黏膜渗透纳米制剂可增强难溶性药物在目标部位的黏膜渗透能力。本工作设计了硫化壳聚糖（TCS）-石胆酸（LA）纳米胶束载荷β-胡萝卜素，一种具有抗癌属性的安全植物化合物，以改善药物的药理和药代特性。通过傅里叶红外光谱（FTIR）表征了TCS-LA纳米胶束，以确认有利于皮肤附着的巯基的存在，并证实了疏水性LA与亲水性CS的共轭形成了一个亲疏水性聚合物衍生物。X射线衍射（XRD）和差示扫描量热（DSC）分析揭示了纳米胶束的结晶性质和热行为。动态光散射（DLS）和透射电子显微镜（TEM）结果显示其平均尺寸小于300 nm，并且表面电荷为+27.0 mV。β-胡萝卜素的包封率和载荷效率分别为64%和58%。体外粘附和体外黏膜穿透分析进一步证实了该纳米制剂在模拟癌症微环境条件下以持续的方式释放药物的潜力。小鼠的抗癌研究表明，载荷纳米胶束可以延缓皮肤癌生长，这一结果通过形态学和生化参数均得到证实。根据本文的结果，可以得出结论，载荷的TCS-LA是一种新颖、稳定、有效、安全的黏膜附着型β-胡萝卜素制剂，有潜在用于治疗皮肤癌的作用。2023年版权所有。由Elsevier B.V.出版。

Mucopermeating nanoformulations can enhance mucosal penetration of poorly soluble drugs at their target site. In this work, thiolated chitosan (TCS)-lithocholic acid (LA) nanomicelles loaded with β-carotene, a safe phytochemical with anticancer properties, were designed to improve the pharmaceutical and pharmacological drug profile. The TCS-LA nanomicelles were characterized by FTIR to confirm the presence of the thiol group that favors skin adhesion, and to corroborate the conjugation of hydrophobic LA with hydrophilic CS to form an amphiphilic polymer derivative. Their crystalline nature and thermal behavior were investigated by XRD and DSC analyses, respectively. According to DLS and TEM, their average size was <300 nm, and their surface charge was +27.0 mV. β-carotene entrapment and loading efficiencies were 64 % and 58 %, respectively. In vitro mucoadhesion and ex vivo mucopenetration analyses further corroborated the potential of the nanoformulation to deliver the drug in a sustained manner under conditions mimicking cancer micro-environment. Anticancer studies in mice demonstrated that the loaded nanomicelles delayed skin cancer growth, as revealed by both morphological and biochemical parameters. Based on the results obtained herein, it can be concluded that drug-loaded TCS-LA is a novel, stable, effective and safe mucoadhesive formulation of β-carotene for the potential treatment of skin cancer.Copyright © 2023. Published by Elsevier B.V.