Preparation and characterization of novel coenzyme Q10 nanoparticles engineered from microemulsion precursors
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The purpose of these studies was to prepare and characterize nanoparticles into which Coenzyme Q10 (CoQ10) had been incorporated (CoQ10-NPs) using a simple and potentially scalable method. CoQ10-NPs were prepared by cooling warm microemulsion precursors composed of emulsifying wax, CoQ10, Brij 78, and/or Tween 20. The nanoparticles were lyophilized, and the stability of CoQ10-NPs in both lyophilized form and aqueous suspension was monitored over 7 days. The release of CoQ10 from the nanoparticles was investigated at 37°C. Finally, an in vitro study of the uptake of CoQ10-NPs by mouse macrophage, J774A.1, was completed. The incorporation efficiency of CoQ10 was approximately 74%±5%. Differential Scanning Calorimetry (DSC) showed that the nanoparticle was not a physical mixture of its individual components. The size of the nanoparticles increased over time if stored in aqueous suspension. However, enhanced stability was observed when the nanoparticles were stored at 4°C. Storage in lyophilized form demonstrated the highest stability. The in vitro release profile of CoQ10 from the nanoparticles showed an initial period of rapid release in the first 9 hours followed by a period of slower and extended release. The uptake of CoQ10-NPs by the J774A.1 cells was over 4-fold higher than that of the CoQ10-free nanoparticles (P<.05). In conclusion, CoQ10-NPs with potential application for oral CoQ10 delivery were engineered readily from microemulsion precursors.
KeywordsCoenzyme Q10 nanoparticles microemulsion stability cell uptake
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- 2.Mortensen SA. Perspectives on therapy of cardiovascular diseases with coenzyme Q10 (ubiquin one). Clin Investig. 1993;71(suppl 8):S116-S123.Google Scholar
- 3.Casey AC, Bliznakov EG. Effect and structure-activity relationship of coenzymes Q on the phagocytic rate of rats. Chem Biol Interact. 1972;16:1504–1510.Google Scholar
- 5.Greenberg S, Frishman WH. Coenzyme Q10: a new drug for cardiovascular disease. J Clin Pharmacol. 1990;30:590–608.Google Scholar
- 6.Kishi H, Kanamori N, Niraoka E, Okamato T, Kishi T. Metabolism of exogenous coenzyme Q10 in vivo and bioavailability of coenzyme Q10 preparations in Japan. In: Folkers K, Yamamura Y, eds. Biomedical and Clinical Aspects of Coenzyme Q. Vol 4. Amsterdam: Elsevier Science; 1984: 131–142.Google Scholar
- 9.Lutka A, Pawlaczyk J. Inclusion complexation of coenzyme Q10 with cyclodextrins. Acta Pol Pharm. 1995;52:379–386.Google Scholar
- 22.Hsu C-H, Cui Z, Jay M. Nanoparticles engineered from microemulsion precursors for coenzyme Q10 (CoQ10) delivery: preparation and characterization [abstract]. AAPS Pharm Sci. 2002;4(4):W5120.Google Scholar
- 24.Nazzal S, Zaghloul AA, Reddy IK, Khan MA. Analysis of ubidecarenone (CoQ10) aqueous simple using reversed phase liquid chromatography. Pharmazie. 2001;56:394–396.Google Scholar
- 26.Martin A, Swarbrick J, Cammarata A. Physical Pharmacy: Physical Chemical Principles in the Pharmaceutical Sciences. 3rd ed. Philadelphia, PA: Lea & Febiger, 1983:452–454.Google Scholar
- 30.Ford AW, Dawson PJ. The effect of carbohydrate additives in the freeze-drying of alkaline phosphatase. J Pharm Pharmacol. 1993;45:86–93.Google Scholar
- 32.Saiki I, Tokushima Y, Nishimura K, Azuma I. Macrophage activation with ubiquinones and their related compounds in mice. Int J Vitam Nutr Res. 1983;53:312–320.Google Scholar