Cordycepin Nanoencapsulated in Poly(Lactic-Co-Glycolic Acid) Exhibits Better Cytotoxicity and Lower Hemotoxicity Than Free Drug.

IF 4.9 Q2 NANOSCIENCE & NANOTECHNOLOGY Nanotechnology, Science and Applications Pub Date : 2020-06-12 eCollection Date: 2020-01-01 DOI:10.2147/NSA.S254770
Gregory Marslin, Vinoth Khandelwal, Gregory Franklin
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引用次数: 12

Abstract

Purpose: Cordycepin, a natural product isolated from the fungus Cordyceps militaris, is a potential candidate for breast cancer therapy. However, due to its structural similarity with adenosine, cordycepin is rapidly metabolized into an inactive form in the body, hindering its development as a therapeutic agent. In the present study, we have prepared cordycepin as nanoparticles in poly(lactic-co-glycolic acid) (PLGA) and compared their cellular uptake, cytotoxicity and hemolytic potential with free cordycepin.

Materials and methods: Cordycepin-loaded PLGA nanoparticles (CPNPs) were prepared by the double-emulsion solvent evaporation method. Physico-chemical characterization of the nanoparticles was done by zetasizer, transmission electron microscopy (TEM) and reverse-phase high-pressure liquid chromatography (RP-HPLC) analyses. Cellular uptake and cytotoxicity of CPNPs and free drug were tested in human breast cancer cells (MCF7). Hemolytic potential of both of these forms was evaluated in rat red blood cells (RBCs).

Results: Physico-chemical characterization revealed that CPNPs were spherical in shape, possessed a size range of 179-246 nm, and released the encapsulated drug sustainably over a period of 10 days. CPNPs exhibited a high level of cellular uptake and cytotoxicity than the free drug in MCF-7 cells. While CPNPs were not toxic to rat RBCs even at high concentrations, free cordycepin induced hemolysis of these cells at relatively low concentration.

Conclusion: Our results reveal that delivery as CPNPs could enhance the clinical efficacy of cordycepin substantially.

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聚乳酸-羟基乙酸纳米包封虫草素具有较好的细胞毒性和较低的血液毒性。
目的:冬虫夏草素是一种从真菌蛹虫草中分离出来的天然产物,是治疗乳腺癌的潜在候选药物。然而,由于其结构与腺苷相似,虫草素在体内被迅速代谢为无活性形式,阻碍了其作为治疗剂的发展。在本研究中,我们在聚乳酸-羟基乙酸(PLGA)中制备了虫草素纳米颗粒,并与游离虫草素比较了它们的细胞摄取、细胞毒性和溶血潜能。材料与方法:采用双乳液溶剂蒸发法制备冬虫夏草素负载PLGA纳米颗粒(CPNPs)。采用zetasizer、透射电子显微镜(TEM)和反相高压液相色谱(RP-HPLC)对纳米颗粒进行了理化表征。在人乳腺癌细胞(MCF7)中检测了CPNPs和游离药物的细胞摄取和细胞毒性。在大鼠红细胞(rbc)中评估了这两种形式的溶血潜能。结果:理化性质表征表明,CPNPs为球形,尺寸范围为179 ~ 246 nm,并能在10 d内持续释放包膜药物。CPNPs在MCF-7细胞中表现出高水平的细胞摄取和细胞毒性。虽然CPNPs在高浓度下对大鼠红细胞没有毒性,但在相对低浓度下,游离虫草素诱导这些细胞溶血。结论:CPNPs给药可显著提高冬虫夏草素的临床疗效。
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来源期刊
Nanotechnology, Science and Applications
Nanotechnology, Science and Applications NANOSCIENCE & NANOTECHNOLOGY-
CiteScore
11.70
自引率
0.00%
发文量
3
审稿时长
16 weeks
期刊介绍: Nanotechnology, Science and Applications is an international, peer-reviewed, Open Access journal that focuses on the science of nanotechnology in a wide range of industrial and academic applications. The journal is characterized by the rapid reporting of reviews, original research, and application studies across all sectors, including engineering, optics, bio-medicine, cosmetics, textiles, resource sustainability and science. Applied research into nano-materials, particles, nano-structures and fabrication, diagnostics and analytics, drug delivery and toxicology constitute the primary direction of the journal.
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