利匹韦林纳米吸附体的制剂开发和体外评估

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmaceutical Innovation Pub Date : 2024-07-19 DOI:10.1007/s12247-024-09852-8
Purnima Rawat, Sharad Gupta, Syed Sarim Imam
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引用次数: 0

摘要

本研究的重点是制备和表征负载利匹韦林的纳米生物体。通过薄膜水合法,使用利匹韦林、磷脂酰胆碱 S-100 (SPC) 和脱氧胆酸钠 (SDC) 开发了制剂。纳米吸附体的特征包括囊泡大小、多分散指数(PDI)、表面电荷和吸附效率(%EE)。使用差示扫描量热法(DSC)和傅立叶变换红外光谱法(FTIR)分析了热行为和药物与赋形剂之间的相互作用。透射电子显微镜(TEM)显示,BS-06 纳米纤维素体具有光滑均匀的表面形态。在 HeLa 和 HEK 293 细胞系上进行了体外细胞毒性试验,并评估了对金黄色葡萄球菌和大肠杆菌的最小抑菌浓度(MIC)。在不同温度下对其稳定性进行了 3 个月的监测。优化配方(BS-06)的囊泡大小为 132.8 ± 4.0 nm,zeta 电位为 -30.10 ± 0.8 mV,PDI 为 0.20,显示出最佳的表面特性和最高的包埋效率。细胞毒性研究表明,BS-06 在 24 和 48 小时内提高了 HeLa 和 HEK 293 细胞系的细胞活力,并增强了对金黄色葡萄球菌和大肠杆菌的抗菌活性。总之,我们的研究结果凸显了负载利匹韦林的纳米生物体作为一种治疗艾滋病毒/艾滋病的给药系统的潜力,它具有更好的溶解性、稳定性和生物相容性。
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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Formulation Development and In-Vitro Assessment of Rilpivirine Nanobilosomes

This study focused on the preparation and characterization of rilpivirine-loaded nanobilosomes. Formulations were developed using rilpivirine, phosphatidylcholine S-100 (SPC), and sodium deoxycholate (SDC) via the thin film hydration method. The nanobilosomes were characterized for vesicle size, polydispersity index (PDI), surface charge, and entrapment efficiency (%EE). Thermal behavior and drug-excipient interactions were analyzed using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). Transmission electron microscopy (TEM) revealed that BS-06 nanobilosomes possess a smooth and uniform surface morphology. In vitro cytotoxicity assays were conducted on HeLa and HEK 293 cell lines, and minimum inhibitory concentration (MIC) was assessed against S. aureus and E. coli. Stability was monitored over 3 months at various temperatures. The optimized formulation (BS-06) exhibited a vesicle size of 132.8 ± 4.0 nm, a zeta potential of -30.10 ± 0.8 mV, and a PDI of 0.20, demonstrating optimal surface characteristics and maximum entrapment efficiency. In vitro release studies indicated a maximum drug release of 84.81 ± 4.6% over 24 h. Cytotoxicity studies showed that BS-06 improved cell viability in HeLa and HEK 293 cell lines at 24 and 48 h and enhanced antibacterial activity against S. aureus and E. coli. Overall, our findings highlight the potential of rilpivirine-loaded nanobilosomes as a promising drug delivery system for HIV/AIDS, with enhanced dissolution, stability and biocompatibility.

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来源期刊
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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