The present study was intended to enhance the permeation of artemether and lumefantrine by encapsulating in dissolvable microneedle arrays for extended action. Lumefantrine-nanoparticles were synthesized using chitosan mediated gelation and optimized by 2² factorial designs. The particle size, zeta potential and % entrapment efficiency of the optimized nanoparticles F5 were 105 ± 3.64 nm, 24.4 ± 0.54 mV and 83.94 ± 1.71%, respectively. The nanoparticles showed a controlled-release of 79.15 ± 2.45% for lumefantrine after 24 h and stability for 6 months. A combination of biocompatible polymers (PVA and PVP K − 12) was used to develop dissolvable microneedle of artemether co-loaded lumefantrine nanoparticles. The SEM and TEM analysis confirmed the needle-shaped morphology with a size of 672 ± 0.99 μm. The in-vitro release of microneedle showed biphasic release pattern for both artemether and lumefantrine, with an initial burst followed by controlled-release profile. The ex-vivo study of optimized formulation showed 70.94 ± 2.45% and 65.87 ± 1.94% permeation for artemether and lumefantrine, respectively, after 24 h. Thus, microneedle-based delivery provides an alternative to painful intravenous administration and a promising approach to increase the penetration of drugs across the skin barrier.

Fabrication of microneedle arrays of artemether co-loaded with lumefantrine nanoparticles.

中文翻译：

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2 2基于阶乘设计的生物相容性微针阵列，其中包含蒿甲醚与褐煤碱纳米颗粒共装载，用于经皮递送

本研究旨在通过封装在可溶解的微针阵列中以扩大作用，从而增强蒿甲醚和卢美汀的渗透性。使用壳聚糖介导的凝胶合成Lumefantrine-纳米颗粒，并通过2 ²因子设计进行优化。优化的纳米颗粒F5的粒径，ζ电势和包封率％分别为105±3.64nm，24.4±0.54mV和83.94±1.71％。纳米颗粒在24小时后显示出对卢发碱的79.15±2.45％的控释和6个月的稳定性。生物相容性聚合物（PVA和PVP K-12）的组合被用来开发可溶负载的蒿甲醚共负载的荧光粉纳米粒子的微针。SEM和TEM分析证实了针状形态，尺寸为672±0.99μm。的微针的体外释放显示了蒿甲醚和lumefantrine的双相释放模式，先是爆发，然后是控释曲线。优化配方的离体研究显示，在24小时后，蒿甲醚和lumefantrine的渗透率分别为70.94±2.45％和65.87±1.94％。因此，基于微针的递送提供了痛苦的静脉内给药的替代方法以及增加药物穿过皮肤屏障的渗透的有前途的方法。

与紫杉精纳米粒子共载的蒿甲醚微针阵列的制备。