含槲皮素-水杨酸物理复合物的表面定制纳米混合胶束用于增强细胞活性和体内活性：基于质量源于设计理念

Surface-tailored nanomixed micelles containing quercetin-salicylic acid physical complex for enhanced cellular and in vivo activities: a quality by design perspective.

作者信息

Sandhu Premjeet Singh, Kumar Rajendra, Katare O P, Singh Bhupinder

机构信息

UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles & Nanocomposites, Panjab University, Chandigarh 160014, India.

Division of Pharmaceutics, University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160014, India.

出版信息

Nanomedicine (Lond). 2017 Jun;12(11):1281-1303. doi: 10.2217/nnm-2017-0040. Epub 2017 May 19.

DOI:10.2217/nnm-2017-0040

PMID:28524720

Abstract

AIM

The development of surface-tailored quercetin (QCT)-salicylic acid (SA) physical complex for effective treatment of skin carcinoma.

MATERIALS & METHODS: QCT-SA nanomixed micelles were prepared by the self-assembly method employing the Quality by Design (QbD) approach and evaluated for various in vitro, ex vivo and in vivo parameters.

RESULTS

The optimized formulation showed enhanced percent permeation (Q), in other words, 78.12 ± 0.47, improved in vitro cellular uptake and annexin-V-apoptosis assay exhibited 60.86% cell death. The 7,12-dimethylbenz(a)anthracene and histopathology protocol revealed the improved antineoplastic action of QCT. The dermatokinetic profile showed the maximum drug concentration (6 h), in other words, 416.02 ± 26 μg/cm in epidermis and 103.65 ± 12 μg/cm in dermis.

CONCLUSION

The overall performance ratified the safety and efficacy of optimized nanomixed micelless of QCT with SA in a synergistic manner.

摘要

目的

开发表面定制的槲皮素（QCT）-水杨酸（SA）物理复合物用于皮肤癌的有效治疗。

材料与方法

采用质量源于设计（QbD）方法通过自组装法制备QCT-SA纳米混合胶束，并对各种体外、离体和体内参数进行评估。

结果

优化后的制剂显示出增强的渗透百分比（Q），即78.12±0.47，体外细胞摄取改善，膜联蛋白-V凋亡检测显示细胞死亡率为60.86%。7,12-二甲基苯并(a)蒽和组织病理学实验表明QCT的抗肿瘤作用得到改善。皮肤动力学曲线显示最大药物浓度（6小时），即表皮中为416.02±26μg/cm，真皮中为103.65±12μg/cm。