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载有雷奈酸锶和熊果酸双载药纳米转脂体的溶解型微针经皮贴剂治疗骨质疏松症的研究:优化、表征、体外和离体评价。

Dissolving microneedle transdermal patch loaded with Risedronate sodium and Ursolic acid bipartite nanotransfersomes to combat osteoporosis: Optimization, characterization, in vitro and ex vivo assessment.

机构信息

School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi 110062, India.

Department of Biomedical Engineering, Chung Yuan Christian University, Taoyuan City 320314, Taiwan.

出版信息

Int J Pharm. 2023 Sep 25;644:123335. doi: 10.1016/j.ijpharm.2023.123335. Epub 2023 Aug 18.

DOI:10.1016/j.ijpharm.2023.123335
PMID:37597597
Abstract

Osteoporosis is a fatal bone-wearing malady and a substantial reason behind the impermanence of human life and economic burden. Risedronate Sodium along with Ursolic acid has been studied to ameliorate osteoporosis. To bypass problems associated with bioavailability, we have developed a microneedle transdermal patch loaded with optimized formulation nanotransfersomes. It was optimized using three factor, three-level Central composite design with independent variables namely, the concentration of phospholipid, surfactant, and sonication time on dependent variables (vesicle size, entrapment efficiency and Polydispersity index). Vesicles of size 271.9 ± 8.45 nm with PDI 0.184 ± 0.01, having entrapment efficiency of 86.12 ± 5.20% and 85.65 ± 4.88% for RIS and UA respectively were observed. In vitro release study showed the sustained release pattern with 78.16 ± 1.12% and 75.72 ± 1.01% release of RIS and UA respectively. Dissolving MN patch prepared from gelatin was found to have good strength and folding endurance with uniform drug content (98.68 ± 0.004%). Ex vivo permeation study revealed that up to 80% of the drug can be permeated within 24 h. CLSM analysis was also performed to show penetration of RU-NTRs. From the results obtained, we can conclude that dissolving MN patch loaded with RU-NTRs has great potential than its conventional counterpart.

摘要

骨质疏松症是一种致命的骨骼疾病,也是人类生命短暂和经济负担沉重的主要原因。研究表明,利塞膦酸钠联合熊果酸可改善骨质疏松症。为了避免与生物利用度相关的问题,我们开发了一种载有优化配方纳米转胞的微针透皮贴剂。该贴剂采用三因素三水平中心复合设计,以磷脂、表面活性剂和超声时间为自变量,以囊泡大小、包封率和多分散指数为因变量进行优化。结果显示,载药纳米转胞的粒径为 271.9±8.45nm,PDI 为 0.184±0.01,载药率分别为 86.12±5.20%和 85.65±4.88%。体外释放实验表明,RIS 和 UA 分别具有 78.16±1.12%和 75.72±1.01%的持续释放效果。从明胶中制备的可溶解微针贴片具有良好的强度和折叠耐力,且药物含量均匀(98.68±0.004%)。体外透皮实验表明,24h 内药物累积渗透量可达 80%。共聚焦激光扫描显微镜分析也显示了 RU-NTRs 的渗透情况。从实验结果可以得出结论,载 RU-NTRs 的可溶解微针贴片比传统制剂具有更大的潜力。

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