Micropellets coated with Kollicoat<sup>®</sup> Smartseal 30D for taste masking in liquid oral dosage forms

Dashevskiy, Andriy; Mohylyuk, Valentyn; Ahmed, Abid Riaz; Kolter, Karl; Guth, Felicitas; Bodmeier, Roland

doi:10.1080/03639045.2017.1323910

Cited by 14 publications

(13 citation statements)

References 22 publications

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“…The first step in developing a functional PPI was to select an appropriate pH-responsive polymer to act as an inert and stable coating in the subcutaneous environment, that also dissolves rapidly in the stomach (i.e., a reverse enteric coating). While many pH-responsive polymers are used commercially and have been reported in the literature, ,, none have been designed for long-term stability in the subcutaneous environment. This is likely due to a considerable challenge posed by reverse enteric coatingswater absorption.…”

Section: Resultsmentioning

confidence: 99%

“…However, these pH-sensitive polymers are not appropriate for long-term exposure to aqueous systems (e.g., subcutaneous tissues); even at near neutral pH values, coatings of these polymers exhibit considerable swelling, permeability, and dissolution behavior that is likely to result in premature release of any encapsulated cargo. 37,40,41 Therefore, to achieve the pH targeting required of a PPI, a pH-responsive polymer is needed to enable the formulation of a reverse enteric coating that is biocompatible and stable in the subcutaneous environment while providing rapid poison release in the gastric environment.…”

Section: ■ Introductionmentioning

confidence: 99%

“…Other types of subcutaneous implants, particularly implantable electronic devices, are designed to remain completely inert and lack any physiological degradation mechanism. − Conceivably, an implant with a biocompatible reverse enteric coating could provide stability in the subcutaneous environment (pH 7.4) while allowing dissolution and cargo release in the low-pH gastric environment. Reverse enteric coatings (e.g., Eudragit E and Kollicoat Smartseal 30 D) are commonly used to taste mask orally administered pharmaceutical formulations and consist of pH-sensitive polymers with low solubility in the oral cavity (average pH of 6.7 for saliva) and high solubility at gastric pH values. However, these pH-sensitive polymers are not appropriate for long-term exposure to aqueous systems (e.g., subcutaneous tissues); even at near neutral pH values, coatings of these polymers exhibit considerable swelling, permeability, and dissolution behavior that is likely to result in premature release of any encapsulated cargo. ,, Therefore, to achieve the pH targeting required of a PPI, a pH-responsive polymer is needed to enable the formulation of a reverse enteric coating that is biocompatible and stable in the subcutaneous environment while providing rapid poison release in the gastric environment.…”

Section: Introductionmentioning

confidence: 99%

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Toward Targeted Invasive Predator Control: Developing pH-Responsive Subcutaneous Implants for Native Mammals

Brewer

McWhorter

Sloper

et al. 2022

ACS Appl. Polym. Mater.

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Introduced predators are a significant threat to global biodiversity and are responsible for most of all modern bird, reptile, and mammal extinctions. In Australia, the introduced feral cat (Felis catus) kills 459 million mammals annually and leaves many species facing extinction. Attempted reintroductions of threatened mammal species often fail due to the persistence of intractable feral cats�termed "problem individuals"�and the swift depredation of the reintroduced population. Biomaterial implants could hold the key to targeting problem individuals. Herein, we report the development of the population-protecting implant, a subcutaneous implant for native mammals. The implant is intended to be inert within the subcutaneous environment for the life of the native mammal and to release a toxic payload in the gastric environment of a feral cat when ingested during a predation event. By toxifying and causing the death of the feral cat, the problem individual is eliminated, and the remaining population of native mammals is protected from further predation. To achieve this, an innovative reverse enteric coating was developed for use as a biomaterial, which exhibited a previously unreported level of pH selectivity for solubility at gastric pH. Large batches of implants were manufactured via fluidized-bed spray coating with a uniform reverse enteric coating and low intrabatch variability. Implants with a 300 μm coating afforded significant stability and retention of the payload at subcutaneous pH in vitro, with rapid release of the payload observed at gastric pH. In addition, implants exhibited favorable stability in vivo in rats, with no observed difference in biocompatibility compared to conventional radio-frequency identification microchips. This work demonstrates a proof of concept of an innovative type of implant and serves as the basis for its future development and translation into the field.

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Section: Resultsmentioning

confidence: 99%

Section: ■ Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Toward Targeted Invasive Predator Control: Developing pH-Responsive Subcutaneous Implants for Native Mammals

Brewer

McWhorter

Sloper

et al. 2022

ACS Appl. Polym. Mater.

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“…The spray-dried solid dispersion was stored, with a desiccant, in a double polybag. [18][19][20]…”

Section: Preparation Of Solid Dispersions By Spmentioning

confidence: 99%

Untitled

Mehta¹

2020

AJP

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Introduction: Many new chemical entities that are getting developed are poorly aqueous soluble and have low bioavailability. Out of many methods available for improving solubility, the solid dispersion by melt extrusion (ME) and spray drying (SP) is scalable and industrially applicable methods. Objective: The main objective of the present study was to explore the application of Kollicoat Smartseal 30D polymer for the solubility enhancement of poorly water-soluble drugs using solid dispersion approach. Materials and Methods: The Biopharmaceutical Classification System Class II drug simvastatin (SIM) was used as a model drug in this study. Solid dispersions of SIM and Kollicoat ® Smartseal 30D were prepared using two different processes, i.e., ME and spray-drying techniques. Both the techniques ME and SP are scalable and industry applicable. Results: The solid dispersion has been characterized using transmission using Fourier transforms infrared spectroscopy, scanning electron microscopy, differential scanning calorimetry, powder X-ray diffraction, saturation solubility, and in vitro drug release studies. Discussion and Conclusion: The improved dissolution profile portrayed the solubility enhancement of SIM in solid dispersions form compared to plain SIM. In nutshell, with the current research, a supportive argument was observed to suggest the suitability of Kollicoat ® Smartseal 30D based solid dispersions for enhancing solubility of poorly soluble drugs.

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“…However, all these methods have an unsatisfactory effect. For example, adding sweeteners is invalid for extremely bitter drugs, the film coating can only coat the tablet, which is difficult for children to swallow and difficult to divide the dose [ 6 ], and chemical modification may influence the in vivo efficacy of the drugs [ 7 ]. Overall, the biggest disadvantage of these taste-masking techniques is that they cannot mask the poor taste of traditional Chinese medicines (TCMs) with multicomponent bitter substances.…”

Section: Introductionmentioning

confidence: 99%

The Taste-Masking Mechanism of Chitosan at the Molecular Level on Bitter Drugs of Alkaloids and Flavonoid Glycosides from Traditional Chinese Medicine

Sun

Chen

et al. 2022

Molecules

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Taste masking of traditional Chinese medicines (TCMs) containing multiple bitter components remains an important challenge. In this study, berberine (BER) in alkaloids and phillyrin (PHI) in flavonoid glycosides, which are common bitter components in traditional Chinese medicines, were selected as model drugs. Chitosan (CS) was used to mask their unfriendly taste. Firstly, from the molecular level, we explained the taste-masking mechanism of CS on those two bitter components in detail. Based on those taste-masking mechanisms, the bitter taste of a mixture of BER and PHI was easily masked by CS in this work. The physicochemical characterization results showed the taste-masking compounds formed by CS with BER (named as BER/CS) and PHI (named as PHI/CS) were uneven in appearance. The drug binding efficiency of BER/CS and PHI/CS was 50.15 ± 2.63% and 67.10 ± 2.52%, respectively. The results of DSC, XRD, FTIR and molecular simulation further indicated that CS mainly masks the bitter taste by disturbing the binding site of bitter drugs and bitter receptors in the oral cavity via forming hydrogen bonds between its hydroxyl or amine groups and the nucleophilic groups of BER and PHI. The taste-masking evaluation results by the electronic tongue test confirmed the excellent taste-masking effects on alkaloids, flavonoid glycosides or a mixture of the two kinds of bitter components. The in vitro release as well as in vivo pharmacokinetic results suggested that the taste-masked compounds in this work could achieve rapid drug release in the gastric acid environment and did not influence the in vivo pharmacokinetic results of the drug. The taste-masking method in this work may have potential for the taste masking of traditional Chinese medicine compounds containing multiple bitter components.

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Micropellets coated with Kollicoat^® Smartseal 30D for taste masking in liquid oral dosage forms

Cited by 14 publications

References 22 publications

Toward Targeted Invasive Predator Control: Developing pH-Responsive Subcutaneous Implants for Native Mammals

Toward Targeted Invasive Predator Control: Developing pH-Responsive Subcutaneous Implants for Native Mammals

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The Taste-Masking Mechanism of Chitosan at the Molecular Level on Bitter Drugs of Alkaloids and Flavonoid Glycosides from Traditional Chinese Medicine

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Micropellets coated with Kollicoat® Smartseal 30D for taste masking in liquid oral dosage forms

Cited by 14 publications

References 22 publications

Toward Targeted Invasive Predator Control: Developing pH-Responsive Subcutaneous Implants for Native Mammals

Toward Targeted Invasive Predator Control: Developing pH-Responsive Subcutaneous Implants for Native Mammals

Untitled

The Taste-Masking Mechanism of Chitosan at the Molecular Level on Bitter Drugs of Alkaloids and Flavonoid Glycosides from Traditional Chinese Medicine

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Micropellets coated with Kollicoat^® Smartseal 30D for taste masking in liquid oral dosage forms