Self-nanoemulsifying particles of coenzyme Q₁₀ with improved nutraceutical potential

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• 作者：Satomi Onoue^a ; ^{onoue@u-shizuoka-ken.ac.jp" class="auth_mail" title="E-mail the corresponding author} ; Atushi Uchida^a ; Tatsuya Nakamura^a ; Kazuki Kuriyama^a ; Junya Hatanaka^b ; ¹ ; Toshiyuki Tanaka^c ; Hiroyuki Miyoshi^c ; Yoshiki Seto^a ; Shizuo Yamada^a
• 关键词：ALT ; alanine aminotransferase ; ANOVA ; analysis of variance ; AST ; aspartate aminotransferase ; β-NADH ; nicotinamide adenine dinucleotide ; CCl4 ; carbon tetrachloride ; Cmax ; maximum concentration ; CoQ10 ; coenzyme Q10 ; DLS ; dynamic light scattering ; DSC ; differential scanning calorimetry ; GI ; gastrointestinal ; HPC ; hydroxypropyl cellulose ; HPLC ; high-performance liquid chromatography ; MCT ; medium-chain triglyceride ; PXRD ; powder X-ray diffraction ; RH ; relative humidity ; SEDDS ; self-emulsified drug de
• 刊名：PharmaNutrition
• 出版年：2015
• 出版时间：October 2015
• 年：2015
• 卷：3
• 期：4
• 页码：153-159
• 全文大小：1673 K

文摘

The major purpose of the present study was to clarify the physicochemical and nutraceutical properties of self-nanoemulsifying particles of coenzyme Q₁₀ (CoQ₁₀/SNEP). Nanoemulsion preconcentrate, containing CoQ₁₀, medium-chain triglyceride, sucrose ester of fatty acid, and hydroxypropyl cellulose, was spray-dried to produce the CoQ₁₀/SNEP. The CoQ₁₀/SNEP was stored at 40 °C with or without 75% relative humidity (RH) for 4 weeks, and its physicochemical properties were characterized in terms of appearance, crystallinity, thermal behavior, dissolution, and self-nanoemulsifying potency. The hepatoprotective effects of CoQ₁₀ and the CoQ₁₀/SNEP were also assessed in a rat model of acute liver injury. Under accelerated conditions (40 °C/75% RH), the CoQ₁₀/SNEP was found to be physicochemically unstable, as evidenced by partial deliquescence, slight degradation, reduced dissolution rate, and larger particle size of resultant micelles. In contrast, there appeared to be no significant transition in physicochemical properties of the CoQ₁₀/SNEP after 4 weeks of storage at 40 °C. The outcomes from stability testing suggested that moisture protection would be needed for long-term storage of the CoQ₁₀/SNEP. In a rat model of acute liver injury, pretreatment with CoQ₁₀/SNEP (100 mg CoQ₁₀/kg, twice) resulted in marked attenuation of hepatic damage as evidenced by decreases of alanine aminotransferase and aspartate aminotransferase, surrogate biomarkers for hepatic injury, by 96% and 82%, respectively, although crystalline CoQ₁₀ was less effective. From these findings, the self-nanoemulsifying approach might be efficacious for improving the nutraceutical values of CoQ₁₀.