Inclusion of Medium-Chain Triglyceride in Lipid-Based Formulation of Cannabidiol Facilitates Micellar Solubilization In Vitro, but In Vivo Performance Remains Superior with Pure Sesame Oil Vehicle

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.

INTERACTION OF 3-HYDROXY PYRIDINE AND SURFACTANT MICELLES: A FLUORESCENCE STUDIES

Objective: Micellar solubilization is a powerful alternative for dissolving hydrophobic compound in aqueous environment. 3-hydroxy pyridine (3- HP) derivatives are the potential endogenous photosensitizers. 3-HP derivatives show protective effect in clinical extreme condition such as hypoxia, hyperthermia, hypokinesia. Micellization of 3-HP followed by solubilization would catalyze its pharmaceutical activities which may serve better results in medicinal and analytical fields. Methods: Fluorescence and absorption spectroscopy techniques are used to monitor the micellar solubilization studies of 3-HP. Solubilization studies of 3-HP with various anionic, cationic and nonionic surfactants have been performed in aqueous medium around 23–25°C temperature. The solubilization action of the surfactant has also been determined by theoretical calculated spectral parameters such as empirical fluorescence coefficient, quantum yield, stokes, shift and molar absorption coefficient. Results: 3-HP shows fluorescence excitation peak at 315 nm and emission peak at 390 nm respectively while the absorbance of 3-HP has been found to be maximum at 305 nm. The fluorescence as well as the theoretically calculated spectral data has been used to characterize the hetero environment of the micelles in terms of their polarity, probe solubilization site and critical micelle concentration. Conclusion: This article briefly discusses the importance of surfactants in biological system model as well as the use of micelles in pharmacy as an important tool that finds numerous applications.

Solubilization Methods for Paclitaxel and Docetaxel: An Overview

Cancer is still a serious disease with high incidence over the past decades. Many anticancer drugs are discovered and used to treat cancer, among them, taxanes such as paclitaxel and docetaxel have high lipophilicity and low aqueous solubility which is further magnified considering the strong need for administering them by intravenous infusion. Currently, the poor water-solubility of taxanes is improved by prodrug formation, conjugation, inclusion complexation, micellar solubilization and liposome-based formulations. Recent achievement for solubilization of taxanes are reviewed and critically discussed regarding their pharmaceutical and chemical applications.

Towards Rational Biosurfactant Design—Predicting Solubilization in Rhamnolipid Solutions

The efficiency of micellar solubilization is dictated inter alia by the properties of the solubilizate, the type of surfactant, and environmental conditions of the process. We, therefore, hypothesized that using the descriptors of the aforementioned features we can predict the solubilization efficiency, expressed as molar solubilization ratio (MSR). In other words, we aimed at creating a model to find the optimal surfactant and environmental conditions in order to solubilize the substance of interest (oil, drug, etc.). We focused specifically on the solubilization in biosurfactant solutions. We collected data from literature covering the last 38 years and supplemented them with our experimental data for different biosurfactant preparations. Evolutionary algorithm (EA) and kernel support vector machines (KSVM) were used to create predictive relationships. The descriptors of biosurfactant (logPBS, measure of purity), solubilizate (logPsol, molecular volume), and descriptors of conditions of the measurement (T and pH) were used for modelling. We have shown that the MSR can be successfully predicted using EAs, with a mean R2val of 0.773 ± 0.052. The parameters influencing the solubilization efficiency were ranked upon their significance. This represents the first attempt in literature to predict the MSR with the MSR calculator delivered as a result of our research.

Cooperativity in micellar solubilization

Enhanced surfactant association by solutes drives cooperative solubilization according to the universal statistical thermodynamic theory.