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Article: Extended Release of Native Drug Conjugated in Polyketal Microparticles

TitleExtended Release of Native Drug Conjugated in Polyketal Microparticles
Authors
Issue Date2016
PublisherAmerican Chemical Society. The Journal's web site is located at http://pubs.acs.org/journals/jacsat/index.html
Citation
Journal of the American Chemical Society, 2016, v. 138 n. 19, p. 6127-6130 How to Cite?
AbstractPolyketals, which can be biodegradable, have good biocompatibility, and are pH-sensitive, could have broad applicability in drug delivery and other biomedical applications. However, facile synthesis of high molecular weight polyketals is challenging, and short durations of drug release from polyketal particulate formulations limit their application in drug delivery. Here we report the synthesis of a di-isopropenyl ether monomer and its use to synthesize high molecular weight estradiol-polyketal conjugates by addition polymerization. Microparticles were prepared from the estradiol-polyketal conjugate, where estradiol was incorporated into the polymer backbone. The particles had high drug loading and significantly prolonged drug release. Release of estradiol from the drug-polyketal conjugate microparticles was acid-responsive, as evidenced by faster drug release at low pH and with co-incorporation of PLGA. Tissue reaction to the microparticles was benign in vivo. Polyketal drug conjugates are promising candidates for long-acting drug delivery systems to treat chronic diseases.
Persistent Identifierhttp://hdl.handle.net/10722/260277
ISSN
2017 Impact Factor: 14.357
2015 SCImago Journal Rankings: 7.123
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorGuo, ST-
dc.contributor.authorNakagawa, Y-
dc.contributor.authorBarhoumi, A-
dc.contributor.authorWang, W-
dc.contributor.authorZhan, CY-
dc.contributor.authorTong, R-
dc.contributor.authorSantamaria, C-
dc.contributor.authorKohane, DS-
dc.date.accessioned2018-09-12T07:02:51Z-
dc.date.available2018-09-12T07:02:51Z-
dc.date.issued2016-
dc.identifier.citationJournal of the American Chemical Society, 2016, v. 138 n. 19, p. 6127-6130-
dc.identifier.issn0002-7863-
dc.identifier.urihttp://hdl.handle.net/10722/260277-
dc.description.abstractPolyketals, which can be biodegradable, have good biocompatibility, and are pH-sensitive, could have broad applicability in drug delivery and other biomedical applications. However, facile synthesis of high molecular weight polyketals is challenging, and short durations of drug release from polyketal particulate formulations limit their application in drug delivery. Here we report the synthesis of a di-isopropenyl ether monomer and its use to synthesize high molecular weight estradiol-polyketal conjugates by addition polymerization. Microparticles were prepared from the estradiol-polyketal conjugate, where estradiol was incorporated into the polymer backbone. The particles had high drug loading and significantly prolonged drug release. Release of estradiol from the drug-polyketal conjugate microparticles was acid-responsive, as evidenced by faster drug release at low pH and with co-incorporation of PLGA. Tissue reaction to the microparticles was benign in vivo. Polyketal drug conjugates are promising candidates for long-acting drug delivery systems to treat chronic diseases.-
dc.languageeng-
dc.publisherAmerican Chemical Society. The Journal's web site is located at http://pubs.acs.org/journals/jacsat/index.html-
dc.relation.ispartofJournal of the American Chemical Society-
dc.rightsThis document is the Accepted Manuscript version of a Published Work that appeared in final form in [JournalTitle], copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see [insert ACS Articles on Request author-directed link to Published Work, see http://pubs.acs.org/page/policy/articlesonrequest/index.html].-
dc.titleExtended Release of Native Drug Conjugated in Polyketal Microparticles-
dc.typeArticle-
dc.identifier.emailWang, W: wangwp@hku.hk-
dc.identifier.authorityWang, W=rp02227-
dc.identifier.doi10.1021/jacs.6b02435-
dc.identifier.hkuros700003529-
dc.identifier.volume138-
dc.identifier.issue19-
dc.identifier.spage6127-
dc.identifier.epage6130-
dc.identifier.isiWOS:000376331000010-
dc.publisher.placeUnited States-

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