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Novel hydrophilic matrix system with non-uniform drug distribution for zero-order release kinetics.

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Title: Novel hydrophilic matrix system with non-uniform drug distribution for zero-order release kinetics.
Authors: Cerea, Matteo1, Maroni, Alessandra1, Palugan, Luca1, Bellini, Marco1, Foppoli, Anastasia1 anastasia.foppoli@unimi.it, Melocchi, Alice1, Zema, Lucia1, Gazzaniga, Andrea1
Source: Journal of Controlled Release. Oct2018, Vol. 287, p247-256. 10p.
Subjects: Hydrophilic compounds, Polymers, Acetaminophen, Drugs, Controlled release drugs
Abstract: Abstract A decrease in the release rate over time is typically encountered when dealing with hydrophilic matrix systems for oral prolonged release due to progressive increase of the distance the drug molecules have to cover to diffuse outwards and reduction of the area of the glassy matrix at the swelling front. In order to solve this issue, a novel formulation approach based on non-uniform distribution of the active ingredient throughout the swellable polymer matrix was proposed and evaluated. Various physical mixtures of polymer (high-viscosity hypromellose) and drug tracer (acetaminophen), having decreasing concentrations of the latter, were applied by powder-layering onto inert core seeds. The resulting gradient matrices showed to possess satisfactory physico-technological characteristics, with spherical shape and consistent thickness of the layers sequentially applied. The non-uniform matrix composition pursued was confirmed by Raman mapping analysis. As compared with a system having uniform distribution of the drug tracer, the multi-layer formulations were proved to enhance linearity of release. The simple design concept, advantageous technique, which involves no solvents nor high-impact drying operations, and the polymeric material of established use make the delivery platform hereby proposed a valuable strategy to improve the performance of hydrophilic matrix systems. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]
Copyright of Journal of Controlled Release is the property of Elsevier B.V. and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
Database: Engineering Source
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  Availability: 0
Header DbId: egs
DbLabel: Engineering Source
An: 131848036
AccessLevel: 6
PubType: Academic Journal
PubTypeId: academicJournal
PreciseRelevancyScore: 0
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  Data: Novel hydrophilic matrix system with non-uniform drug distribution for zero-order release kinetics.
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  Data: <searchLink fieldCode="JN" term="%22Journal+of+Controlled+Release%22">Journal of Controlled Release</searchLink>. Oct2018, Vol. 287, p247-256. 10p.
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  Data: <searchLink fieldCode="DE" term="%22Hydrophilic+compounds%22">Hydrophilic compounds</searchLink><br /><searchLink fieldCode="DE" term="%22Polymers%22">Polymers</searchLink><br /><searchLink fieldCode="DE" term="%22Acetaminophen%22">Acetaminophen</searchLink><br /><searchLink fieldCode="DE" term="%22Drugs%22">Drugs</searchLink><br /><searchLink fieldCode="DE" term="%22Controlled+release+drugs%22">Controlled release drugs</searchLink>
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  Data: Abstract A decrease in the release rate over time is typically encountered when dealing with hydrophilic matrix systems for oral prolonged release due to progressive increase of the distance the drug molecules have to cover to diffuse outwards and reduction of the area of the glassy matrix at the swelling front. In order to solve this issue, a novel formulation approach based on non-uniform distribution of the active ingredient throughout the swellable polymer matrix was proposed and evaluated. Various physical mixtures of polymer (high-viscosity hypromellose) and drug tracer (acetaminophen), having decreasing concentrations of the latter, were applied by powder-layering onto inert core seeds. The resulting gradient matrices showed to possess satisfactory physico-technological characteristics, with spherical shape and consistent thickness of the layers sequentially applied. The non-uniform matrix composition pursued was confirmed by Raman mapping analysis. As compared with a system having uniform distribution of the drug tracer, the multi-layer formulations were proved to enhance linearity of release. The simple design concept, advantageous technique, which involves no solvents nor high-impact drying operations, and the polymeric material of established use make the delivery platform hereby proposed a valuable strategy to improve the performance of hydrophilic matrix systems. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]
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  Data: <i>Copyright of Journal of Controlled Release is the property of Elsevier B.V. and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.)
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RecordInfo BibRecord:
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      – Type: doi
        Value: 10.1016/j.jconrel.2018.08.027
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      – Code: eng
        Text: English
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        PageCount: 10
        StartPage: 247
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      – SubjectFull: Hydrophilic compounds
        Type: general
      – SubjectFull: Polymers
        Type: general
      – SubjectFull: Acetaminophen
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      – SubjectFull: Drugs
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      – SubjectFull: Controlled release drugs
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      – TitleFull: Novel hydrophilic matrix system with non-uniform drug distribution for zero-order release kinetics.
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            NameFull: Foppoli, Anastasia
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              Text: Oct2018
              Type: published
              Y: 2018
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              Value: 287
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