Abstract
Oral sesame oil-based formulation facilitates the delivery of poorly water-soluble drug cannabidiol (CBD) to the lymphatic system and blood circulation. However, this natural oil-based formulation also leads to considerable variability in absorption of CBD. In this work, the performance of lipid-based formulations with the addition of medium-chain triglyceride (MCT) or surfactants to the sesame oil vehicle has been tested in vitro and in vivo using CBD as a model drug. The in vitro lipolysis has shown that addition of the MCT leads to a higher distribution of CBD into the micellar phase. Further addition of surfactants to MCT-containing formulations did not improve distribution of the drug into the micellar phase. In vivo, formulations containing MCT led to lower or similar concentrations of CBD in serum, lymph and MLNs, but with reduced variability. MCT improves the emulsification and micellar solubilization of CBD, but surfactants did not facilitate further the rate and extent of lipolysis. Even though addition of MCT reduces the variability, the in vivo performance for the extent of both lymphatic transport and systemic bioavailability remains superior with a pure natural oil vehicle.
Highlights
Introduction30% to 60% of new active drugs have poor aqueous solubility issues, and conventional formulations usually do not facilitate the absorption of these compounds from the gastrointestinal (GI) tract [1]
Sesame oil-based formulation has been previously reported to lead to substantial increase in bioavailability and intestinal lymphatic transport of CBD in rats, but with considerable variability
The medium-chain triglyceride (MCT) incorporated into sesame oil enhanced the micellar solubility of CBD in vitro, but surfactants used in this study may have reduced the lipolysis of triglycerides in comparison to other MCT-containing formulations
Summary
30% to 60% of new active drugs have poor aqueous solubility issues, and conventional formulations usually do not facilitate the absorption of these compounds from the gastrointestinal (GI) tract [1]. Lipid-based formulations have been proposed to facilitate the intraluminal solubility and systemic bioavailability of these poorly watersoluble compounds [1,2,3,4]. One of the most common lipidic core excipients used in various lipid-based formulations is different vegetable fats, for example sesame oil [5,6,7]. The main component in most natural vegetable oils is long-chain triglycerides (LCTs), which are digested in the intestinal lumen by lipases to generate free fatty acids and Pharmaceutics 2021, 13, 1349.
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