纳米脂质体嵌入纳米絮凝剂用于蒿甲醚和卢曼芬特林的重塑给药:体外和体内研究。

IF 1.6 4区 医学 Q4 BIOCHEMICAL RESEARCH METHODS Assay and drug development technologies Pub Date : 2024-02-01 Epub Date: 2024-01-09 DOI:10.1089/adt.2023.031
Dyandevi Mathure, Prashant Sonawane, Hemantkumar Ranpise, Rajendra Awasthi
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引用次数: 0

摘要

抗疟药物被封装在以纳米技术为基础的载体中,是因为没有足够的新治疗方案,而且人们对现有治疗方案的抗药性越来越强。这种方法利用疟原虫的两个或多个生化靶点。蒿甲醚和卢曼芬特林(AL)的联合给药结合了蒿甲醚的协同作用,使其早期起效,然后是卢曼芬特林的长效作用。由于蒿甲醚和卢曼芬特林的溶解度较低,其生物利用度较低。因此,通过在预制纳米脂质体(AL-负载脂质体)中加入钙离子,为所选药物开发了一种替代脂质制剂,即纳米钙酸盐。使用磷脂酰 90H 和胆固醇,通过薄膜水合方法制备出药物负载脂质体。合成的 AL 负载脂质体被进一步掺入纳米絮凝物中。对这些制剂进行了体外和体内参数评估。纳米絮凝物的粒径为200.7 nm,zeta电位为-9.4 mV,对蒿甲醚和鲁班群的包载效率分别为73.12% ± 1.82%和61.46% ± 0.78%。而脂质体的粒径为 210 nm,对蒿甲醚和卢门蒽林的包封效率分别为 67.34% ± 1.52% 和 53.24% ± 0.78%。X 射线衍射研究证实,脂质体和纳米絮凝剂中的蒿甲醚和卢门蒽林呈无定形状态。纳米包衣显示出负载药物的控释曲线。与游离药物相比,纳米絮凝物在大鼠体内的组织分布较少,生物利用率提高了 20 倍。因此,纳米包衣酸盐为治疗疟疾提供了现有剂型的一种有趣替代品。
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Nanoliposomes Embedded Nanocochleates for Codelivery of Artemether and Lumefantrine: An In Vitro and In Vivo Study.

Antimalarial drugs are being encapsulated in nanotechnology-based carriers because there are not enough new treatment options and people are becoming more resistant to the ones that are already available. This approach uses two or more biochemical targets of malarial parasites. The codelivery of artemether and lumefantrine (AL) combines the synergistic effect of artemether for an early onset of action followed by the prolonged effect of lumefantrine. The bioavailability of artemether and lumefantrine is low due to their low solubility. Thus, an alternative lipidic formulation, namely nanocochleate, was developed for the selected drugs by adding calcium ions into preformed nanoliposomes (AL-loaded liposomes). Using phospholipon 90H and cholesterol, a thin-film hydration method produced drug-loaded liposomes. The synthesized AL-loaded liposomes were further incorporated into nanocochleates. The formulations were evaluated for in vitro and in vivo parameters. Nanocochleates had a particle size of 200.7 nm, a zeta potential of -9.4 mV, and an entrapment efficiency of 73.12% ± 1.82% and 61.46% ± 0.78%, respectively, for artemether and lumefantrine. Whereas liposomes had a particle size of 210 nm and an entrapment efficiency of 67.34% ± 1.52% and 53.24% ± 0.78%, respectively, for artemether and lumefantrine. An X-ray diffraction study confirmed the amorphous state of artemether and lumefantrine in liposomes and nanocochleate. Nanocochleate showed a controlled release profile for loaded drugs. When compared with free drugs, nanocochleate showed low tissue distribution and a 20-fold increase in bioavailability in rats. Thus, nanocochleate offers an interesting alternative to an existing dosage form for the treatment of malaria.

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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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