Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery

Kim, Min Soo; Yeom, Dong Woo; Kim, Dae Jung; Yoon, Ho Yub; Kim, Chang‐Hyun; Son, Ho Yong; Kim, Jin Han; Lee, Sang Kil; Choi, Young Wook

doi:10.2147/dddt.s123412

Cited by 27 publications

(9 citation statements)

References 33 publications

(32 reference statements)

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“…A normal distribution is considered a crucial assumption for statistical analysis. Normal probability plots for standardized residuals were linear, indicating that the experimental run data were normally distributed ( Supplementary Figure S1A ).4, 43 4 Pareto charts indicating the relative importance of the individual and interaction effects based on Student’s t -tests are shown in Supplementary Figure S1B . Statistically significant independent factors were extended the dotted bar which positioned at α = 0.05.…”

Section: Resultsmentioning

confidence: 99%

Development of a Solid Supersaturable Micelle of Revaprazan for Improved Dissolution and Oral Bioavailability Using Box-Behnken Design

Goo¹,

Sa²,

Choi³

et al. 2021

IJN

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Purpose To enhance the oral bioavailability of revaprazan (RVP), a novel solid, supersaturable micelle (SSuM) was developed. Methods Surfactants and solid carriers were screened based on a solubility and a flowability test, respectively. Supersaturating agents, including Poloxamer 407 (P407), were screened. The SSuM was optimized using a Box-Behnken design with three independent variables, including Gelucire 44/14:Brij L4 (G44/BL4; X 1 ) and the amounts of Florite PS-10 (FLO; X 2 ) and Vivapur 105 (VP105; X 3 ), and three response variables, ie, dissolution efficiency at 30 min (Y 1 ), dissolution enhancing capacity (Y 2 ), and Carr’s index (Y 3 ). The solid state property was evaluated, and a dissolution test was conducted. RVP, Revanex ® , solid micelle (P407-free from the composition of SSuM), and SSuM were orally administrated to rats (RVP 20 mg equivalent/kg) for in vivo pharmacokinetic study. Results G44 and BL4 showed great solubility, with a critical micelle concentration range of 119.2–333.0 μg/mL. P407 had an excellent supersaturating effect. FLO and VP105 were selected as solid carriers, with a critical solidifying ratio (g/mL) of 0.30 and 0.91, respectively. With optimized values of X 1 (–0.41), X 2 (0.31), and X 3 (–0.78), RVP (200 mg)-containing SSuM consisting of G44 (253.8 mg), BL4 (106.2 mg), FLO (99.3 mg), VP105 (199.8 mg), and P407 (40 mg) was developed, resulting in Y 1 (40.3%), Y 2 (0.008), and Y 3 (12.3%). RVP existed in an amorphous state in the optimized SSuM, and the SSuM formed a nanosized dispersion in the aqueous phase, with approximately 71.7% dissolution at 2 h. The optimized SSuM improved the relative bioavailability of RVP in rats by approximately 478%, 276%, and 161% compared to raw RVP, Revanex ® , and solid micelle, respectively. Conclusion The optimized SSuM has great potential for the development of solidified formulations of poorly water-soluble drugs with improved oral absorption.

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Section: Resultsmentioning

confidence: 99%

Development of a Solid Supersaturable Micelle of Revaprazan for Improved Dissolution and Oral Bioavailability Using Box-Behnken Design

Goo¹,

Sa²,

Choi³

et al. 2021

IJN

Self Cite

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“…However, the amount of β-carotene in the intestinal phase (bioaccessibility) increased significantly, which is in agreement with the expected behaviour for these polymers that swell at neutral pHs. Kim et al [ 54 ] reported that ethylcellulose coatings are able to retard the gastric and intestinal drug release, which is then gradually released in the colon. Drug release was impeded by the layer of ethylcellulose, regardless the acidity of the medium.…”

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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“…A double-layer coated colon-specific drug delivery system was developed by Kim et al The system consisted of a chitosan-based polymeric subcoating of the core tablet (containing citric acid for microclimate acidification), followed by an enteric EC coating. The system showed drug release in a controlled manner by inhibiting drug release in the stomach and intestine, but releasing the drug gradually in the colon [32]. The example of utilizing EC as a release-retarding coating is a commercially available preparation called Micro-K ® in hard gelatin capsules, containing small crystalline particles of potassium chloride (KCl).…”

Section: Applicability Of Ec In Pharmaceutical Formulationsmentioning

confidence: 99%

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

2019

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Polymers constitute the most important group of excipients utilized in modern pharmaceutical technology, playing an essential role in the development of drug dosage forms. Synthetic, semisynthetic, and natural polymeric materials offer opportunities to overcome different formulative challenges and to design novel dosage forms for controlled release or for site-specific drug delivery. They are extensively used to design therapeutic systems, modify drug release, or mask unpleasant drug taste. Cellulose derivatives are characterized by different physicochemical properties, such as swellability, viscosity, biodegradability, pH dependency, or mucoadhesion, which determine their use in industry. One cellulose derivative with widespread application is ethylcellulose. Ethylcellulose is used in pharmaceutical technology as a coating agent, flavoring fixative, binder, filler, film-former, drug carrier, or stabilizer. The aim of this article is to provide a broad overview of ethylcellulose utilization for pharmaceutical purposes, with particular emphasis on its multidirectional role in the development of oral and topical drug dosage forms.

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Development of a chitosan based double layer-coated tablet as a platform for colon-specific drug delivery

Cited by 27 publications

References 33 publications

Development of a Solid Supersaturable Micelle of Revaprazan for Improved Dissolution and Oral Bioavailability Using Box-Behnken Design

Development of a Solid Supersaturable Micelle of Revaprazan for Improved Dissolution and Oral Bioavailability Using Box-Behnken Design

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

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

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