| The main active ingredient of traditional Chinese medicine licorice, Glycyrrhetinic acid has significant anti-inflammatory, antibacterial, antiviral, protect liver cells and immune regulation, and other aspects of pharmacological activity [1-3], for local inflammation, such as phlebitis have better results. But the effect of its oral and intramuscular route is poor. Therefore, the development of transdermal drug delivery formulations significant.The ethosomes is a vesicle structure of the new transdermal drug delivery carrier. Because of its high entrapment efficiency, good stability, high membrane deformability of advantages, and can carry the drug to reach the deeper skin[4-6]. But its clinical application for the liquid preparations often inconvenience and be limited use. This experiment made ethosomes into hydrogel patch by secondary preparation, and glycyrrhetinic acid ethosomes equipment and prescription screening, prescription screening and optimization of the hydrogel patch, quality standards, in vitro release experiments pharmacodynamic and animal experiments in order to increase the drug encapsulation efficiency and cumulative, improving glycyrrhetinic acid anti-inflammatory efficacy.Using injection prepared by glycyrrhetinic acid ethosome, HPLC method for the determination of glycyrrhetinic acid ethosomes content and the encapsulation efficiency of ethosome, and examines the ethosome preparation excipients on the encapsulation efficiency impact of the law, by orthogonal experiment to determine the optimal prescription of glycyrrhetinic acid ethosome plasmid.With JEM-2000EX transmission electron microscope observation of glycyrrhetinic acid ethosome plasmid form, laser dynamic scattering instrument Zetasizernanos ZEN3600determination ethosomes size distribution and Zeta potential. Kept for60days, at4℃,25℃,40℃for ethosomes avoid light. Investigated at different times under the acid value (AV) and peroxide value (POV) variation, evaluation of the chemical stability of the glycyrrhetinic acid and alcohol plasmid stability. The results showed that ethosome plasmids into ellipsoidal or spherical, the average encapsulation efficiency was (7563±86)%, with an average particle size (106.2±2054) nm. The Zata potential (-41.3±2.8) mV; the ethosomes stored at low temperature4℃, the acid value and peroxide value have no significant changes and ethosomes is stable performance in the system.Tack force (T), holding the stick force (C), the peel force (P) as an index, the initial of glycyrrhetinic acid ethosome hydrogel patch optimized prescription by a single factor and orthogonal experiments, and then verified by repeated experiments and found that the plasmid of glycyrrhetinic acid and alcohol hydrogel patch prescription best ratio:0.30%of aluminum hydroxide,3.25%sodium polyacrylate,33.00%glycerol,3.50%povidone K-120,0.30%citric acid,0.60%glycyrrhetinic acid ethosomes53.65%distilled water. Place the temperature is25℃, stirring time is15min, tartaric acid add3times.Through to the glycyrrhetinic acid ethosome and its hydrogel patches in vitro release experiments investigation and its hydrogel patches in vitro of drug release behavior and law; transdermal absorption test with the modified Franz diffusion cells.comparison of glycyrrhetinic acid ethosomes hydrogel patches, gel patches of glycyrrhetinic acid water and glycyrrhetinic acid+Space ethosomes hydrogel patch, glycyrrhetinic acid (32%), alcoholaqueous solution of percutaneous cumulative penetration and penetration rate, Investigation of glycyrrhetinic acid ethosome hydrogel patch in vitro geological laws through skin.The results showed that glycyrrhetinic acid ethosomes hydrogel patch compared with the other three agents, can significantly increase the glycyrrhetinic acid of amount through skin (P<0.01).the experiments establish rabbit ear vein injury animal model by fluorouracil (5-UF),The histopathological producer and HE staining,oberserved the vessel wall of inflammatory cells vascular wall damage, microcirculation, and peritubular vascular tissue edema incidence under the microscopeinfiltration. Fisher’s exact test between any two group’s differences was significant.(P<0.05) Comparative Study the GA ethosomes hydrogel patch, wishful golden powder, GA hydrogel patch, blank group topical effect of the prevention of fluorouracil chemotherapy phlebitis. |
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