A liposome-micelle-hybrid (LMH) oral delivery system for poorly water-soluble drugs: Enhancing solubilisation and intestinal transport.

Romana, B; Hassan, MM; Sonvico, F; Garrastazu Pereira, G; Mason, AF; Thordarson, P; Bremmell, KE; Barnes, TJ; Prestidge, CA

A liposome-micelle-hybrid (LMH) oral delivery system for poorly water-soluble drugs: Enhancing solubilisation and intestinal transport.

Romana, B Hassan, MM Sonvico, F

Garrastazu Pereira, G Mason, AF Thordarson, P Bremmell, KE Barnes, TJ Prestidge, CA

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Publisher:: Elsevier BV
Publication Type:: Journal Article
Citation:: European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 2020, 154, pp. 338-347
Issue Date:: 2020-09

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Field	Value	Language
dc.contributor.author	Romana, B
dc.contributor.author	Hassan, MM
dc.contributor.author	Sonvico, F https://orcid.org/0000-0001-7372-1456
dc.contributor.author	Garrastazu Pereira, G
dc.contributor.author	Mason, AF
dc.contributor.author	Thordarson, P
dc.contributor.author	Bremmell, KE
dc.contributor.author	Barnes, TJ
dc.contributor.author	Prestidge, CA
dc.date.accessioned	2021-06-21T00:47:51Z
dc.date.available	2021-06-21T00:47:51Z
dc.date.issued	2020-09
dc.identifier.citation	European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, 2020, 154, pp. 338-347
dc.identifier.issn	0939-6411
dc.identifier.issn	1873-3441
dc.identifier.uri	http://hdl.handle.net/10453/149663
dc.description.abstract	A novel liposome-micelle-hybrid (LMH) carrier system was developed as a superior oral drug delivery platform compared to conventional liposome or micelle formulations. The optimal LMH system was engineered by encapsulating TPGS micelles in the aqueous core of liposomes and its efficacy for oral delivery was demonstrated using lovastatin (LOV) as a model poorly soluble drug with P-gp (permeability glycoprotein) limited intestinal absorption. LOV-LMH was characterised as unilamellar, spherical vesicles encapsulating micellar structures within the interior aqueous core and showing an average diameter below 200 nm. LMH demonstrated enhanced drug loading, water apparent solubility and extended/controlled release of LOV compared to conventional liposomes and micelles. LMH exhibited enhanced LOV absorption and transportation in a Caco-2 cell monolayer model of the intestine by inhibiting the P-gp transporter system compared to free LOV. The LMH system is a promising novel oral delivery approach for enhancing bioavailability of poorly water-soluble drugs, especially those presenting P-gp effluxes limited absorption.
dc.format	Print-Electronic
dc.language	eng
dc.publisher	Elsevier BV
dc.relation.ispartof	European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
dc.relation.isbasedon	10.1016/j.ejpb.2020.07.022
dc.rights	info:eu-repo/semantics/closedAccess
dc.subject	1115 Pharmacology and Pharmaceutical Sciences
dc.subject.classification	Pharmacology & Pharmacy
dc.subject.mesh	Caco-2 Cells
dc.subject.mesh	Humans
dc.subject.mesh	Water
dc.subject.mesh	Lovastatin
dc.subject.mesh	Liposomes
dc.subject.mesh	Hydroxymethylglutaryl-CoA Reductase Inhibitors
dc.subject.mesh	Drug Delivery Systems
dc.subject.mesh	Administration, Oral
dc.subject.mesh	Cell Survival
dc.subject.mesh	Intestinal Absorption
dc.subject.mesh	Micelles
dc.subject.mesh	Solubility
dc.title	A liposome-micelle-hybrid (LMH) oral delivery system for poorly water-soluble drugs: Enhancing solubilisation and intestinal transport.
dc.type	Journal Article
utslib.citation.volume	154
utslib.for	1115 Pharmacology and Pharmaceutical Sciences
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Faculty of Health
pubs.organisational-group	/University of Technology Sydney/Faculty of Health/Graduate School of Health
pubs.organisational-group	/University of Technology Sydney/Faculty of Health/Graduate School of Health/GSH.Pharmacy
utslib.copyright.status	closed_access	*
dc.date.updated	2021-06-21T00:47:50Z
pubs.publication-status	Published
pubs.volume	154

Abstract:

A novel liposome-micelle-hybrid (LMH) carrier system was developed as a superior oral drug delivery platform compared to conventional liposome or micelle formulations. The optimal LMH system was engineered by encapsulating TPGS micelles in the aqueous core of liposomes and its efficacy for oral delivery was demonstrated using lovastatin (LOV) as a model poorly soluble drug with P-gp (permeability glycoprotein) limited intestinal absorption. LOV-LMH was characterised as unilamellar, spherical vesicles encapsulating micellar structures within the interior aqueous core and showing an average diameter below 200 nm. LMH demonstrated enhanced drug loading, water apparent solubility and extended/controlled release of LOV compared to conventional liposomes and micelles. LMH exhibited enhanced LOV absorption and transportation in a Caco-2 cell monolayer model of the intestine by inhibiting the P-gp transporter system compared to free LOV. The LMH system is a promising novel oral delivery approach for enhancing bioavailability of poorly water-soluble drugs, especially those presenting P-gp effluxes limited absorption.

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http://hdl.handle.net/10453/149663