In vitro apoptotic potential and ex vivo permeation analysis of ulipristal acetate loaded niosomes for management of uterine fibroids.

IF 3 4区医学 Q2 CHEMISTRY, APPLIED

Journal of microencapsulation Pub Date : 2025-05-28 DOI:10.1080/02652048.2025.2507639

Priyadarshi Aparajay, Harishkumar Madhyastha, Shuvadip Bhowmik, Abhimanyu Dev

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引用次数: 0

Abstract

Aim: To develop and optimise a niosomal formulation of ulipristal acetate (UPA) for enhanced cytotoxicity against uterine fibroids.

Methods: Quality by Design, thin film hydration, dynamic light scattering, transmission electron microscopy, cytotoxicity assays, flow cytometry, reactive oxygen species (ROS) generation analysis.

Results: Optimised UPA-loaded niosomes (UPA-NS) exhibited mean diameter of 170.7 ± 3.46 nm, polydispersity index of 0.23 ± 0.02, zeta potential of -18.2 ± 2.31 mV, encapsulation efficiency of 90.57 ± 3.22%w/w and 10.65 ± 1.64%w/w loading efficiency. UPA-NS showed 89 ± 3.22%w/w drug release at pH 5.5 within 24 hours compared to 36 ± 5.44%w/w at pH 7.4. UPA-NS demonstrated 70% cytotoxicity in HEC-6 cells at 0.5 μg/mL compared to 44% for free UPA. Flow cytometry showed 23% live cells for UPA-NS vs 33% for free UPA after 16 hours. UPA-NS induced higher ROS generation than free UPA.

Conclusions: The niosomal formulation enhanced the cytotoxicity and ROS-generating potential of UPA against uterine fibroid cells.

查看原文本刊更多论文

醋酸乌普利司酯负载乳小体治疗子宫肌瘤的体外凋亡电位及体外渗透分析。

目的：开发和优化醋酸乌普利司酯（UPA）的niosomal配方，以增强对子宫肌瘤的细胞毒性。方法：质量设计、薄膜水合、动态光散射、透射电镜、细胞毒性、流式细胞术、活性氧（ROS）生成分析。结果：优化后的UPA-NS平均直径为170.7±3.46 nm，多分散性指数为0.23±0.02，zeta电位为-18.2±2.31 mV，包封效率为90.57±3.22%w/w，负载效率为10.65±1.64%w/w。pH值为5.5时，24小时内UPA-NS的释药率为89±3.22%w/w， pH值为7.4时为36±5.44%w/w。0.5 μg/mL的UPA- ns对HEC-6细胞的毒性为70%，而游离UPA的毒性为44%。流式细胞术显示，16小时后，UPA- ns组活细胞23%，而游离UPA组活细胞33%。UPA- ns诱导的ROS生成高于游离UPA。结论：niosomal制剂增强了UPA对子宫肌瘤细胞的细胞毒性和ros生成潜能。

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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来源期刊

Journal of microencapsulation 工程技术-工程：化工

CiteScore

6.30

自引率

2.60%

发文量

审稿时长

3 months

期刊介绍： The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.