湖北枫杨总黄酮单一基质可溶性微针的制备及性能评价 点击下载
| 论文标题： | 湖北枫杨总黄酮单一基质可溶性微针的制备及性能评价 |
| 英文标题： | |
| 中文摘要： | 目的 筛选单一基质，制备湖北枫杨总黄酮可溶性微针（PHTF-MN），并对其进行表征及镇痛效果评价。方法以微针外观形貌及穿刺率为评价指标，从聚乙烯醇（PVA），相对分子量58000、1300000的聚乙烯吡咯烷酮（PVPK30、PVPK90），相对分子量15000、60000的透明质酸钠（HA1.5w、HA6w）中筛选基质。采用所选基质，以分层浇注法制备PHTF-MN，并对所得微针的外观形貌、总黄酮含量、机械性能、穿刺性能、溶解性能、释药行为进行表征。以雄性BALB/c小鼠为对象，以阿司匹林（ASA）为阳性对照，采用福尔马林致痛模型对所得微针的镇痛作用进行评价。结果由30%HA1.5w所制空白微针的平整度较优，穿刺率（4层石蜡封口膜）可达78%。以该单一基质所制PHTF-MN（基质中PHTF的含量分别为10、20、30、40、50mg/g）的微针阵列整齐、针尖完整，其总黄酮含量的RSD均小于7%（n＝8）；单针受力分别为1.46、1.07N（基质中PHTF的含量分别为30、50mg/g时）；皮肤穿刺率接近100%，并可见角质层刺破痕迹及药物残留（基质中PHTF的含量为50mg/g时）；固定30min后，针体几乎完全溶解，皮肤滞留率均超过90%（基质中PHTF的含量分别为10、30、50mg/g时）；8h内的累积释放量为（134.64±2.03）μg/cm2，释药行为与一级动力学方程的拟合度（R2＝0.9501）最高（基质中PHTF的含量为50mg/g时）；低、高剂量PHTF-MN（以总黄酮计85.26、145.03μg/片，1片/d）能显著缩短小鼠的Ⅱ相疼痛反应累积时间（P＜0.05），疼痛抑制率（43.67%、59.78%）与ASA（53.70%）接近。结论成功制备了以HA1.5w为单一基质的PHTF-MN；该制剂制备流程简单、载药均匀、机械性能良好、不易断裂，兼具快速溶解性，其释药行为符合一级动力学模型，且镇痛作用与ASA相当。 |
| 英文摘要： | OBJECTIVE To screen a single matrix， prepare dissolving microneedles of Pterocarya hupehensis total flavonoids（PHTF-MN）， and characterize it while evaluating its analgesic effects.METHODS Using microneedle morphology and puncture rate as evaluation indicators， the matrix was screened from polyvinyl alcohol （PVA）， polyvinylpyrrolidone K30 （PVP K30）， PVP K90， and sodium hyaluronate with relative molecular weights of 15 000 and 60 000 （HA 1.5w and HA 6w ）. PHTF-MN was prepared by the layer-by-layer casting method with the selected matrix， and the appearance and morphology， total flavonoid content， mechanical properties， puncture performance， dissolution properties， and drug release behavior of the obtained PHTF-MN were characterized. Using male BALB/c mice as test subjects and aspirin （ASA） as a positive control， the analgesic effects of the microneedles were evaluated using a formalin-induced pain model.RESULTS Blank microneedles prepared with 30% HA 1.5w exhibited optimal surface flatness and the membrane puncture rate （through 4 layers of parafilm membrane） reaching 78%. The PHTF-MNs （with PHTF contents of 10， 20， 30， 40， and 50 mg/g in the matrix） exhibited uniform arrays and intact tips， with RSDs for total flavonoid contents all below 7% （ n ＝8）. The single-needle puncture forces were 1.46 and 1.07 N （with PHTF contents of 30 and 50 mg/g in the matrix， respectively）. The skin penetration rate approached 100%， with visible puncture marks in the stratum corneum and drug residue （with a PHTF content of 50 mg/g in the matrix）. After 30 min of fixation， the needles had almost completely dissolved， and the skin retention rates all exceeded 90% （with PHTF contents of 10， 30， and 50 mg/g in the matrix， respectively）. The cumulative release within 8 h was （134.64±2.03） μg/cm 2 ， and the fit to the first-order kinetic equation （ R 2 ＝0.950 1） was highest （with a PHTF content of 50 mg/g in the matrix）. Low- and high-dose PHTF-MN （containing 85.26 and 145.03 μg of total flavonoids per patch， respectively； 1 patch/day） significantly shortened the cumulative time of phase Ⅱ pain response in mice （ P ＜0.05）， with pain inhibition rates （43.67% and 59.78%） comparable to those of ASA （53.70%）.CONCLUSIONS PHTF-MN using HA 1.5w as a single matrix was successfully prepared. This formulation features a simplified preparation process， uniform drug loading， favorable mechanical properties， resistance to fracture， and rapid dissolution. Its drug release behavior conforms to a first-order kinetic model， and its analgesic effect is comparable to that of ASA. |
| 期刊： | 2026年第37卷第16期 |
| 作者： | 高星星；陈丹；夏燕；丁琳；陈星月；向阳；刘伦志；袁林 |
| 英文作者： | GAO Xingxing，CHEN Dan，XIA Yan，DING Lin，CHEN Xingyue，XIANG Yang，LIU Lunzhi，YUAN Lin |
| 关键字： | 湖北枫杨；总黄酮；可溶性微针；经皮递送；镇痛作用 |
| KEYWORDS： | Pterocarya hupehensis;Total flavonoids;dissolving microneedles;transdermal delivery;Analgesic effect |
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