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Objective To explore the pharmacokinetic properties of curcumin nano emulsion and its pharmacodynamic effects on hyperlipidemia in rats. Methods The method for determination of curcumin was established by HPLC-MS. The pharmacokinetics characteristics of curcumin nano emulsion oral administration system were investigated. SD rats were used as model animals to establish hyperlipidemia animal models, and the pharmacodynamic effects of curcumin nano emulsion on hyperlipidemia induced by high fat diet was preliminarily investigated. Results The results of pharmacokinetic studies in vivo showed that the relative bioavailability of curcumin nano emulsion was 313.47% with bulk drug group as the reference preparation. The relative bioavailability of curcumin nano emulsion was 279.52 % with tablets as reference preparation. Cmax of curcumin nano emulsion group was 201.48 % of that of bulk drug group and 193.02 % of that of tablet group, and had higher MRT value (183.52 % of that of bulk drug group and 154.21 % of that of tablet group) than bulk drug group and tablet group. Pharmacodynamics research results showed that curcumin nano emulsion oral administration system could significantly reduce the levels of triglyceride and LDL-c in serum of model rats, and relieve liver lipid deposition and liver injury caused by high-fat diet in model animals. Conclusion The oral administration system of curcumin nano emulsion could effectively improve the bioavailability of curcumin, which has a good hypolipidemic effect. It also could control the weight gain of hyperlipidemia rats and improve the changes of liver coefficient caused by lipid metabolism disorder.
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Objective: To study the relationship between the drug form of curcumin self-nano-emulsion (Cur-SNEDDS) after being dispersed in artificial gastrointestinal fluid and intestinal absorption in rats. Methods: The change trend of curcumin concentration-time curve was used to express the change of precipitation growth. The content and existing form of precipitation were studied by polarized light microscope (PLMC), HPLC, UV full-wavelength (UV) scanning, X-ray powder diffraction (XRD), differential scanning calorimeter (DSC), infrared spectrum (FT-IR), Raman spectrum and nuclear magnetic resonance hydrogen spectrum (1H-NMR). At the same time, the rat valgus intestinal sac model was used to investigate the effect of SNEDDS on the apparent permeability coefficient (Papp) of curcumin. Results: The content of curcumin in the precipitation produced by Cur-SNEDDS dispersion was about 95% of that of curcumin API, and the chemical structure did not change, but the crystal form changed, resulting in amorphous precipitation. Curcumin intermolecular interaction occurred in the dispersion system, and hydrogen bonds were formed. Compared with curcumin, Cur-SNEDDS significantly increased the release rate and degree of curcumin in vitro, and enhanced the absorption of curcumin in duodenum, jejunum, ileum and colon, and the Papp value increased by 6.22, 12.97, 25.71 and 36.75 times, respectively. Conclusion: After Cur-SNEDDS dispersion, the crystal structure of curcumin is changed, which exists in free, amorphous and crystal form, so as to significantly improve the in vitro release and intestinal absorption of curcumin.
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Objective@#To evaluate the immunogenicity of split influenza H1N1 vaccine formulated with an oil-in-water nano-emulsion adjuvant in aged mice and young mice.@*Methods@#A nano-emulsion adjuvant formulated split influenza H1N1 vaccine was used to immunize aged and young mice through intramuscular injection. Each mouse was immunized with 0.012 μg of hemagglutinin (HA) twice with an interval of 28 d. Hemagglutination inhibition (HI) titers in serum were measured 27 d after first immunization. Serum HI, IgG1 and IgG2a titers were detected 14 d after the last immunization. No adjuvant-formulated vaccine and normal saline (NS) were used to set up control groups. Virus challenge test was carried out using 10 times the median lethal dose (LD50) of A/Puerto Rico/8/34 (H1N1) strain two weeks after the last immunization and the protective effects were assessed through measuring the dynamic changes in body weight and survival rate.@*Results@#Higher levels of serum HI, IgG1 and IgG2a antibodies and higher HI antibody conversion rates were induced in the adjuvant groups, especially in the aged mice group, than in the control groups. Nano-emulsion adjuvant improved the immunogenicity of HA and mouse immunity to A/Puerto Rico/8/34 (H1N1).@*Conclusions@#Nano-emulsion adjuvant could enhance the immunogenicity of influenza antigens, especially in aged mice.
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Objective To establish an HPLC approach for determining the plasma drug concentration of evodiamine (EVO) in evodiamine novel nano emulsion (ENNE) in rats, and to investigate the pharmacokinetics and bioequivalence of ENNE in rats. Methods Twelve SD rats were evenly randomized into two groups andwere administered intragastrically with ENNE (containing EVO 100mg/kg) or EVO (100mg/kg). The plasma drug concentrations of EVO were measured at 5min,min, 15 min, 30 min, 45 min, 1 h, 2 h, 5 h, 8 h, 12 h, 24 h, 48 h and 72 h after administration of ENNE or EVO by HPLC. The chromatographic conditions were as following: the mobile phase was methanol and 0.1% of formic acid-water solution (66: 34, V/V), the flow rate was 1 mL/min, the injection volume was 100 μL, and the detection wavelength was 225 nm. The concentration-time curve was drawn by excel software, and the main pharmacokinetic parameters and bioequivalence were calculated by DAS 2. 1. 1 software. Results The established method was fast, accurate, and had good linear correlation. The AUCo-∞ of ENNE and EVO were (8 248. 88 ± 69. 92) μg • h • L-1 and (884. 82 ± 83. 52) μg • h • L-1, and the t1/2 of ENNE and EVO were (1. 70 ± 0. 60) h and (1. 05 ± 0. 45) h, respectively. The AUCo-∞ of ENNE was 9 times that of EVO, and the t1/2 of ENNE was 1. 62 times that of EVO. ENNE and EVO were not bioequivalent. Conclusion Bioavailability and absorption of ENNE are higher than EVO, and ENNE and EVO are not bioequivalent.
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Objective To study on whitening and anti -aging effect of ginseng saponin and its safety.Methods Whitening effect:using vitamin C as the control drug, the inhibition rate of tyrosinase was determined.Anti senescence effect: the aging model of D-was established, and the DPPH was applied to the skin of the rat's neck, and the drug was prepared by 2 times a day.Skin safety evaluation: the skin changes of the skin of the ginseng saponins were observed after the skin was given ginseng saponin and control drugs.Results When the concentration of ginsenoside was 7 mg/mL, the inhibition rate order was, the water solution of vitamin C >ginsenoside nano >ginsenoside aqueous solution ; In the aging model, the surface of the elastic fibers and the skin surface was parallel to the skin, but the elastic fibers were arranged in a more tortuous and non parallel to the skin;DPPH free radical scavenging effect order was, Vitamin C aqueous solution>ginsenoside nano>ginsenoside aqueous solution, and with the dosage of ginsenoside increasing, the efficiency of ginsenoside DPPH scavenging free radical increased significantly;Skin safety evaluation results showed that ginseng saponin nanometer milk smeared skin, no redness, irritation and other phenomena occured.Conclusion Ginseng saponin nanometer milk has obvious whitening effect, and can not cause damage to the skin, is safe and reliable.
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Background: Acne vulgaris is a very common skin disease with a significant detrimental effect on the quality of life of the patients. Aims: To assess the comparative efficacy and safety of a nano-emulsion gel formulation of adapalene and clindamycin combination with its conventional formulation in the treatment of acne vulgaris of the face. It was a prospective, randomized, open label, active-controlled, multicentric, clinical trial. Methods: Eligible patients suffering from acne vulgaris of the face were randomized to receive once-daily treatment with a nano-emulsion gel or conventional gel formulation of adapalene 0.1% and clindamycin (as phosphate) 1% combination for 12 weeks. Total, inflammatory and noninflammatory lesion counts, with grading of acne severity were carried out on a monthly basis. Safety assessments were done to determine the comparative local and systemic tolerability. Two-tailed significance testing was carried out with appropriate statistical tests, and P-values < 0.05 were considered as significant. Results: 209/212 patients enrolled in the study were eligible for efficacy and safety assessments in both nano-emulsion gel (118/119 patients) and conventional gel (91/93 patients) groups. Significantly better reductions in total (79.7% vs. 62.7%), inflammatory (88.7% vs. 71.4%) and noninflammatory (74.9% vs. 58.4%) lesions were reported with the nano-emulsion gel as compared to the conventional gel (P < 0.001 for all). Mean acne severity score also reduced significantly more with the nano-emulsion formulation (1.9 ± 0.9 vs. 1.4 ± 1.0; P < 0.001) than the comparator. Significantly lower incidence and lesser intensity of adverse events like local irritation (4.2% vs. 19.8%; P < 0.05) and erythema (0.8% vs. 9.9%; P < 0.05) were recorded with the nano-emulsion gel. Conclusions: The nano-emulsion gel formulation of adapalene and clindamycin combination appears to be more efficacious and better tolerated than the conventional formulation for the treatment of acne vulgaris in Indian patients. Further studies can elucidate the comparative treatment benefits of this nano-emulsion gel formulation.