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壳聚糖包覆脂质体稳定并增强吲哚菁绿的经皮传递用于黑素瘤光动力治疗。

Chitosan-coated liposomes to stabilize and enhance transdermal delivery of indocyanine green for photodynamic therapy of melanoma.

机构信息

Department of Bioscience and Bioengineering, Institute of Bioscience, Sejong University, Seoul, Republic of Korea; Department of Pharmaceutical Sciences, Woosuk University, Jeonbuk, Republic of Korea.

Department of Bioscience and Bioengineering, Institute of Bioscience, Sejong University, Seoul, Republic of Korea.

出版信息

Carbohydr Polym. 2019 Nov 15;224:115143. doi: 10.1016/j.carbpol.2019.115143. Epub 2019 Aug 2.

Abstract

Indocyanine green (ICG) has been used clinically and noticed as a promising candidate for the topical melanoma photodynamic therapy (PDT). Despite its high potentials in topical PDT, the use of ICG has been hampered by the instability in aqueous solution. In the present study, chitosan-coated liposomes were adopted as a formulation strategy which could stabilize and enhance skin permeation of ICG. Chitosan-coating was verified by the significantly increased liposomal size and reversed zeta potential from negative to positive value by positive chitosan coating. Chitosan-coating liposomes protected ICG from degradation while uncoated liposomes did not. Moreover, they significantly increased cellular uptake and photocytotoxicity of ICG in B16-F10 melanoma cells in a chitosan-dependent manner. The skin permeation of ICG was also drastically improved by chitosan-coated liposomes. These findings emphasize the promising potential of ICG-loaded chitosan-coated liposomes for topical PDT of melanoma.

摘要

吲哚菁绿(ICG)已在临床上得到应用,并被认为是一种很有前途的局部黑素瘤光动力疗法(PDT)候选药物。尽管 ICG 在局部 PDT 中具有很高的潜力,但由于其在水溶液中的不稳定性,其应用受到了限制。在本研究中,壳聚糖包被的脂质体被用作一种制剂策略,可以稳定和增强 ICG 的皮肤渗透。壳聚糖包被通过显著增加脂质体的粒径和将负的 zeta 电位反转为正值来证实。壳聚糖包被脂质体保护 ICG 免受降解,而未包被的脂质体则不能。此外,壳聚糖包被脂质体以壳聚糖依赖的方式显著增加了 B16-F10 黑素瘤细胞中 ICG 的细胞摄取和光细胞毒性。ICG 的皮肤渗透也被壳聚糖包被的脂质体大大改善。这些发现强调了载有 ICG 的壳聚糖包被脂质体在局部 PDT 治疗黑素瘤方面的潜在应用前景。

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