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Article: A Soluplus/Poloxamer 407-based self-nanoemulsifying drug delivery system for the weakly basic drug carvedilol to improve its bioavailability

TitleA Soluplus/Poloxamer 407-based self-nanoemulsifying drug delivery system for the weakly basic drug carvedilol to improve its bioavailability
Authors
KeywordsBioavailability
Carvedilol
Drug dissolution
pH-dependent solubility
Precipitation inhibitor
Issue Date2020
PublisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/nanomed
Citation
Nanomedicine: Nanotechnology, Biology and Medicine, 2020, v. 27, p. article no. 102199 How to Cite?
AbstractCarvedilol (CAR), a β-adrenoceptor and α1-receptor blocker, has pH-dependent solubility, which greatly limits its oral bioavailability. In this work, a precipitation inhibitor-based self-nanoemulsifying drug delivery system (PI-SNEDDS) was developed by employing Soluplus and Poloxamer 407 to improve drug dissolution and to inhibit drug precipitation in the gastrointestinal tract. In vitro phase distribution and in vivo dissolution studies indicated that PI-SNEDDS significantly increased drug content in the oil phase of the nanoemulsions in the stomach and greatly inhibited the subsequent precipitation of CAR in the intestine compared with the carvedilol self-nanoemulsifying drug delivery system (CAR SNEDDS) and the carvedilol tablets. Moreover, a 1.56-fold increase in the relative bioavailability of CAR was observed for the CAR PI-SNEDDS (397.41%) compared to a CAR SNEDDS (254.09%) with commercial capsules as a reference. Therefore, our developed PI-SNEDDS is a promising vehicle for improving the dissolution and bioavailability of poorly soluble drugs with pH-dependent solubility. © 2020 Elsevier Inc.
Persistent Identifierhttp://hdl.handle.net/10722/289622
ISSN
2019 Impact Factor: 5.182
2015 SCImago Journal Rankings: 1.886
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorHan, H-
dc.contributor.authorLi, Y-
dc.contributor.authorPeng, Z-
dc.contributor.authorLONG, K-
dc.contributor.authorZheng, C-
dc.contributor.authorWang, W-
dc.contributor.authorWebster, TJ-
dc.contributor.authorGe, L-
dc.date.accessioned2020-10-22T08:15:10Z-
dc.date.available2020-10-22T08:15:10Z-
dc.date.issued2020-
dc.identifier.citationNanomedicine: Nanotechnology, Biology and Medicine, 2020, v. 27, p. article no. 102199-
dc.identifier.issn1549-9634-
dc.identifier.urihttp://hdl.handle.net/10722/289622-
dc.description.abstractCarvedilol (CAR), a β-adrenoceptor and α1-receptor blocker, has pH-dependent solubility, which greatly limits its oral bioavailability. In this work, a precipitation inhibitor-based self-nanoemulsifying drug delivery system (PI-SNEDDS) was developed by employing Soluplus and Poloxamer 407 to improve drug dissolution and to inhibit drug precipitation in the gastrointestinal tract. In vitro phase distribution and in vivo dissolution studies indicated that PI-SNEDDS significantly increased drug content in the oil phase of the nanoemulsions in the stomach and greatly inhibited the subsequent precipitation of CAR in the intestine compared with the carvedilol self-nanoemulsifying drug delivery system (CAR SNEDDS) and the carvedilol tablets. Moreover, a 1.56-fold increase in the relative bioavailability of CAR was observed for the CAR PI-SNEDDS (397.41%) compared to a CAR SNEDDS (254.09%) with commercial capsules as a reference. Therefore, our developed PI-SNEDDS is a promising vehicle for improving the dissolution and bioavailability of poorly soluble drugs with pH-dependent solubility. © 2020 Elsevier Inc.-
dc.languageeng-
dc.publisherElsevier Inc. The Journal's web site is located at http://www.elsevier.com/locate/nanomed-
dc.relation.ispartofNanomedicine: Nanotechnology, Biology and Medicine-
dc.subjectBioavailability-
dc.subjectCarvedilol-
dc.subjectDrug dissolution-
dc.subjectpH-dependent solubility-
dc.subjectPrecipitation inhibitor-
dc.titleA Soluplus/Poloxamer 407-based self-nanoemulsifying drug delivery system for the weakly basic drug carvedilol to improve its bioavailability-
dc.typeArticle-
dc.identifier.emailWang, W: wangwp@hku.hk-
dc.identifier.authorityWang, W=rp02227-
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1016/j.nano.2020.102199-
dc.identifier.pmid32275957-
dc.identifier.scopuseid_2-s2.0-85084318277-
dc.identifier.hkuros315973-
dc.identifier.volume27-
dc.identifier.spagearticle no. 102199-
dc.identifier.epagearticle no. 102199-
dc.identifier.isiWOS:000549858200001-
dc.publisher.placeUnited States-
dc.identifier.issnl1549-9634-

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