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Antioxidant Activity Of Coenzyme Q10 Nanocrystal And Its Effects On Skin Photoaging

Posted on:2011-10-19Degree:MasterType:Thesis
Country:ChinaCandidate:F J WangFull Text:PDF
GTID:2154360308971292Subject:Pharmacognosy
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Coenzyme Q10 is mitochondrial energy source and natural antioxidants in organism, having an important physiological role and clinical value. However, the coenzyme Q10 is a fat-soluble substances, with poor human absorption, low bioavailability and poor stability constituting a bottleneck in its formulation and application.In recent years, nanosuspension is a new nano-drug delivery system, can increase drug solubility, stability and bioavailability,but also achieve targeted drug delivery, controlled drug release, increase drug stability, reduce side effects, reduce the dosage and so on.Therefore, the aims of the study is to assess coenzyme Q10 suspension containing nano-medicine system from aspects of quality control and the pharmacodynamic. First of all, investigated preparation for the characterization of nano suspensions the quality of coenzyme Q10; we did pharmacokinetics experimental in rats to investigate in vivo absorption and metabolism; to investigate effect of oral coenzyme Q10 nano-suspension on antioxidative enzyme system,we detect the SOD, CAT, GSH-Px activity and MDA content; carried out in vitro rat skin permeation tests, to investigate the penetration ability of coenzyme Q10 nano-suspension, and the establishment of UVB light skin aging model to study nanosuspension coenzyme Q10 to see skin photoaging ability. Thus, for the clinical application of coenzyme Q10, health products, food and cosmetics fields widely used, open up good prospects. The results of the research topics are as follows:1,Stability of quality assessment and quality evaluation of coenzyme Q10 and stability of nano-suspension Transmission electron microscopy shows that coenzyme Q10 as spherical particles, diameter of 200±50nm, good dispersion and stability of the system. X-ray diffraction and DSC show amorphous form of Coenzyme Q10 present in the nano-suspension. Nano Suspensions of coenzyme Q10,freeze-dried powder in saturated solubility and dissolution rate of coenzyme Q are much higher than the original drug, nanoparticle size could be reduced, increasing the particle surface area, to further increase its solubility;2,Pharmacokinetics Tmax (3.3±0.23 h) was significantly smaller than the original drug coenzyme Q10 Tmax values (P<0.05), showed that coenzyme Q10 by the nano-absorption in rats after the accelerated time to peak early. Nanocrystalline drug Cmax (3.23±0.09μg/ mL) was significantly higher than the original drug Cmax values (P<0.05), AUC=78±2.49μg/(mL·h) value is also larger than the original drug AUC values that coenzyme Q10 in rats after by the ultra fine powder to achieve a higher plasma concentration, bioavailability body also increased significantly 1 times the original drug;3,Antioxidant activity in mouse Compared to ordinary powder group and positive control group had significantly higher ultrafine plasma SOD, CAT and GSH-Px activity and liver SOD activity (P<0.05),and significantly reduced plasma and liver MDA content in mice (P<0.05), dose-dependent manner, coenzyme Q10 on the ultrastructure of mouse liver and kidney without any pathological effects of the new formulation is safe and reliable;4,UVB Skin aging and penetration ability The studies about skin permeation in vitro showed that coenzyme Q10 nano-suspension has good penetration capacity, steady-state penetration rate of Js was 17.54±1.10, is a commercial product is marketed product 12 times. UVB skin aging in the experiment, compared with ordinary powder Li Jiafen positive control group and U.S.group had significantly higher ultrafine plasma and skin in the SOD, CAT and GSH-Px activity (P<0.05),and significantly reduced in mice MDA content in plasma and skin (P<0.05), increased content of hydroxyproline in the skin.In summary, the coenzyme Q10 nanosuspension is coenzyme Q10 amorphous dispersion, has high drug loading, and particle shape are mostly spherical.well dispersed system with particle size of about 200±50 nm, and has good stability. Coenzyme Q10 nanosuspension increases drug solubility, stability and bioavailability, and increased efficacy, reduces side effects and the dosage and so on.
Keywords/Search Tags:coenzyme Q10, nanosuspension, pharmacokinetics, antioxidant activity, skin penetration, photoaging
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