Phytantriol and glyceryl monooleate cubic liquid crystalline phases as sustained-release oral drug delivery systems for poorly water-soluble drugs II. In-vivo evaluation

The Journal of Pharmacy and Pharmacology
Tri-Hung NguyenBen J Boyd

Abstract

Lipid-based liquid crystals formed from phytantriol (PHY) and glyceryl monooleate (GMO) retain their cubic-phase structure on dilution in physiologically relevant simulated gastrointestinal media, suggesting their potential application as sustained-release drug-delivery systems for poorly water-soluble drugs. In this study the potential of PHY and GMO to serve as sustained-release lipid vehicles for a model poorly-water-soluble drug, cinnarizine, was assessed and compared to that of an aqueous suspension formulation. Small-angle X-ray scattering was used to confirm the nanostructure of the liquid-crystalline matrix in the presence of the selected model drug, cinnarizine. Oral bioavailability studies were conducted in rats, and disposition of lipid and drug in segments of the gastrointestinal tract was determined over time. Differences in the digestibility and stability of formulations under digestion conditions were investigated using an in-vitro lipolysis model. The oral bioavailability of cinnarizine using the PHY formulation was 41%, compared to 19% for the GMO formulation and 6% for an aqueous suspension. The PHY formulation provided a T(max) for cinnarizine of 33 h, with absorption apparent up to 55 h after administration....Continue Reading

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Citations

Mar 12, 2015·Journal of Exposure Science & Environmental Epidemiology·Lien TaevernierBart De Spiegeleer
Oct 13, 2011·The Journal of Pharmacy and Pharmacology·Shinri TakasugaMine Kinoshita
Apr 17, 2013·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·Mehmet Nail NasirMagali Deleu
Aug 2, 2017·Molecular Pharmaceutics·Saiman ZhangMing Chen

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