Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

Wasilewska, Katarzyna; Winnicka, Katarzyna

doi:10.3390/ma12203386

Cited by 125 publications

(83 citation statements)

References 71 publications

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“…Indeed, ethylcellulose is insoluble in water at any physiological pH, and there are no digestive enzymes able to metabolize ethylcellulose. However, it can swell in the presence of gastric juice making it permeable for water and allowing β-carotene diffusion and release [ 53 ]. That should be the reason for the low amount of β-carotene obtained in the gastric (2.7%) and intestinal (8.3%) phases, respectively ( Table 2 ).…”

Section: Resultsmentioning

confidence: 99%

Bio-Based Nanoparticles as a Carrier of β-Carotene: Production, Characterisation and In Vitro Gastrointestinal Digestion

et al. 2020

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β-carotene loaded bio-based nanoparticles (NPs) were produced by the solvent-displacement method using two polymers: zein and ethylcellulose. The production of NPs was optimised through an experimental design and characterised in terms of average size and polydispersity index. The processing conditions that allowed to obtain NPs (<100 nm) were used for β-carotene encapsulation. Then β-carotene loaded NPs were characterised in terms of zeta potential and encapsulation efficiency. Transmission electron microscopy, Fourier transform infrared spectroscopy and X-ray diffraction analysis were performed for further morphological and chemical characterisation. In the end, a static in vitro digestion following the INFOGEST protocol was performed and the bioaccessibility of β-carotene encapsulated in both NPs was determined. Results show that the best conditions for a size-controlled production with a narrow size distribution are lower polymer concentrations and higher antisolvent concentrations. The encapsulation of β-carotene in ethylcellulose NPs resulted in nanoparticles with a mean average size of 60 ± 9 nm and encapsulation efficiency of 74 ± 2%. β-carotene loaded zein-based NPs resulted in a mean size of 83 ± 8 nm and encapsulation efficiency of 93 ± 4%. Results obtained from the in vitro digestion showed that β-carotene bioaccessibility when encapsulated in zein NPs is 37 ± 1%, which is higher than the value of 8.3 ± 0.1% obtained for the ethylcellulose NPs.

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Section: Resultsmentioning

confidence: 99%

Bio-Based Nanoparticles as a Carrier of β-Carotene: Production, Characterisation and In Vitro Gastrointestinal Digestion

et al. 2020

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“…Importantly, there were no adverse reactions reported during the study period. The use of an ethyl cellulose and alginate coating on the study product resulted in granules of amino acids that were stable in the stomach with a gradual disintegration during small-intestine transit [29,31]. This may explain the favourable gastrointestinal tolerability in this study.…”

Section: Discussionmentioning

confidence: 74%

“…It may also be helpful during pregnancy for women struggling with nausea and vomiting associated with the taste and smell of protein substitutes [28]. The excipients used for the coating of the study product are considered safe for pregnancy and lactation [29].…”

Section: Discussionmentioning

confidence: 99%

An Observational Study Evaluating the Introduction of a Prolonged-Release Protein Substitute to the Dietary Management of Children with Phenylketonuria

et al. 2020

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Dietary restriction of phenylalanine combined with a protein substitute prevents intellectual disability in patients with phenylketonuria (PKU). However, current protein substitutes are associated with low adherence owing to unpalatability and burdensome administration regimens. This prospective, observational acceptability study in children with PKU assessed the use of a prolonged-release protein substitute designed with an ethyl cellulose and arginate coating masking the bitter taste, smell and reducing the osmolarity of free amino acids. The study product was mixed with the subject’s food or drink and replaced ≥1 dose per day of the subject’s usual protein substitute for 7 days. Seven of 13 subjects were able to take their prescribed dose over the 7 day period. Most subjects mixed the test protein substitute with food or fruit juice. Reduced blood phenylalanine levels (n = 5) and improved phenylalanine/tyrosine ratio (n = 4) were recorded from baseline to Day 7, respectively. Four subjects reported fewer gastrointestinal symptoms compared to baseline. There were no cases of diarrhoea, constipation, bloating, nausea or vomiting. No adverse reactions were reported. In conclusion, the novel prolonged-release protein substitute was taken in a different way to a typical protein substitute and enabled satisfactory blood phenylalanine control. The study product was well tolerated; subjects experienced fewer gastrointestinal symptoms than with their previous treatment. Although the results of this pilot study provide reassuring data, longer-term studies evaluating adherence and blood phenylalanine control are necessary.

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“…Coating materials for sustained drug release are usually water-insoluble and pH-independent, and are exemplified by ethyl cellulose, polyvinyl acetate, and polymethacrylate copolymers [ 68 , 70 ]. These polymers have good film forming properties and mechanical strength, making them suitable for sustained drug release coating [ 71 ]. The combined use of hydrophobic and hydrophilic polymers has also been attempted to optimize drug release.…”

Section: Pharmaceutical Application Of Film Coatingmentioning

confidence: 99%

Pharmaceutical Application of Tablet Film Coating

et al. 2020

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Tablet film coating is a common but critical process providing various functionalities to tablets, thereby meeting diverse clinical needs and increasing the value of oral solid dosage forms. Tablet film coating is a technology-driven process and the evolution of coated dosage forms relies on advancements in coating technology, equipment, analytical techniques, and coating materials. Although multiple coating techniques are developed for solvent-based or solvent-free coating processes, each method has advantages and disadvantages that may require continuous technical refinement. In the film coating process, intra- and inter-batch coating uniformity of tablets is critical to ensure the quality of the final product, especially for active film coating containing active pharmaceutical ingredients in the coating layer. In addition to experimental evaluation, computational modeling is also actively pursued to predict the influence of operation parameters on the quality of the final product and optimize process variables of tablet film coating. The concerted efforts of experiments and computational modeling can save time and cost in optimizing the tablet coating process. This review provides a brief overview of tablet film coating technology and modeling approaches with a focus on recent advancements in pharmaceutical applications.

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Ethylcellulose–A Pharmaceutical Excipient with Multidirectional Application in Drug Dosage Forms Development

Cited by 125 publications

References 71 publications

Bio-Based Nanoparticles as a Carrier of β-Carotene: Production, Characterisation and In Vitro Gastrointestinal Digestion

Bio-Based Nanoparticles as a Carrier of β-Carotene: Production, Characterisation and In Vitro Gastrointestinal Digestion

An Observational Study Evaluating the Introduction of a Prolonged-Release Protein Substitute to the Dietary Management of Children with Phenylketonuria

Pharmaceutical Application of Tablet Film Coating

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