Preparation and in vivo pharmacokinetic evaluation of stable microemulsion system of cholecalciferol

Abstract

The objectives of the study were to formulate stable oil-in-water microemulsion (ME) system of cholecalciferol, a lipophilic and unstable prohormone for bone health, and evaluate its pharmacokinetic profile in beagle dogs. ME system consisting of caprylic/capric triglyceride (Captex 355), propylene glycol esters of fatty acids (Capryol 90), and macrogol 15 hydroxystearate (Solutol HS15) was approximately 100 nm in size with polydispersity index < 0.3 and zeta potential of - 5 mV. Incorporation of the liable compound in the oil droplet markedly impeded its chemical degradation, maintaining drug content over 93% after 2 years storage under ambient condition (25 °C/60% RH). In an absorption study using beagle dogs (n = 6 per group), there were no significant (P > 0.05) differences in pharmacokinetic parameters between novel ME-based drink and conventional tablet dosage form. Therefore, novel ME-based drink could be used as a convenient way to provide cholecalciferol supplementation for patients with dysphagia.

Graphical Abstract

Keywords:

• Microemulsion
• cholecalciferol
• chemical stability
• oral absorption
• pharmacokinetics

Disclosure statement

The authors report no conflicts of interest in this work.

Additional information

Funding

This research was supported by a grant Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science, ICT & Future Planning (NRF-2016R1C1B1010687).