High-throughput screening of PLGA thin films utilizing hydrophobic fluorescent dyes for hydrophobic drug compounds
Hydrophobic, antirestenotic drugs such as paclitaxel (PCTX) and rapamycin are often incorporated into thin film coatings for local delivery using implantable medical devices and polymers such as drug-eluting stents and balloons. Selecting the optimum coating formulation through screening the release...
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sg-ntu-dr.10356-806402023-07-14T15:49:59Z High-throughput screening of PLGA thin films utilizing hydrophobic fluorescent dyes for hydrophobic drug compounds Steele, Terry W. J. Huang, Charlotte L. Kumar, Saranya Widjaja, Effendi Boey, Freddy Yin Chiang Loo, Joachim Say Chye Venkatraman, Subbu S. School of Materials Science & Engineering PLGA Paclitaxel Hydrophobic, antirestenotic drugs such as paclitaxel (PCTX) and rapamycin are often incorporated into thin film coatings for local delivery using implantable medical devices and polymers such as drug-eluting stents and balloons. Selecting the optimum coating formulation through screening the release profile of these drugs in thin films is time consuming and labor intensive. We describe here a high-throughput assay utilizing three model hydrophobic fluorescent compounds: fluorescein diacetate (FDAc), coumarin-6, and rhodamine 6G that were incorporated into poly(d,l-lactide-co-glycolide) (PLGA) and PLGA–polyethylene glycol films. Raman microscopy determined the hydrophobic fluorescent dye distribution within the PLGA thin films in comparison with that of PCTX. Their subsequent release was screened in a high-throughput assay and directly compared with HPLC quantification of PCTX release. It was observed that PCTX controlled-release kinetics could be mimicked by a hydrophobic dye that had similar octanol–water partition coefficient values and homogeneous dissolution in a PLGA matrix as the drug. In particular, FDAc was found to be the optimal hydrophobic dye at modeling the burst release as well as the total amount of PCTX released over a period of 30 days. NRF (Natl Research Foundation, S’pore) Accepted version 2017-03-16T06:25:21Z 2019-12-06T13:53:43Z 2017-03-16T06:25:21Z 2019-12-06T13:53:43Z 2011 Journal Article Steele, T. W. J., Huang, C. L., Kumar, S., Widjaja, E., Boey, F. Y. C., Loo, J. S. C., et al. (2011). High-throughput screening of PLGA thin films utilizing hydrophobic fluorescent dyes for hydrophobic drug compounds. Journal of Pharmaceutical Sciences, 100(10), 4317-4329. 0022-3549 https://hdl.handle.net/10356/80640 http://hdl.handle.net/10220/42180 10.1002/jps.22625 en Journal of Pharmaceutical Sciences © 2011 Wiley-Liss, Inc. This is the author created version of a work that has been peer reviewed and accepted for publication by Journal of Pharmaceutical Sciences, Wiley-Liss, Inc. It incorporates referee’s comments but changes resulting from the publishing process, such as copyediting, structural formatting, may not be reflected in this document. The published version is available at: [http://dx.doi.org/10.1002/jps.22625]. 29 p. application/pdf |
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PLGA Paclitaxel Steele, Terry W. J. Huang, Charlotte L. Kumar, Saranya Widjaja, Effendi Boey, Freddy Yin Chiang Loo, Joachim Say Chye Venkatraman, Subbu S. High-throughput screening of PLGA thin films utilizing hydrophobic fluorescent dyes for hydrophobic drug compounds |
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Hydrophobic, antirestenotic drugs such as paclitaxel (PCTX) and rapamycin are often incorporated into thin film coatings for local delivery using implantable medical devices and polymers such as drug-eluting stents and balloons. Selecting the optimum coating formulation through screening the release profile of these drugs in thin films is time consuming and labor intensive. We describe here a high-throughput assay utilizing three model hydrophobic fluorescent compounds: fluorescein diacetate (FDAc), coumarin-6, and rhodamine 6G that were incorporated into poly(d,l-lactide-co-glycolide) (PLGA) and PLGA–polyethylene glycol films. Raman microscopy determined the hydrophobic fluorescent dye distribution within the PLGA thin films in comparison with that of PCTX. Their subsequent release was screened in a high-throughput assay and directly compared with HPLC quantification of PCTX release. It was observed that PCTX controlled-release kinetics could be mimicked by a hydrophobic dye that had similar octanol–water partition coefficient values and homogeneous dissolution in a PLGA matrix as the drug. In particular, FDAc was found to be the optimal hydrophobic dye at modeling the burst release as well as the total amount of PCTX released over a period of 30 days. |
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School of Materials Science & Engineering |
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School of Materials Science & Engineering Steele, Terry W. J. Huang, Charlotte L. Kumar, Saranya Widjaja, Effendi Boey, Freddy Yin Chiang Loo, Joachim Say Chye Venkatraman, Subbu S. |
format |
Article |
author |
Steele, Terry W. J. Huang, Charlotte L. Kumar, Saranya Widjaja, Effendi Boey, Freddy Yin Chiang Loo, Joachim Say Chye Venkatraman, Subbu S. |
author_sort |
Steele, Terry W. J. |
title |
High-throughput screening of PLGA thin films utilizing hydrophobic fluorescent dyes for hydrophobic drug compounds |
title_short |
High-throughput screening of PLGA thin films utilizing hydrophobic fluorescent dyes for hydrophobic drug compounds |
title_full |
High-throughput screening of PLGA thin films utilizing hydrophobic fluorescent dyes for hydrophobic drug compounds |
title_fullStr |
High-throughput screening of PLGA thin films utilizing hydrophobic fluorescent dyes for hydrophobic drug compounds |
title_full_unstemmed |
High-throughput screening of PLGA thin films utilizing hydrophobic fluorescent dyes for hydrophobic drug compounds |
title_sort |
high-throughput screening of plga thin films utilizing hydrophobic fluorescent dyes for hydrophobic drug compounds |
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2017 |
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https://hdl.handle.net/10356/80640 http://hdl.handle.net/10220/42180 |
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1772828015210790912 |