一种脂质体水凝胶系统的开发和评价,用于提高高剂量的屈螺酮的递送。

IF 2.3 4区 医学 Q3 ENGINEERING, BIOMEDICAL Journal of Biomaterials Applications Pub Date : 2025-03-01 Epub Date: 2024-12-04 DOI:10.1177/08853282241305516
Xuena Zhang, Xuehan Wang, Juan Xu, Ting Wang
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引用次数: 0

摘要

屈螺酮(Drospirenone, DROP)是一种高效、低毒、安全的新一代黄体酮,可抵消雌激素相关的钠潴留,耐受性良好,对经前综合征(PMS)有积极作用。然而,DROP的水溶性低,化学性质不稳定,导致其生物利用度低。在这项研究中,我们开发了一个两步递送系统,以提高屈螺酮的溶解度和稳定性。制备了螺螺酮脂质体复合物,优化包封工艺,包封率为(84.9±0.73)%,溶解度提高878倍。为了解决高载药脂质体的不稳定性,我们使用纤维素基水凝胶固定了螺螺酮脂质体包合物。经扫描电镜和红外光谱分析证实,该系统在水凝胶中实现了脂质体的均匀负载。0.5 g水凝胶可载量达96.48 mg,包封率为(80.4±1.17%)。这表明具有增强水溶性和改善稳定性的屈螺酮具有更广泛的应用潜力。同时,它还为缓释系统或大剂量给药提供支持。
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Development and evaluation of a liposome hydrogel system for enhanced delivery of drospirenone at higher doses.

Drospirenone (DROP) is a highly effective, low-toxicity, safe new generation progestin that counteracts estrogen-related sodium retention, is well tolerated, and has a positive effect on premenstrual syndrome (PMS). However, the low water solubility of DROP and its chemical instability resulted in low bioavailability. In this study, we developed a two-step delivery system to enhance drospirenone's solubility and stability. We prepared a drospirenone liposome complex to optimize the encapsulation process and achieve an encapsulation efficiency of (84.9 ± 0.73) %, with an 878-fold increase in solubility under optimal conditions. To address the instability of high drug-loading liposomes, we immobilized the drospirenone liposome inclusion complex using a cellulose-based hydrogel. The system achieved uniform loading of liposomes in the hydrogel, as confirmed by SEM and FTIR analysis. 0.5 g hydrogel can be loaded with up to 96.48 mg drospirenone, and the encapsulation efficiency is (80.4 ± 1.17%). It was indicating the potential for wider application of drospirenone with enhanced water solubility and improved stability. At the same time, it also provides support for sustained-release systems or large dose drug delivery.

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来源期刊
Journal of Biomaterials Applications
Journal of Biomaterials Applications 工程技术-材料科学:生物材料
CiteScore
5.10
自引率
3.40%
发文量
144
审稿时长
1.5 months
期刊介绍: The Journal of Biomaterials Applications is a fully peer reviewed international journal that publishes original research and review articles that emphasize the development, manufacture and clinical applications of biomaterials. Peer-reviewed articles by biomedical specialists from around the world cover: New developments in biomaterials, R&D, properties and performance, evaluation and applications Applications in biomedical materials and devices - from sutures and wound dressings to biosensors and cardiovascular devices Current findings in biological compatibility/incompatibility of biomaterials The Journal of Biomaterials Applications publishes original articles that emphasize the development, manufacture and clinical applications of biomaterials. Biomaterials continue to be one of the most rapidly growing areas of research in plastics today and certainly one of the biggest technical challenges, since biomaterial performance is dependent on polymer compatibility with the aggressive biological environment. The Journal cuts across disciplines and focuses on medical research and topics that present the broadest view of practical applications of biomaterials in actual clinical use. The Journal of Biomaterial Applications is devoted to new and emerging biomaterials technologies, particularly focusing on the many applications which are under development at industrial biomedical and polymer research facilities, as well as the ongoing activities in academic, medical and applied clinical uses of devices.
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