual polymers can be addressed. Main body Polymer blends combine two or more polymers resulting in improved, augmented, or customized properties and functionality which can result in significant advantages in drug delivery applications. This review discusses the rationale for the use of polymer blends and blend polymer-polymer interactions. It provides examples of their use in commercially marketed products and drug delivery systems. Examples of polymer blends in amorphous solid dispersions and biodegradable systems are also discussed. A classification scheme for polymer blends based on the level of material processing and interaction is presented. Conclusion The use of polymer blends represents a valuable and under-utilized resource in addressing a diverse range of drug delivery challenges. It is anticipated that new drug molecule development challenges such as bioavailability enhancement and the demand for enabling excipients will lead to increased applications of polymer blends in pharmaceutical products. Graphical abstract

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Section: Film Coatings and Oral Filmsmentioning

confidence: 99%

Applications of polymer blends in drug delivery

Nyamweya¹

2021

Futur J Pharm Sci

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“…Some of the pharmaceutical applications of pectin are to diminish lipid digestion [ 12 ]⁠, to improve lipid hepatic accumulation [ 13 ]⁠, glucose tolerance for antidiabetic effects [ 14 ]⁠, and its anti-inflammatory activity in high methoxyl pectins [ 15 ]⁠. Recently, the low hydrophilic of pectin has taken advantage to improve carrier properties and diffusion control of nicotine in transdermal patches [ 16 , 17 ]⁠ and drug delivery such as theophylline tablets [ 18 ]⁠ and lidocaine and aspirin in ionic liquid [ 19 ]⁠.…”

Section: Introductionmentioning

confidence: 99%

Optimization and Preliminary Physicochemical Characterization of Pectin Extraction from Watermelon Rind (Citrullus lanatus) with Citric Acid

Pérez

Gómez

Vega

2022

International Journal of Food Science

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Watermelon rind was used for the pectin extraction with citric acid as the extractant solvent. The effects of pH (2.0-3.0), extraction time (45-75 min), and liquid-solid ratio (10 : 1 to 40 : 1 mL/g) on the pectin yield, degree of esterification, methoxyl content, and anhydrouronic acid content were investigated using Box-Behnken surface response experimental design. The pH was the most significant variable for the pectin yield and properties. The responses optimized separately showed different optimal conditions for each one of the variables studied in this work. Therefore, the desirability function was used to determine the sole theoretical optimum for the highest pectin yield and highest anhydrouronic acid content, which was found to be pH of 2.0, extraction time of 62.31 min, and liquid-solid ratio of 35.07 mL/g. Under this optimal condition, the pectin yield, degree of esterification, methoxyl content, and anhydrouronic acid content were 24.30%, 73.30%, 10.45%, and 81.33%, respectively. At optimal conditions, watermelon rind pectin can be classified as high methoxyl and rapid-set pectin with high quality and high purity. Practical Applications. This study evaluated the pectin extraction from watermelon rind and carried out an optimization of multiple responses as a function of pH, time, and liquid-solid ratio to obtain the best preliminary quality parameters (pectin yield and anhydrouronic acid content). The results revealed that watermelon rind waste can be an inexpensive source to obtain good pectin quality and high purity. According to the chemical characterization and physicochemical properties studied, the extracted pectin from watermelon rind would have a high potential to be used in food industry.

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“…One significant implication of elevated gastric pH is the fast ionisation of the hydrophilic weak acid, e.g., alginic acid (pKa 3.4) [9], leading to a premature disintegration of the enteric coating in the gastric environment [10]. In this context, shellac-based coating provided gastric protection at elevated gastric pH.…”

Section: Introductionmentioning

confidence: 99%

“…We have previously reported the use of fatty glycerides dispersion in aqueous alginate solution to provide a pH-dependent release profile [10]. More recently, an O/W emulsion of waxes in alginate solution was developed to boost the gastric-resistant properties of the coated films [4].…”

Section: Introductionmentioning

confidence: 99%

A Novel Multilayer Natural Coating for Fed-State Gastric Protection

et al. 2022

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Several nutraceutical products require gastric protection against the hostile environment in the stomach. Currently marketed synthetic and semi-synthetic coatings suffer from major shortcomings such as poor gastric protection, slow-release response to pH change, and the use of artificial ingredients. The challenge of coating natural products is further exacerbated by the relatively high gastric pH in the fed state. In this work, a novel natural enteric coating is presented as a breakthrough alternative to current solutions. Two coating systems were devised: (i) a triple-layer coating that comprises a wax layer embedded between two alginate-based coatings, and (ii) a double-layer coating, where an overcoat of organic acids (fumaric or citric acid) is applied to an alginate-based coating. The multi-layer architecture did not impact the pH-responsive nature of the coating even when more biologically relevant Krebs bicarbonate buffer of lower buffer capacity was used. Interestingly, the gastric protection barrier of organic acid-based coating remained resistant at elevated gastric pH 2, 3, or 4 for 2 h. This is the first report of using an alginate-based coating to provide gastric protection against fed-state stomach conditions (pH 2–4). Being biodegradable, naturally occurring, and with no limit on daily intake, the reported novel coating provides a superior platform to current coating solutions for pharmaceutical and nutraceutical products.

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A novel natural GRAS-grade enteric coating for pharmaceutical and nutraceutical products

Cited by 17 publications

References 31 publications

Applications of polymer blends in drug delivery

Applications of polymer blends in drug delivery

Optimization and Preliminary Physicochemical Characterization of Pectin Extraction from Watermelon Rind (Citrullus lanatus) with Citric Acid

A Novel Multilayer Natural Coating for Fed-State Gastric Protection

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