用于治疗耐药性疟疾的新型壳聚糖包裹姜黄素纳米叶绿体的开发与表征

IF 1.6 4区 医学 Q4 BIOCHEMICAL RESEARCH METHODS Assay and drug development technologies Pub Date : 2024-01-01 Epub Date: 2023-12-27 DOI:10.1089/adt.2023.064
Bhargav Eranti, Padmanabha Reddy Yiragamreddy, Koteshwara Kunnatur Balasundara
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引用次数: 0

摘要

本研究旨在通过壳聚糖配制和包衣姜黄素(CR)来提高其药效。硅学分子对接研究显示,姜黄素与青蒿素的结合能几乎相似且较低,这表明姜黄素在靶位点具有很高的稳定性。可以证实,CR 能有效治疗和减少恶性疟原虫寄生。傅立叶变换红外研究证实,制剂中的一些药物峰出现了移动和消失,这表明药物与磷脂发生了络合。与纯 CR(7.99 ± 1.95 μg/mL)相比,F2EXT3 开发的制剂具有更高的溶解度(24.31 ± 3.47 μg/mL)。质子核磁共振研究证实,F2EXT3 中形成了姜黄素-磷脂氢键。体外药物释放研究表明,所开发的制剂 F2EXT3 在 48 小时内的药物释放率为 71.98%,表现较好;这可能是由于药物在磷脂中的有效包裹效率,聚乙二醇 4000 和壳聚糖的存在进一步帮助了药物的持续释放。扫描电子显微镜研究表明,优化后的 F2EXT3 CR 纳米叶绿体接近球形,尺寸分布窄,表面光滑。F2EXT3 的 zeta 电位为 -3.5 mV。稳定性研究表明,该制剂在 6 个月后仍保持稳定。从hemin试验中观察到,CR和F2EXT3(50 μg/mL姜黄素)的IC50值分别为47 ± 2.45和22 ± 1.58 μM。要评估所开发制剂的功效,还需要对抗药性和敏感性菌株进行进一步的体内抗疟活性试验。
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Development and Characterization of Novel Chitosan-Coated Curcumin Nanophytosomes for Treating Drug-Resistant Malaria.

This study aimed at enhancing the efficacy of curcumin (CR) by formulating and coating it with chitosan. In silico molecular docking studies revealed that CR exhibited almost similar and low binding energies when compared to artemisinin, indicating high stability at the target site. It can be confirmed that CR is effective in treating and reducing Plasmodium falciparum parasites. Fourier transform infrared studies confirmed that there was a shift and disappearance of some drug peaks in the formulation which revealed complexation with phospholipids. The F2EXT3-developed formulation exhibited greater solubility (24.31 ± 3.47 μg/mL) when compared to pure CR (7.99 ± 1.95 μg/mL). Proton nuclear magnetic resonance studies confirmed the formation of Curcumin-phospholipid hydrogen bonding in F2EXT3. The in vitro drug release studies revealed that the developed formulation F2EXT3 exhibited better drug release at 71.98% at 48 h; this might be due to the effective entrapment efficiency of the drug inside the phospholipid, presence of polyethylene glycol 4000 and chitosan further assisted in sustained release of the drug. Scanning electron microscopy studies revealed that optimized F2EXT3 CR nanophytosomes were nearly spherical with narrow size distribution and smooth surface. The zeta potential of the F2EXT3 showed -3.5 mV. Stability studies revealed that the formulation remained stable even after 6 months. It was observed from the hemin assay that CR and F2EXT3 exhibited (50 μg/mL curcumin) exhibited IC50 values of 47 ± 2.45 and 22 ± 1.58 μM, respectively. Further in vivo antimalarial activity on resistant and sensitive strains needs to be performed to evaluate the efficacy of the developed formulation.

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来源期刊
Assay and drug development technologies
Assay and drug development technologies 医学-生化研究方法
CiteScore
3.60
自引率
0.00%
发文量
33
审稿时长
>12 weeks
期刊介绍: ASSAY and Drug Development Technologies provides access to novel techniques and robust tools that enable critical advances in early-stage screening. This research published in the Journal leads to important therapeutics and platforms for drug discovery and development. This reputable peer-reviewed journal features original papers application-oriented technology reviews, topical issues on novel and burgeoning areas of research, and reports in methodology and technology application. ASSAY and Drug Development Technologies coverage includes: -Assay design, target development, and high-throughput technologies- Hit to Lead optimization and medicinal chemistry through preclinical candidate selection- Lab automation, sample management, bioinformatics, data mining, virtual screening, and data analysis- Approaches to assays configured for gene families, inherited, and infectious diseases- Assays and strategies for adapting model organisms to drug discovery- The use of stem cells as models of disease- Translation of phenotypic outputs to target identification- Exploration and mechanistic studies of the technical basis for assay and screening artifacts
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