绿原酸-甲氨蝶呤可溶性微针的制备及初步评价OA

Objective To prepare chlorogenic acid-methotrexate dissolvable microneedles(CGA-MTX-DMNs)and evaluate their characteristics,quality and in vitro percutaneous permeability.Methods CGA-MTX-DMNs were prepared using a centrifugation method and characterized.The in vitro transdermal permeation properties of CGA-MTX-DMNs were evaluated using a modified Franz diffusion cell method.Results The prepared CGA-MTX-DMNs patch exhibited a complete array with high needle density,a needle length of approximately 518μm,and good mechanical strength.The average drug content of CGA and MTX was(57.97±1.76)μg/patch and(56.32±1.66)μg/patch,respectively.The microneedles were substantially dissolved within 2 hours,ef-fectively penetrated the stratum corneum,and the micropores closed naturally within 15 min after insertion with almost no skin irritation.In vitro transdermal tests demonstrated that the 6 hours cumulative permeation rates of CGA and MTX in CGA-MTX-DMNs patch were 93.96％and 86.92％,respectively,which were 22.1-fold and 3.0-fold higher than those of their corresponding solution alone groups.Conclusion CGA-MTX-DMNs with satis-factory mechanical properties and transdermal efficiency were successfully developed,enabling efficient transder-mal drug delivery.