Innovative Rocuronium Bromide Topical Formulation for Targeted Skin Drug Delivery: Design, Comprehensive Characterization, In Vitro 2D/3D Human Cell Culture and Permeation.

Innovative Rocuronium Bromide Topical Formulation for Targeted Skin Drug Delivery: Design, Comprehensive Characterization, In Vitro 2D/3D Human Cell Culture and Permeation.
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用于靶向皮肤药物输送的创新性溴化溴化物局部配方:设计,全面表征,体外2D/3D人类细胞培养和渗透。

DOI:
10.3390/ijms24108776
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发表时间:
2023-05-15
影响因子:
5.6
通讯作者:
--
中科院分区:
生物学2区
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皮肤鳞状细胞癌(cSCC)是第二种最常见的非黑色素瘤皮肤癌,与长期暴露于太阳的紫外线(UV)辐射有关。罗库溴铵(RocBr)是一种FDA批准的药物,靶向抑制UV诱导的cSCC发展的p53相关蛋白激酶(PRPK)。本研究旨在研究RocBr的理化性质和体外行为。技术,如热分析,电子显微镜,光谱学和体外试验用于表征RocBr。成功地开发和评价了RocBr的局部油/水乳液洗剂制剂。用Strat-M®合成仿生膜和EpiDerm™ 3D人类皮肤组织定量RocBr从其洗剂制剂的体外渗透行为。RocBr药物的显著膜保留是明显的,并且与溶液相比,用洗剂制剂获得更多的保留。这是第一个系统和全面的研究报告这些发现。
Cutaneous squamous cell carcinoma (cSCC) is the second-most common type of non-melanoma skin cancer and is linked to long-term exposure to ultraviolet (UV) radiation from the sun. Rocuronium bromide (RocBr) is an FDA-approved drug that targets p53-related protein kinase (PRPK) that inhibits the development of UV-induced cSCC. This study aimed to investigate the physicochemical properties and in vitro behavior of RocBr. Techniques such as thermal analysis, electron microscopy, spectroscopy and in vitro assays were used to characterize RocBr. A topical oil/water emulsion lotion formulation of RocBr was successfully developed and evaluated. The in vitro permeation behavior of RocBr from its lotion formulation was quantified with Strat-M® synthetic biomimetic membrane and EpiDerm™ 3D human skin tissue. Significant membrane retention of RocBr drug was evident and more retention was obtained with the lotion formulation compared with the solution. This is the first systematic and comprehensive study to report these findings.
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