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Lanoconazole-loaded emulsion stabilized with cellulose nanocrystals decorated with polyphosphoesters reduced inflammatory edema in a mouse model
Polymer Journal ( IF 2.3 ) Pub Date : 2021-08-23 , DOI: 10.1038/s41428-021-00548-1
Suphatra Hiranphinyophat 1, 2 , Akihisa Otaka 2 , Yasuhiko Iwasaki 2, 3 , Syuji Fujii 4
Affiliation  

Efficient topical delivery of antifungal drugs, such as lanoconazole (LCZ), is challenging due to the limited water solubility and required prolonged duration of treatment. In this study, LCZ-loaded emulsions stabilized with cellulose nanocrystals grafted with polyphosphoesters (LCZ-loaded CP-PEs) were developed to enhance the anti-inflammatory efficacy of LCZ on skin. A high drug-loading efficiency (>80%) of LCZ in CP-PEs with a small mean droplet size of 1.0–1.5 μm was achieved. The sustained release of LCZ and superior skin permeation of the LCZ-loaded CP-PEs, likely due to the excellent stability and rigidity of oil droplets, assured prolonged local action. In addition, the excellent anti-inflammatory efficacy of the LCZ-loaded CP-PEs was clarified using a mouse ear model of 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation. Treatment with the LCZ-loaded CP-PEs significantly reduced auricular thickness compared to treatments with a commercial ointment and control solution containing LCZ. These results suggest that LCZ-loaded CP-PEs are a promising alternative for the treatment of inflammatory skin diseases, such as tinea pedis.



中文翻译:

用聚磷酸酯装饰的纤维素纳米晶体稳定的负载拉诺康唑的乳液减少了小鼠模型中的炎性水肿

由于有限的水溶性和需要延长的治疗时间,抗真菌药物,如拉诺康唑 (LCZ) 的有效局部给药具有挑战性。在这项研究中,开发了用接枝聚磷酸酯的纤维素纳米晶体稳定的负载 LCZ 的乳液(负载 LCZ 的 CP-PEs),以增强 LCZ 对皮肤的抗炎作用。CP-PE 中 LCZ 的载药效率高(>80%),平均液滴尺寸为 1.0-1.5 μm。LCZ 的持续释放和负载 LCZ 的 CP-PE 的卓越皮肤渗透性,可能是由于油滴的出色稳定性和刚性,确保了长时间的局部作用。此外,使用 12-O-十四烷酰佛波醇-13-乙酸酯 (TPA) 诱导的炎症的小鼠耳模型阐明了负载 LCZ 的 CP-PE 的优异抗炎功效。与使用含有 LCZ 的商业软膏和对照溶液处理相比,使用负载 LCZ 的 CP-PE 处理显着降低了耳廓厚度。这些结果表明,负载 LCZ 的 CP-PE 是治疗炎症性皮肤病(如足癣)的一种有前途的替代品。

更新日期:2021-08-23
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