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OBJECTIVE To investigate the penetration effect of solid microneedle in vivo and in vitro, the model drug ketoprofen was administered in the form of a patch. METHODS Using a rat skin penetration test, the effects of microneedle length, pre-treatment pressure, pre-treatment time, and types of needle on the penetration enhancement of ketoprofen in vitro were investigated. The pharmacokinetic characteristics of ketoprofen patches applied to the back of rats after different microneedle treatments were investigated, as well as the effect of the ketoprofen patch on promoting permeability in vivo. RESULTS In vitro, skin permeation tests revealed that after microneedle pretreatment, the permeation rate and permeation volume of the patch were significantly increased (P<0.05) and the permeation time lag was significantly shortened (P<0.05) after microneedle pretreatment, while the permeation promotion effect was related to the pressure, time, microneedle length and type of microneedle pretreatment. After microneedle pretreatment of the skin (pressure: 1-7 N, time: 1-5 min, microneedle length: 200 μm-300 μm), the cumulative permeation amount of the experimental drug for 24 hours increased by 1.16-3.09 times, and the permeation delay decreases by 0.20-2.50 h. As the results of in vivo pharmacokinetic in rats, ρmax (10.86±0.80) μg·mL-1 and AUC0→t (108.10±17.06) μg·h·mL-1 after 300 μm roller microneedle pretreatment of the skin, which were significantly greater than the control ρmax (0.42±0.03) μg·mL-1 and AUC0→t (7.46±0.98) μg·h·mL-1(P<0.05). ρmax and AUC0→t were increased by 25.9 times and 15 times. CONCLUSION Solid microneedle pretreatment of skin significantly improves in vitro penetration and in vivo skin absorption of ketoprofen patches through rat skin, with a more significant promotion effect in vivo penetration.
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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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