Fabrication of Risedronate Sodium-Loaded Dissolving Microneedles and Evaluation of Its Therapeutic Effects on Postmenopausal Osteoporosis
OBJECTIVE To prepare risedronate sodium(RIS)-loaded dissolving microneedle(DMN)and evaluate its efficacy in preventing postmenopausal osteoporosis.METHODS The preparation process of RIS-DMN was optimized by Box-Behnken design of response surface methodology.The appearance,solubility,mechanical property,safety and transdermal effect of RIS-DMN were characterized by scanning electron microscope,intradermal dissolution test,puncture test,skin barrier recovery test and in vitro perme-ation test.The pharmacodynamic evaluation of RIS-DMN was performed in ovariectomized osteoporosis model rats.RESULTS The optimal formulation were determined to be 45%for solute(mixed with 1∶0.86 PVP K30 and CS)and 55%for solvent.It was found that the RIS-DMN have good physical characteristics and properties,and showed great effects in regulating the level of Ca2+,P3+and alkaline phosphatase(ALP).Meanwhile,the RIS-DMN showed great effects in repairing bone microstructure and improving bone den-sity in ovariectomized osteoporosis model rats,as similar as oral administration.CONCLUSION The RIS-DMN has stable quality,convenient use and precise efficacy,shows great potential in the treatment of postmenopausal osteoporosis.