Skin permeability and transdermal delivery route of 30-nm cyclosporin A-loaded nanoparticles using PLGA-PEG-PLGA triblock copolymer
Skin permeability and transdermal delivery route of 30-nm cyclosporin A-loaded nanoparticles using PLGA-PEG-PLGA triblock copolymer
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DOI：
10.1016/j.colsurfa.2020.124866
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发表时间：
2020-09
期刊：
影响因子：
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通讯作者：
Issei Takeuchi;A. Kagawa;K. Makino
中科院分区：
文献类型：
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作者：
Issei Takeuchi;A. Kagawa;K. Makino
本研究的目的是研究使用聚(dl-丙交酯-共-乙交酯)-嵌段-聚(乙二醇)-嵌段-聚(dl-丙交酯-共-乙交酯)三嵌段共聚物(PLGA-PEG-PLGA)作为药物载体时疏水性药物的皮肤渗透性。采用反溶剂扩散法与优先溶剂化相结合的方法制备了两种平均粒径为30 nm的PLGA-PEG-PLGA纳米粒子和用于对比的聚(dl-丙交酯-共-乙交酯)(PLGA)纳米粒子。环孢素A用作疏水性模型药物。从体外释放试验的结果可以看出，PLGA-PEG-PLGA纳米颗粒中药物从纳米颗粒中的释放相对较快。这一结果表明，与PLGA纳米颗粒相比，PLGA-PEG-PLGA纳米颗粒的热力学活性增加，促进药物扩散到角质层中。使用大鼠皮肤和透皮递送途径对皮肤渗透性的研究结果表明，PLGA-PEG-PLGA纳米颗粒可用于有效的药物皮肤渗透，并且可以将药物递送至表皮和真皮层深处。另外，在使用模仿人体皮肤的Strat-M®进行的膜渗透性测试中，与使用PLGA纳米颗粒时相比，使用PLGA-PEG-PLGA纳米颗粒时药物的膜渗透量显着增加。
The aim of this study was to investigate the skin permeability of a hydrophobic drug when using poly(dl-lactide-co-glycolide)-block-poly(ethylene glycol)-block-poly(dl-lactide-co-glycolide) triblock copolymers (PLGA-PEG-PLGA) as a drug carrier. Two types of PLGA-PEG-PLGA nanoparticles with an average particle size of 30 nm and poly(dl-lactide-co-glycolide) (PLGA) nanoparticles for comparison were prepared using a combination of an antisolvent diffusion method with preferential solvation. Cyclosporin A was used as a hydrophobic model drug. From the results of thein vitrorelease test, it was confirmed that the release of the drug from the nanoparticles was relatively fast in the PLGA-PEG-PLGA nanoparticles. This result suggested that, compared to PLGA nanoparticles, the thermodynamic activity of PLGA-PEG-PLGA nanoparticles increased and the diffusion of the drug into the stratum corneum was promoted. The results of studies on skin permeability using rat skin and a transdermal delivery route showed that PLGA-PEG-PLGA nanoparticles were useful for efficient drug skin permeation and can deliver the drugs deep into the epidermal and dermal layers. Additionally, in the membrane permeability tests using Strat-M®, which imitates human skin, the membrane permeation amount of the drug was significantly increased when PLGA-PEG-PLGA nanoparticles were used compared with when PLGA nanoparticles were used.