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

[Display omitted] 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 effi...

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Bibliographic Details
Published in:European journal of pharmaceutics and biopharmaceutics 2020-09, Vol.154, p.338-347
Main Authors: Romana, Bilquis, Hassan, Md. Musfizur, Sonvico, Fabio, Garrastazu Pereira, Gabriela, Mason, Alex F., Thordarson, Pall, Bremmell, Kristen E., Barnes, Timothy J., Prestidge, Clive A.
Format: Article
Language:English
Subjects:
Bioavailability
Caco-2 cells
Liposomes
LMH
Lovastatin
Micelles
P-gp
Permeability
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Summary:[Display omitted] 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.
ISSN:0939-6411
1873-3441
DOI:10.1016/j.ejpb.2020.07.022