大麻二酚可溶性微针的制备、表征及初步药效学研究OA

Objective To prepare cannabidiol(CBD)-loaded dissolving microneedles(DMNs),and characterize their properties and conduct a preliminary pharmacodynamic evaluation,aiming to achieve precise drug delivery,reduce dosage,minimize adverse effects,and thereby optimize the balance between efficacy and safety.Methods CBD-loaded DMNs were fabricated using a layer-by-layer casting method,with the preparation process optimized through single-factor experiments.The morphology and mechanical properties of the microneedles were evaluated for quality assessment.The in vivo analgesic efficacy was investigated using a mouse acetic acid-induced writhing model.Results The optimal preparation parameters were determined as follows:using PVP K30 and PVP K90 as the matrix materials for the needle tips and backing layer,re-spectively,employing a two-step centrifugation method with a tip solution centrifugation time of 5 min and a fixed centrifuge speed of 4 500 r·min-1.The resulting microneedles exhibited intact morphology and satisfactory mechanical strength,with a single needle fracture force of no less than 2.9 N.Pharmacodynamic results showed that the CBD-loaded DMNs exhibited a higher pain inhibition rate compared to the CBD gel formulations,despite being administered at a much lower dose.Conclu-sion This study successfully developed CBD-loaded dissolving microneedles,which demonstrated significant analgesic effi-cacy at an extremely low dosage,indicating promising application prospects.