Abstract
Therapeutic applications of coenzyme Q10 (CoQ10) are greatly limited by its lack of solubility in aqueous media. In this study, polyethylene glycol monostearate (stPEG) was used to construct micelles containing CoQ10 as a new formulation. The micellar formulations (stPEG/CoQ10) were prepared using five types of stPEG with 10, 25, 40, 55, and 140 PEG repeat units, respectively. The micellar preparation was simple, consisting of only stPEG and CoQ10. Next, we compared the physical properties and blood circulation of these micelles. The CoQ10 load of this formulation was approximately 15 w/w%. Based on the dynamic light scattering method, the average molecular size of the stPEG/CoQ10 micelles was approximately 15 to 60 nm. The zeta potentials of these micelles were approximately −10 to −25 mV. The micelles using stPEG25, 40, and 55 demonstrated high solubility in water. Furthermore, these micelles had in vitro antioxidant activity. On comparing the blood circulation of micelles using stPEG25, 40, 55, and 140, micelles using stPEG55 had a significantly higher circulation in blood. The stPEG55/CoQ10 micelle demonstrated a protective effect against acetaminophen-induced liver injury in mice. In conclusion, these data indicate that the intravenous administration of the stPEG/CoQ10 micellar aqueous formulation is of great value against oxidant stress.
Highlights
Coenzyme Q10 (CoQ10) has been reported to have a wide range of positive therapeutic effects on human health [1]
CoQ10 was purchased from the Tokyo Chemical Industry (Tokyo, Japan). stPEG10, stPEG25, stPEG40, and stPEG55 were purchased from FUJIFILM Wako Pure Chemical (Osaka, Japan). stPEG140 was kindly supplied by Kao Co., Ltd. (Tokyo, Japan)
Using stPEGs as the amphiphilic block polymer and preparing stPEG solutions at an excessively maximum fluorescence emission wavelength shifts toward blue when the PNA molecule moves from higher concentration than Critical Micelle Concentrations (CMC), we obtained micelle formulations with significantly improved CoQ10 an aqueous tofor a stPEG10 hydrophobic one
Summary
Coenzyme Q10 (CoQ10) has been reported to have a wide range of positive therapeutic effects on human health [1]. It is a powerful endogenous antioxidant, reducing the potential negative effects of free radicals [2,3]. Its structure consists of a benzoquinone ring prenylated with an isoprenoid chain. Because of the long side chain of the molecule consisting of 10 isoprenoid units, CoQ10 is extremely lipophilic and practically insoluble in water. The oral bioavailability of CoQ10 is generally very low and was related to the dissolution rate of the formulation [7]. Intravenous administration systems are important because of this low oral bioavailability
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