A New Generation of Nutra-ceuticals and Cosme-ceuticals Complexing lipophilic bioactives with γ-Cyclodextrin

Abstract

We previously reported the bioavailability enhancement of lipophilic Coenzyme Q10 (CoQ10) by complexing with γ-Cyclodextrin (γCD) in spite of poorly-soluble characteristics in water. We recently found the most plausible explanation mechanism which is due to the significant increase of water solubility of CoQ10 with the aid of sodium taurocholate (Na TCA) as a major component of bile acid in small intestine. By adding Na TCA into a water suspension of CoQ10-γCD complex, water soluble Na TCA-γCD complex is formed by the substitution of guest molecule from CoQ10 to Na TCA since Na TCA has higher association constant with γCD than CoQ10. Generally CoQ10 molecule agglutinates in water to form visible particles. But the dissociated CoQ10 from γCD cavity could be significantly solubilized in water captured in the midst of Na TCA micelle. This method could be applied for the other nutra-ceuticals like Curcumin and R-α-Lipoic acid. In the wake of the breakthrough projects using various nutra-ceutical-γCD complexes and Na TCA, we could also establish this new nanotech formulation system in personal care field by the combination of cosme-ceutical-γCD complexes with a cosmetic ingredient, dipotassium glycyrrhizate (GZK 2 ) which has high association constant as well as Na TCA.

Evaluation of Solubility Characteristics of a Hybrid Complex of Components of Soy

“…CoQ10 can be released in solution from CoQ10/γCD inclusion complexes, and the released CoQ10 forms micelles with NaTC. 26 It has been speculated that DDZ/γCD and GST/γCD inclusion complexes dissolved in FaSSIF solution allow DDZ and GST to be incorporated into NaTC since NaTC is contained in FaSSIF solution. Inclusion complexes prepared for DDZ/βCD with coprecipitation using an organic solvent have been reported.…”

Solubility of Piperine and Its Inclusion Complexes in Biorelevant Media and Their Effect on Attenuating Mouse Ileum Contractions

“…Furthermore, guest drugs of the γCD inclusion complex can be easily encapsulated in taurocholic acid. 27 With CP (PP/αCD), the solubilized PP molecules were incorporated into the mixed micelles with αCD forming an inclusion complex with lecithin that induced the supersaturation phenomenon. With CP (PP/γCD), PP was encapsulated in taurocholic acid that helped to maintain solubility.…”

Micelle Formation of Coenzyme Q10 with Dipotassium Glycyrrhizate Using Inclusion Complex of Coenzyme Q10 with γ-Cyclodextrin

“…In Figure 3, the slope of the regression line below the plateau indicated the overall equilibrium constant in eqs 3 and 4. The overall equilibrium constant K is the product of (8) where Y is defined as the product of the 0.4th power of the CoQ 10 concentration in the micelle of CoQ 10 with GZK 2 and the γ-CD concentration in the water-soluble inclusion complex GZK 2 with γ-CD. The concentration of free GZK 2 is shown in Figure 4.…”