John Garner

Malemide-PEG-PLGA and mPEG-PLGA from PolySciTech used in developing ligand-decorated, curcumin-loaded nanoparticles for breast-cancer treatment

Blog Post created by John Garner on Apr 3, 2018

Curcumin nanoparticles.jpg

There is a greater interface between herbal/traditional medicine and scientific medicine than most know about. Medicine can be derived from many natural sources (e.g. Paclitaxel derived from Pacific Yew tree) and medicinal chemists often focus on discovering new therapeutic agents derived from nature. Tumeric, and more specifically the extracted curcumin, has been of great interest lately due to curcumin’s anti-cancer properties. Simply eating tumeric spice, however, does not yield a significant anticancer effect for the majority of the body as curcumin has very poor absorption across the intestine. However, properly formulated and purified curcumin, can be a very powerful anticancer agent. It has an advantage over other chemotherapeutics in that it has minimal side-effects. Recently, researchers at Yantie University (China) used Maleimide-PEG-PLGA (PolyVivo AI020) and mPEG-PLGA (PolyVivo AK037) from PolySciTech ( to generate curcumin loaded nanoparticles with Fab targeting ligands for treating breast cancer. This research holds promise for effective breast-cancer treatment with minimal chemotherapy side effects. Read more:  Duan, Dongyu, Aiping Wang, Ling Ni, Liping Zhang, Xiuju Yan, Ying Jiang, Hongjie Mu, Zimei Wu, Kaoxiang Sun, and Youxin Li. "Trastuzumab-and Fab′ fragment-modified curcumin PEG-PLGA nanoparticles: preparation and evaluation in vitro and in vivo." International Journal of Nanomedicine 13 (2018): 1831.


“Abstract: Introduction: Nanoparticles (NPs) modified with bio-ligands represent a promising strategy for active targeted drug delivery to tumour. However, many targeted ligands, such as trastuzumab (TMAB), have high molecular weight, limiting their application for targeting. In this study, we prepared Fab’ (antigen-binding fragments cut from TMAB)-modified NPs (Fab′-NPs) with curcumin (Cur) as a model drug for more effective targeting of human epidermal growth factor receptor 2 (HER2/ErbB2/Neu), which is overexpressed on breast cancer cells. Material and methods: The release kinetics was conducted by dialysis bags. The ability to kill HER2-overexpressing BT-474 cells of Fab′-Cur-NPs compared with TMAB-Cur-NPs was conducted by cytotoxicity experiments. Qualitative and quantitative cell uptake studies using coumarin-6 (fluorescent probe)-loaded NPs were performed by fluorescence microscopy and flow cytometry. Pharmacokinetics and biodistribution experiments in vivo were assessed by liquid chromatography–tandem mass spectrometry (LC-MS/MS). Results: The release kinetics showed that both Fab′-Cur-NPs and TMAB-Cur-NPs provided continuous, slow release of curcumin for 72 h, with no significant difference. In vitro cytotoxicity experiments showed that Fab′-Cur-NPs manifested prominent ability to kill HER2-overexpressing BT-474 cells compared with TMAB-Cur-NPs. Qualitative and quantitative cell uptake studies indicated that the accumulation of Fab′-NPs was greater than that of TMAB-NPs in BT-474 (HER2+) cells; However, there was no significant difference in MDA-MB-231 (HER2−) cells. Pharmacokinetics and biodistribution experiments in vivo demonstrated that the half-life (t1/2) and area under the blood concentration-time curve (AUC0-t) of Fab′-Cur-NPs increased 5.30-fold and 1.76-fold relative to those of TMAB-Cur-NPs, respectively. Furthermore, the tumor accumulation of Fab′-Cur-NPs was higher than that of TMAB-Cur-NPs. Conclusion: Fab′ fragment has greater capacity than the intact antibody to achieve tumor targeting through NP-based delivery. Keywords: trastuzumab-modified curcumin nanoparticles, Fab′-modified curcumin nanoparticles, pharmacokinetics, biodistribution, tumour targeting, breast cancer”


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