Construction And Bacteriostasis Of Garlic Oil Self-microemulsifying Drug Delivery System

Garlic oil is a volatile oil extracted from garlic bulbs,which has the functions of anti-bacterial and anti-inflammatory,anti-oxidation,lowering blood sugar,lowering blood lipid,preventing cancer,protecting liver and enhancing immunity.It is widely used in medicine,functional food and agriculture.Garlic oil has complex functional components,unstability and high storage cost,which limits the development and application.In this thesis,garlic oil was prepared into garlic oil self-microemulsifying system(GO-SMEDDS),and its quality was evaluated and its bacteriostasis was studied.The main conclusions of this paper are as follows:1.Preparation of GO-SMEDDS.Through raw materials intermiscibility investigation and pseudo ternary phase diagram drawing,filter the liquid GO-SMEDDS preliminary formula,and then the optimal mixing the D-design,with an average particle size,multiple scattering coefficient,light transmittance as evaluation index,the preliminary formula to optimize the matching and eventually optimize the liquid GO-SMEDDS formula for IPP:garlic oil:EL-35:propanediol=3:3:10:4.The liquid go-smedds is a transparent liquid with orange light,and the solution is clear and transparent after self-emulsification.Solid GO-SMEDDS was prepared by physical adsorption method,and the formula of solid GO-SMEDDS was calcium silicate:liquid GO-SMEDDS=1:2 through the investigation of powder fluidity.The solid GO-SMEDDS is a milky powder.2.Quality evaluation of GO-SMEDDS.The morphology of GO-SMEDDS was observed by particle size and potentiometer,transmission electron microscope and field emission scanning electron microscope.It was found that the turbidity point of the liquid GO-SMEDDS was 70℃,the particle size of the self-emulsifying emulsion was 29.683±0.247nm,the PDI was 0.1797±0.006,the self-emulsifying time was 59.8s,and the particle size was the same as that of the liquid GO-SMEDDS.The solid GO-SMEDDS were agglomerated blocks under the scanning electron microscope,with the particle size of 51.233±1.215 nm and the PDI of 0.588±0.09 after rewatering.Under the transmission electron microscope,the spherical size was consistent with the particle size.An intelligent Fourier transform infrared spectrometer was used to observe whether chemical changes occurred in GO-SMEDDS.The infrared spectrum showed that the characteristic peak disappeared after the garlic oil was micro-emulsified,indicating that the garlic oil was embedded in SMEDDS and the physical adsorption method would not destroy SMEDDS.High pressure liquid chromatography was developed for the determination of the allicin,with hot and cold cycle stability experiment,the factors affecting stability and the stability of room temperature stability test to investigate the GO-SMEDDS,experiments show that the GO-SMEDDS stratification,hot and cold cycle will not lead to liquid but will reduce the content of allicin;High temperature and light have an effect on the allicin of GO-SMEDDS.The finished products should be stored in the dark at a temperature<25℃.No stratification was found in GO-SMEDDS which had been placed at room temperature for 6 months,and the content of allicin was higher than that of garlic oil of the same concentration.SMEDDS technology can enhance the stability of garlic oil.In the in vitro simulated digestion experiment,it was found that the gastric and intestinal fluid had a certain effect on the allicin of garlic oil,and the SMEDDS technology could effectively protect this effect.By reverse dialysis method respectively to investigate the GO-SMEDDS release in the artificial gastric juice and intestinal juice,and the release curve fitting equation,the results are as follows:garlic oil in artificial gastric juice and intestinal juice release rate was 0.7%and 0.5%,the accumulation of liquid was 20.03%and 5.26%,the GO-SMEDDS solid GO-SMEDDS was 12.07%and 3.91%,showed that SMEDDS greatly increased the release rate of garlic oil;The best kinetic model of garlic oil is the retger-peppas equation,the liquid GO-SMEDDS is the retger-peppas equation,and the solid GO-SMEDDS is the Gompertz first-order equation.3.Antibacterial study of GO-SMEDDS.Paper and turbidimetric method were carried out to study the GO-SMEDDS for escherichia coli,pseudomonas aeruginosa,staphylococcus aureus,bacillus subtilis,candida albicans and the bacteriostasis effect of yeast,found that garlic oil of the 6 kinds of bacteria have strong bacteriostatic and bactericidal effect,specific inhibition effect for the fungus(candida albicans and saccharomyces cerevisiae)>of gram-negative bacteria(staphylococcus aureus and bacillus subtilis)>pseudomonas aeruginosa>e.coli.The antibacterial effect of go-smedds was slightly less than that of simple garlic oil,and the antibacterial effect of liquid GO-SMEDDS was better than that of solid GO-SMEDDS.The antibacterial mechanism of liquid GO-SMEDDS on gramsella was preliminarily explored from the permeability of cell membrane(wall)by means of scanning electron microscope observation,the change of electric conductivity and the content of macromolecular enzyme in the liquid,etc.Found that liquid after the GO-SMEDDS effect on bacteria,to destroy the cell wall,causing cell deformation,Alkaline phosphatase enzyme leakage,further effects on cell membrane,make its choice through the sexual,characterized by increased conductivity,transaminase energy increases,affecting cell normal degradation and synthesis of the peptide and protein metabolism,resulting in bacterial death.