Geza Jakab, Istvan Antal
Department of Pharmaceutics, Semmelweis University, Budapest
Introduction: Self-emulsifying drug delivery systems (SEDDS) are isotropic mixtures of oil, surfactant, co-surfactant and the lipophilic compound, which are spontaneously form oil-in-water (o/w) emulsions upon mild agitation followed by dilution in gastro-intestinal fluids. Baicalin is a flavone glycoside, extracted from the roots of Scutellaria baicalensis Georgi. It was shown, that the poorly water soluble and poorly permeable polyphenolic flavonoid has remarkable pharmacological effects including antioxidant, antimicrobial and anti-tumor actions. Baicalin belongs Class IV. according to the Biopharmaceutical Classification System (BCS).
Aims: The aim of the study was to investigate the thermodynamic solubility of baicalin in different types of oils, sufactants and co-surfactants. Optimising the ideal oil/surfactant/co-surfactant ratios to achive minimal droplet sizes and stabile nanoemulsions. Transforming the best precontentrate to solid carrier, and after drying, preparation of pellets by extrusion-spheronization method. Reconstitution the droplet size and dissolution profiles in different pH dissolution medias.
Method: Our methods were followings: thermodynamic solubility analysis; emulsification efficacy screening; construction of ternary phase diagram; central composite design; droplet size, Zeta-potential, turbidity, stability measurements; AFM and SEM imaging; FT-IR, Raman spectroscopy; DSC; In-process control analysis; dissolution and reconstitution study.
Results: Physical characterizations of matrix pellets were performed and all of the investigated parameters have met the Ph. Eur. 9. requirements. Reconstitution from the solid carrier was succesfull in both different dissolution medias, nanoemulsion formulation of baicalin significantly improved its dissolution rate. Droplet size after dispergation of preconcentrate was highly desirable with 55.15 ± 0.3166 nm, the Zeta-potential was -22.3 ± 1.44 mV, which is also acceptable.
Conclusion: The low aqueous solubility of baicalin can be improved by SEDDS, and the preconcentrate could be effectively adsorbed to solid carriers.
Doctoral School: Pharmaceutical Sciences
Program: Modern Trends in Pharmaceutical Scientific Research
Supervisor: Dr. Istvan Antal
E-mail address: email@example.com