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首页> 美国卫生研究院文献>International Journal of Nanomedicine >Enhanced local bioavailability of single or compound drugs delivery to the inner ear through application of PLGA nanoparticles via round window administration
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Enhanced local bioavailability of single or compound drugs delivery to the inner ear through application of PLGA nanoparticles via round window administration

机译：通过圆窗给药应用PLGA纳米颗粒提高了单一或复合药物向内耳的局部生物利用度

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In this paper, the potential of poly(d,l-lactide-co-glycolide acid) (PLGA) nanoparticles (NPs) for carrying single or compound drugs traversing the round window membrane (RWM) was examined after the round window (RW) administration of different NPs to guinea pigs. First, coumarin-6 was incorporated into PLGA NPs as a fluorescent probe to investigate its ability to cross the RWM. Then, PLGA NPs with salvianolic acid B (Sal B), tanshinone IIA (TS IIA), and total panax notoginsenoside (PNS) including notoginsenoside R1 (R1), ginsenoside Rg1 (Rg1), and ginsenoside Rb1 (Rb1) were developed to evaluate whether NPs loaded with compound drugs would pass through the RWM and improve the local bioavailability of these agents. PLGA NPs loaded with single or compound drugs were prepared by the emulsification solvent evaporation method, and their particle size distribution, particle morphology, and encapsulation efficiency were characterized. In vitro release study showed sustained-release profiles of Sal B, TS IIA, and PNS from the NPs. The pharmacokinetic results showed that NPs applied to the RWM significantly improved drug distribution within the inner ear. The AUC0–t of coumarin-6 in the perilymph (PL) following RW administration of NPs was 4.7-fold higher than that of coumarin-6 solution, and the Cmax was 10.9-fold higher. Furthermore, the AUC0–t of R1, Rg1, and Rb1 were 4.0-, 3.1-, and 7.1-fold greater, respectively, after the application of NPs compared to the compound solution, and the Cmax were, respectively, 14.4-, 10.0-, and 16.7-fold higher. These findings suggest that PLGA NPs with unique properties at the nanoscale dimensions have a powerful ability to transport single or compound drugs into the PL through the RWM and remarkably enhance the local bioavailability of the encapsulated drugs in the inner ear. The use of PLGA NPs as nanoscale delivery vehicles to carry drugs across the RWM may be a promising strategy for the treatment of inner ear diseases.
机译：在本文中，研究了聚（d，l-丙交酯-共-乙交酯乙交酯）（PLGA）纳米颗粒（NPs）携带单一或复合药物穿越圆窗膜（RWM）的潜力。给豚鼠施用不同的NP。首先，将香豆素6作为荧光探针掺入PLGA NP中，以研究其穿越RWM的能力。然后，开发了具有丹酚酸B（Sal B），丹参酮IIA（TS IIA）和总三七总皂苷（PNS）的PLGA NP，包括三七皂苷R1（R1），人参皂苷Rg1（Rg1）和人参皂苷Rb1（Rb1）。装有复合药物的NPs是否会通过RWM并提高这些药物的局部生物利用度。通过乳化溶剂蒸发法制备了载有单一或复合药物的PLGA NP，并对其粒径分布，颗粒形貌和包封效率进行了表征。体外释放研究显示了NP中Sal B，TS IIA和PNS的持续释放曲线。药代动力学结果表明，应用于RWM的NP显着改善了内耳内的药物分布。 NP RW给药后，外周淋巴（PL）中香豆素6的AUC0-t比香豆素6溶液的AUC0-t高4.7倍，Cmax则高10.9倍。此外，与复合溶液相比，施用NP后R1，Rg1和Rb1的AUC0-t分别大4.0-，3.1-和7.1-倍，Cmax分别为14.4、10.0 -和16.7倍高。这些发现表明，在纳米尺度上具有独特性质的PLGA NP具有强大的能力，可以通过RWM将单一或复合药物转运到PL中，并显着提高内耳中封装药物的局部生物利用度。使用PLGA NPs作为纳米级运载工具在RWM中携带药物可能是治疗内耳疾病的有前途的策略。

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