Use of hydrophilic pharmaceutical excipients to modulate release of metal ions from silicone elastomers
Silicone elastomers based on polydimethylsiloxane are biocompatible and non-biodegradable thermosetting polymers used in various drug delivery applications, including subdermal implants, vaginal rings, and intrauterine devices. Without exception, all marketed silicone elastomer drug delivery product...
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2025-12-01
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| Series: | Drug Delivery |
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| Online Access: | https://www.tandfonline.com/doi/10.1080/10717544.2025.2545515 |
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| author | Xin Shen Xinyu Zhao Clare F. McCoy Yahya H. Dallal Bashi Peter Boyd R. Karl Malcolm |
| author_facet | Xin Shen Xinyu Zhao Clare F. McCoy Yahya H. Dallal Bashi Peter Boyd R. Karl Malcolm |
| author_sort | Xin Shen |
| collection | DOAJ |
| description | Silicone elastomers based on polydimethylsiloxane are biocompatible and non-biodegradable thermosetting polymers used in various drug delivery applications, including subdermal implants, vaginal rings, and intrauterine devices. Without exception, all marketed silicone elastomer drug delivery products provide sustained or controlled release of highly hydrophobic small drug molecules, since drug solubility in the silicone matrix is a prerequisite for molecular diffusion and release. We are interested in developing multipurpose silicone elastomer vaginal rings for local administration of metal ions—such as copper and zinc—for non-hormonal contraception and antimicrobial therapy. However, sustained/controlled release of metal ions from silicone elastomers containing metal nanopowders or metal salts is challenging due to their limited solubility in silicone. In this study, we assess the potential for enhancing the release of copper or zinc ions from silicone elastomer devices by co-formulating copper nanopowder, zinc nanopowder, copper sulfate, or zinc acetate with four common pharmaceutical excipients—gelatin, polyvinylpyrrolidone, sucrose, and hydroxypropyl methylcellulose. The study demonstrates that (i) copper/zinc nanopowders and salts can be successfully incorporated into addition-cure silicone elastomers, (ii) in vitro release of Cu2+/Zn2 ions from silicone elastomers loaded with divalent salts was ∼100 times greater compared to nanopowders; (iii) incorporation of gelatin, polyvinylpyrrolidone, sucrose and hydroxypropyl methylcellulose significantly enhanced the release of Cu2+/Zn2+ ions (up to ∼30-fold), and (iv) enhanced release was due to water absorption into the silicone elastomer devices, causing swelling of the devices to an extent proportional to the excipient loading. |
| format | Article |
| id | doaj-art-9beedab72bfa4b9b9ce8434d0fed62d9 |
| institution | Kabale University |
| issn | 1071-7544 1521-0464 |
| language | English |
| publishDate | 2025-12-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj-art-9beedab72bfa4b9b9ce8434d0fed62d92025-08-21T13:08:36ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642025-12-0132110.1080/10717544.2025.2545515Use of hydrophilic pharmaceutical excipients to modulate release of metal ions from silicone elastomersXin Shen0Xinyu Zhao1Clare F. McCoy2Yahya H. Dallal Bashi3Peter Boyd4R. Karl Malcolm5School of Pharmacy, Queen’s University Belfast, Belfast, UKSchool of Pharmacy, Queen’s University Belfast, Belfast, UKSchool of Pharmacy, Queen’s University Belfast, Belfast, UKCollege of Pharmacy, University of Sharjah, Sharjah, United Arab EmiratesSchool of Pharmacy, Queen’s University Belfast, Belfast, UKSchool of Pharmacy, Queen’s University Belfast, Belfast, UKSilicone elastomers based on polydimethylsiloxane are biocompatible and non-biodegradable thermosetting polymers used in various drug delivery applications, including subdermal implants, vaginal rings, and intrauterine devices. Without exception, all marketed silicone elastomer drug delivery products provide sustained or controlled release of highly hydrophobic small drug molecules, since drug solubility in the silicone matrix is a prerequisite for molecular diffusion and release. We are interested in developing multipurpose silicone elastomer vaginal rings for local administration of metal ions—such as copper and zinc—for non-hormonal contraception and antimicrobial therapy. However, sustained/controlled release of metal ions from silicone elastomers containing metal nanopowders or metal salts is challenging due to their limited solubility in silicone. In this study, we assess the potential for enhancing the release of copper or zinc ions from silicone elastomer devices by co-formulating copper nanopowder, zinc nanopowder, copper sulfate, or zinc acetate with four common pharmaceutical excipients—gelatin, polyvinylpyrrolidone, sucrose, and hydroxypropyl methylcellulose. The study demonstrates that (i) copper/zinc nanopowders and salts can be successfully incorporated into addition-cure silicone elastomers, (ii) in vitro release of Cu2+/Zn2 ions from silicone elastomers loaded with divalent salts was ∼100 times greater compared to nanopowders; (iii) incorporation of gelatin, polyvinylpyrrolidone, sucrose and hydroxypropyl methylcellulose significantly enhanced the release of Cu2+/Zn2+ ions (up to ∼30-fold), and (iv) enhanced release was due to water absorption into the silicone elastomer devices, causing swelling of the devices to an extent proportional to the excipient loading.https://www.tandfonline.com/doi/10.1080/10717544.2025.2545515Drug deliverygelatinpolyvinylpyrrolidonehydroxypropyl methylcellulosesucrosesilicone rubber |
| spellingShingle | Xin Shen Xinyu Zhao Clare F. McCoy Yahya H. Dallal Bashi Peter Boyd R. Karl Malcolm Use of hydrophilic pharmaceutical excipients to modulate release of metal ions from silicone elastomers Drug Delivery Drug delivery gelatin polyvinylpyrrolidone hydroxypropyl methylcellulose sucrose silicone rubber |
| title | Use of hydrophilic pharmaceutical excipients to modulate release of metal ions from silicone elastomers |
| title_full | Use of hydrophilic pharmaceutical excipients to modulate release of metal ions from silicone elastomers |
| title_fullStr | Use of hydrophilic pharmaceutical excipients to modulate release of metal ions from silicone elastomers |
| title_full_unstemmed | Use of hydrophilic pharmaceutical excipients to modulate release of metal ions from silicone elastomers |
| title_short | Use of hydrophilic pharmaceutical excipients to modulate release of metal ions from silicone elastomers |
| title_sort | use of hydrophilic pharmaceutical excipients to modulate release of metal ions from silicone elastomers |
| topic | Drug delivery gelatin polyvinylpyrrolidone hydroxypropyl methylcellulose sucrose silicone rubber |
| url | https://www.tandfonline.com/doi/10.1080/10717544.2025.2545515 |
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