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IF 3.4 4区医学 Q2 PHARMACOLOGY & PHARMACY

AAPS PharmSciTech Pub Date : 2025-04-02 DOI:10.1208/s12249-025-03094-8

Priyanka Rathore, Rishikesh Gupta, Prem Prakash Singh, Anshu Awasthi, Ankita Kishore, Kuldeep K. Bansal, Alok Kumar Mahor

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引用次数: 0

摘要

本研究提出了一种综合制药工程方法，通过创新的纳米复合凝胶配方，开发出一种先进的透皮给药系统，用于治疗皮肤色素沉着。利用系统化的质量源于设计（QbD）方法和盒-贝肯设计（Box-Behnken design），我们开发了一种新型氟西诺龙负载壳聚糖-氧化石墨烯纳米复合材料（FCGN1），旨在优化药物性能和疗效。该纳米复合制剂表现出了关键的药物质量属性：精确控制的纳米级粒度为 144.78 ± 0.15 nm，稳定的 zeta 电位为 -17.93 ± 3.75 mV，药物夹带效率高达 81.3 ± 3.64%。优化后的凝胶配方（FNTG3）表现出卓越的透皮给药特性，在 15 小时内达到约 70% 的渗透率和 190 µg/cm2 的显著通量，大大优于目前市场上的替代品。全面的药物评估包括超过 45 天的严格稳定性研究，证实了一致的物理稳定性和持续的药物渗透性。使用紫外线诱导的大鼠色素沉着模型进行的体内评估验证了该制剂的皮肤耐受性和去色素沉着潜力，表明其性能可与商用氢醌疗法媲美，甚至更胜一筹。组织病理学分析表明，纳米复合材料系统的协同设计具有明显的祛斑效果。氟西诺龙、壳聚糖和氧化石墨烯的战略整合促进了药物释放动力学的增强和皮肤渗透性的改善，凸显了合理制药设计在开发先进局部给药系统方面的潜力。这项研究为开发具有更佳治疗性能的复杂药物剂型提供了一个稳健的框架，为皮肤病应用领域的纳米级给药技术提供了重要启示。研究结果强调了系统优化和多功能成分设计在创造创新药物制剂方面的重要性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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QbD-Based Development of Fluocinolone Nanocomposite Transdermal Gel: Optimization, Characterization, and Enhanced Anti-hyperpigmentation Efficacy Assessment

The current study presents a comprehensive pharmaceutical engineering approach to developing an advanced transdermal drug delivery system for addressing skin hyperpigmentation through innovative nanocomposite gel formulation. Utilizing a systematic Quality-by-Design (QbD) methodology with Box-Behnken design, we developed a novel fluocinolone-loaded chitosan-graphene oxide nanocomposite (FCGN1) aimed at optimizing pharmaceutical performance and therapeutic efficacy. The nanocomposite formulation demonstrated critical pharmaceutical quality attributes: a precisely controlled nanoscale particle size of 144.78 ± 0.15 nm, stable zeta potential of -17.93 ± 3.75 mV, and high drug entrapment efficiency of 81.3 ± 3.64%. The optimized gel formulation (FNTG3) exhibited superior transdermal delivery characteristics, achieving approximately 70% permeation within 15 h and a significant flux rate of 190 µg/cm², which substantially outperforms current market alternatives. The comprehensive pharmaceutical evaluation included rigorous stability studies over 45 days, confirming consistent physical stability and sustained drug permeation. In vivo assessments using a UVB-induced hyperpigmentation rat model validated the formulation's dermal tolerability and depigmentation potential, demonstrating comparable or superior performance to commercial hydroquinone treatments. Histopathological analyses revealed pronounced depigmentation effects, attributable to the synergistic design of the nanocomposite system. The strategic integration of fluocinolone, chitosan, and graphene oxide facilitated enhanced drug release kinetics and improved skin penetration, highlighting the potential of rational pharmaceutical design in developing advanced topical delivery systems. This research provides a robust framework for developing sophisticated pharmaceutical dosage forms with enhanced therapeutic performance, offering significant insights into nanoscale drug delivery technologies for dermatological applications. The findings underscore the importance of systematic optimization and multifunctional component design in creating innovative pharmaceutical formulations.

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来源期刊

AAPS PharmSciTech 医学-药学

CiteScore

6.80

自引率

3.00%

发文量

264

审稿时长

2.4 months

期刊介绍： AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.