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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 permeation 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 density 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.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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