RVG29肽修饰雷公藤红素传递体鼻用原位凝胶的制备及体外释药性能评价OA

Objective:To prepare RVG29 peptide modified celastrol transfersomes in situ nasal gel(RVG29-CLT-TFs/DGG)and investigate its in vitro drug release behavior.Methods:RVG29 peptide modified celastrol transfersomes(RVG29-CLT-TFs)were prepared by film hydration-sonication method.Deacetyl gellan gum(DGG)was selected as the gel ma-trix,with its amount determined based on viscosity,critical ion concentration,gel strength,water retention capacity,volume ex-pansion and pH value as the inspection indices.The optimal concentration of DGG and RVG29-CLT-TFs were mixed evenly in a volume ratio of 1∶1 to obtain RVG29-CLT-TFs/DGG.The drug release characteristics of RVG29-CLT-TFs were studied using PBS buffer(pH=7.4,containing 1.0%Tween 80).Results:The average particle size of RVG29-CLT-TFs was(112.33±0.26)nm,with a polydispersity index of 0.203±0.018 and a Zeta potential of(-41.13±1.7)mV.The entrapment efficiency and drug loading were(94.22±0.21)%and(2.31±0.25)%,respectively.A concentration of 1.0%DGG was determined as the opti-mal gel matrix and mixed it with RVG29-CLT-TFs at a ratio of 1∶1(v/v)to obtain RVG29-CLT-TFs/DGG.The viscosity of RVG29-CLT-TFs/DGG before phase transition was(10.33±0.47)mPa·s,wihch increased to(337.00±0.82)mPa·s after phase transition.The gel strength was(30.0±0.8)s,and the water retention capacity exceeded 85%.The S%was(1.33±0.02)%,the pH value was 6.18±0.02,and the critical ion concentration required for 1 mL of RVG29-CLT-TFs/DGG was 250 μL of artificial nasal liquid.The in vitro release results showed that the cumulative release rate of RVG29-CLT-TFs/DGG over 72 h was lower than that of both CLT and RVG29-CLT-TFs.Conclusion:The combination of RVG29-CLT-TFs and DGG can obvi-ously improve the drug CLT release rate and realize sustained release,and the preparation process is simple and feasible.