| Objective: The volatile oil of Magnoliae has many pharmacological effects including anti-inflammatory,antibacterial,antiviral and so on,which is widely used in the treatment of allergic rhinitis in clinic.However,due to its disadvantages of the nasal drug such as volatility and can not to be kept well,poor stability,factors that affecting drug efficacy and clinical efficacy.Therefore,it is of great significance to improve the clinical efficacy of the volatile oil of Magnoliae preparation.The biological adhesion microspheres were prepared by using chitosan as carrier material and investigated its quality,function and safety evaluation to provide new drug experimental study of the development of the Magnoliae chitosan microspheres.Method:(1)Gas chromatography was used to establish the content determination method of eucalyptol in the volatile oil of Magnoliae chitosan microspheres.(2)The difference between the multiple emulsion cross-linking method and the emulsion cross-linking method for preparation of microspheres was investigated.A single factor study was carried out on the microsphere preparation process,including colostrum mixing method,emulsification speed,emulsification time,emulsification temperature,curing time,curing temperature,continuous phase selection,emulsifier type and concentration,chitosan deacetylation degree and concentration,dosage,oil / water ratio,crosslinking dose.L9(34)Orthogonal test was used to optimize the prescription and technology with the size distribution of microspheres,drug loading,entrapment efficiency as combined index.(3)The quality of the product was evaluated by microsphere morphology,particle size distribution,entrapment efficiency,drug loading,adhesion,swelling properties,drug release.The rat foot swelling test and antibacterial test was used to evaluate its efficacy.(4)The rat foot swelling test and antibacterial test was used to evaluate its anti-inflammatory effect.(5)The safety of the rat nasal mucosal morphology test was evaluated by hemolysis test,toad jaw cilia toxicity test and rat nasal mucosal morphology test.Results:(1)Gas Chromatography was established to determine the content of eucalyptol in the volatile oil of Magnoliae chitosan microspheres;(2)The optimal preparation process of microspheres was as follows: the concentration of chitosan was 3%,the ratio of oil to water was 4,the stirring speed was 600r/min,the dosage was 1.(3)The appearance of the microspheres was round,the particle size was 69.37% in the proportion of 30-70?m,the particle size distribution was uniform with the span was 1.1.The average drug loading and entrapment efficiency of three batches of microspheres were 6.03% and 28.66%,respectively.Toad maxilla mucosa test showed that the microspheres had good adhesion and good swelling properties.From the release curve,we could see that the drug released a lot in the initial stage,which was good for the absorption of the drug by the intranasal administration.(4)The results showed that there was a significant difference between the experimental group and the blank control group(P <0.05),indicating that the product had certain anti-inflammatory effect;The results showed that the minimum inhibitory concentration of the volatile oil of Magnoliae chitosan microspheres against streptococcus,staphylococcus aureus and pseudomonas aeruginosa were 36.0,72.0 and 180.0 mg/m L respectively,which indicated that the product had certain bacteriostatic effect.(5)Hemolysis test showed that the product has no hemolytic effect;Toad maxilla mucosa toxicity test showed that this product has no obvious side effects on toad maxilla mucosa cilia.The morphology of nasal mucosa was observed in rats,and there was no significant difference between the experimental group and control group,which showed that product meets nasal administration requirements.Conclusion: The content determination method of eucalyptol in volatile oil of Magnoliae by Gas chromatography is highly sensitivity,accurate and easy to operate.The optimum preparation technology parameters of the microspheres are reasonable,operable,product quality consistent with nasal drug delivery requirements.This product has good antibacterial and anti-inflammatory effects,safety and non-irritating,which provides experimental data for the volatile oil of Magnoliae chitosan microspheres drug development. |
PDF Full Text Request