Liu Yang, Cheng Maosen, Zhao Junqi, Zhang Xiaoying, Huang Zhen, Zang Yuhui, Ding Ying, Zhang Junfeng, Ding Zhi
State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210023, China.
Department of Anesthesiology, The Second Affiliated Hospital of Nanjing Medical University, Nanjing 210011, China.
Biomedicines. 2021 May 23;9(6):592. doi: 10.3390/biomedicines9060592.
This study aimed to improve the transdermal delivery of lidocaine hydrochloride (LidH) using elastic nano-liposomes (ENLs) and microneedle (MN) array pretreatment. LidH-containing ENLs were prepared using soybean phosphatidylcholine and cholesterol, with Span 80 or Tween 80, using a reverse-phase evaporation method. The ENL particle size, stability, and encapsulation efficiency (EE) were characterized and optimized based on the component ratio, pH, and type of surfactant used. In vitro transdermal diffusion study was performed on MN-pretreated mouse skin using Franz diffusion cells. The anesthetic effects of LidH in various formulations after dermal application were evaluated in vivo in rats by measuring the tail withdrawal latency after photothermic stimulation. Stable LidH-loaded Tween 80 or Span 80 ENLs were obtained with particle sizes of 115.8 and 146.6 nm and EEs of 27% and 20%, respectively. The formulations did not exert any cytotoxicity in HaCaT cells. Tween 80 and Span 80 ENL formulations showed enhanced LidH delivery on pretreated mice skin in vitro and prolonged the anesthetic effect in vivo compared to that by LidH application alone. LidH-loaded ENLs applied to MN-pretreated skin can shorten the onset time and prolong the anesthetic effect safely, which merits their further optimization and practical application.
本研究旨在利用弹性纳米脂质体（ENLs）和微针（MN）阵列预处理来改善盐酸利多卡因（LidH）的经皮递送。采用反相蒸发法，使用大豆磷脂酰胆碱、胆固醇以及Span 80或吐温80制备含LidH的ENLs。基于所用表面活性剂的组成比例、pH值和类型，对ENL的粒径、稳定性和包封率（EE）进行了表征和优化。使用Franz扩散池对MN预处理的小鼠皮肤进行体外经皮扩散研究。通过测量光热刺激后大鼠的甩尾潜伏期，在体内评估了不同制剂中LidH经皮给药后的麻醉效果。获得了稳定的负载LidH的吐温80或Span 80 ENLs，粒径分别为115.8和146.6 nm，EE分别为27%和20%。这些制剂在HaCaT细胞中未表现出任何细胞毒性。与单独应用LidH相比，吐温80和Span 80 ENL制剂在体外预处理的小鼠皮肤上显示出增强的LidH递送，并在体内延长了麻醉效果。应用于MN预处理皮肤的负载LidH的ENLs可以缩短起效时间并安全地延长麻醉效果，这值得进一步优化和实际应用。
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