Glycerol-silicone elastomers as active matrices with controllable release profiles

Piotr Mazurek, Michael A. Brook, Anne Ladegaard Skov*

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

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Abstract

Drug release regimes must be controlled for optimal therapeutic effect. While it is relatively straightforward to create first order release matrices, it can be challenging to avoid an initial burst. Matrices with zero-order profiles are perceived to be beneficial in many cases, but are even more difficult to formulate. We describe the straightforward synthesis of elastomeric composites prepared from silicone in which the active is dispersed in glycerol. The release of glycerol-soluble actives from films of these materials was shown to be tunable with respect to the order of release (zero- or first-order) simply by changing glycerol content. Importantly, release from the elastomers showed no burst effect. The discrete glycerol domains embedded within a silicone matrix act as reservoirs for active substances. Upon contact with aqueous media the active substances are released from matrices exhibiting zero-order, near zero-order or first-order release kinetics. Various parameters that could influence the release process include glycerol content, glycerol domain size or membrane thickness are thoroughly investigated, elucidating guidelines for creating matrices capable of delivering active substances at desired rates. Additionally, the composites proved to absorb significant amounts of liquid water (up to 1850 % of sample mass), a feature that can be tuned by manipulation of the composite structure.
Original languageEnglish
JournalLangmuir
Volume34
Issue number38
Pages (from-to)11559-11566
Number of pages8
ISSN0743-7463
DOIs
Publication statusPublished - 2018

Cite this

@article{07f26aa259674e1595a73dbf4ce61a20,
title = "Glycerol-silicone elastomers as active matrices with controllable release profiles",
abstract = "Drug release regimes must be controlled for optimal therapeutic effect. While it is relatively straightforward to create first order release matrices, it can be challenging to avoid an initial burst. Matrices with zero-order profiles are perceived to be beneficial in many cases, but are even more difficult to formulate. We describe the straightforward synthesis of elastomeric composites prepared from silicone in which the active is dispersed in glycerol. The release of glycerol-soluble actives from films of these materials was shown to be tunable with respect to the order of release (zero- or first-order) simply by changing glycerol content. Importantly, release from the elastomers showed no burst effect. The discrete glycerol domains embedded within a silicone matrix act as reservoirs for active substances. Upon contact with aqueous media the active substances are released from matrices exhibiting zero-order, near zero-order or first-order release kinetics. Various parameters that could influence the release process include glycerol content, glycerol domain size or membrane thickness are thoroughly investigated, elucidating guidelines for creating matrices capable of delivering active substances at desired rates. Additionally, the composites proved to absorb significant amounts of liquid water (up to 1850 {\%} of sample mass), a feature that can be tuned by manipulation of the composite structure.",
author = "Piotr Mazurek and Brook, {Michael A.} and Skov, {Anne Ladegaard}",
year = "2018",
doi = "10.1021/acs.langmuir.8b02039",
language = "English",
volume = "34",
pages = "11559--11566",
journal = "Langmuir",
issn = "0743-7463",
publisher = "American Chemical Society",
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}

Glycerol-silicone elastomers as active matrices with controllable release profiles. / Mazurek, Piotr; Brook, Michael A.; Skov, Anne Ladegaard.

In: Langmuir, Vol. 34, No. 38, 2018, p. 11559-11566.

Research output: Contribution to journalJournal articleResearchpeer-review

TY - JOUR

T1 - Glycerol-silicone elastomers as active matrices with controllable release profiles

AU - Mazurek, Piotr

AU - Brook, Michael A.

AU - Skov, Anne Ladegaard

PY - 2018

Y1 - 2018

N2 - Drug release regimes must be controlled for optimal therapeutic effect. While it is relatively straightforward to create first order release matrices, it can be challenging to avoid an initial burst. Matrices with zero-order profiles are perceived to be beneficial in many cases, but are even more difficult to formulate. We describe the straightforward synthesis of elastomeric composites prepared from silicone in which the active is dispersed in glycerol. The release of glycerol-soluble actives from films of these materials was shown to be tunable with respect to the order of release (zero- or first-order) simply by changing glycerol content. Importantly, release from the elastomers showed no burst effect. The discrete glycerol domains embedded within a silicone matrix act as reservoirs for active substances. Upon contact with aqueous media the active substances are released from matrices exhibiting zero-order, near zero-order or first-order release kinetics. Various parameters that could influence the release process include glycerol content, glycerol domain size or membrane thickness are thoroughly investigated, elucidating guidelines for creating matrices capable of delivering active substances at desired rates. Additionally, the composites proved to absorb significant amounts of liquid water (up to 1850 % of sample mass), a feature that can be tuned by manipulation of the composite structure.

AB - Drug release regimes must be controlled for optimal therapeutic effect. While it is relatively straightforward to create first order release matrices, it can be challenging to avoid an initial burst. Matrices with zero-order profiles are perceived to be beneficial in many cases, but are even more difficult to formulate. We describe the straightforward synthesis of elastomeric composites prepared from silicone in which the active is dispersed in glycerol. The release of glycerol-soluble actives from films of these materials was shown to be tunable with respect to the order of release (zero- or first-order) simply by changing glycerol content. Importantly, release from the elastomers showed no burst effect. The discrete glycerol domains embedded within a silicone matrix act as reservoirs for active substances. Upon contact with aqueous media the active substances are released from matrices exhibiting zero-order, near zero-order or first-order release kinetics. Various parameters that could influence the release process include glycerol content, glycerol domain size or membrane thickness are thoroughly investigated, elucidating guidelines for creating matrices capable of delivering active substances at desired rates. Additionally, the composites proved to absorb significant amounts of liquid water (up to 1850 % of sample mass), a feature that can be tuned by manipulation of the composite structure.

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DO - 10.1021/acs.langmuir.8b02039

M3 - Journal article

VL - 34

SP - 11559

EP - 11566

JO - Langmuir

JF - Langmuir

SN - 0743-7463

IS - 38

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