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首页> 外文期刊>Artificial cells, nanomedicine, and biotechnology. >Microneedle-mediated transdermal delivery of nanostructured lipid carriers for alkaloids from Aconitum sinomontanum
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Microneedle-mediated transdermal delivery of nanostructured lipid carriers for alkaloids from Aconitum sinomontanum

机译：微针介导的山茱Ac生物碱类纳米脂质载体的透皮递送

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摘要

A combination method using microneedle (MN) pretreatment and nanostructured lipid carriers (NLCs) was developed to improve the transdermal delivery of therapeutics. The MN treatment of the skin and co-administration of NLCs loaded with total alkaloids isolated from Aconitum sinomontanum (AAS–NLCs) significantly increased the skin permeation of the drugs. Fluorescence imaging confirmed that MNs could provide microchannels penetrating the stratum corneum, and delivery of NLCs through the channels led to their deeper permeation. In vivo studies showed that combination of AAS–NLCs with MNs (AAS–NLCs–MN) in transdermal delivery could improve the bioavailability and maintain stable drug concentrations in the blood. Moreover, AAS–NLCs–MN showed benefits in eliminating paw swelling, decreasing inflammation and pain, and regulating immune function in adjuvant arthritis rats. After administration of AAS–NLCs–MN, no skin irritation was observed in rabbits, and electrocardiograms of rats showed improved arrhythmia. These results indicated that the dual approach combining MN insertion and NLCs has the potential to provide safe transdermal delivery and to improve the therapeutic efficacy through sustained release of AAS.
机译：开发了一种使用微针（MN）预处理和纳米结构脂质载体（NLC）的组合方法，以改善治疗剂的透皮递送。 MN的皮肤治疗和与NLCs的联合使用可增加从皮肤乌头（AAS-NLCs）分离出的总生物碱的含量。荧光成像证实，MNs可以提供穿透角质层的微通道，而NLCs通过通道传递导致其更深的渗透。体内研究表明，透皮递送中AAS-NLC与MN（AAS-NLCs-MN）的组合可提高生物利用度并维持血液中稳定的药物浓度。此外，AAS-NLCs-MN在消除佐剂关节炎大鼠中的爪肿胀，减轻炎症和疼痛以及调节免疫功能方面显示出优势。给予AAS-NLCs-MN后，兔子未见皮肤刺激，大鼠心电图显示心律失常有所改善。这些结果表明，结合MN插入和NLC的双重方法具有提供安全的透皮递送和通过持续释放AAS提高治疗功效的潜力。

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