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通过杂化纳米粒子共给药锌酞菁和槲皮素以增强光动力疗法。

Co-administration of zinc phthalocyanine and quercetin via hybrid nanoparticles for augmented photodynamic therapy.

机构信息

Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S. Nagar-160062, Punjab, India; Department of Nanomaterials and Application Technology, Center of Innovative and Applied Bioprocessing (CIAB), Sector 81 (Knowledge City), Mohali-140306, Punjab, India; School of Pharmaceutical Sciences, University of Geneva, CMU - 1 Rue Michel Servet 1206, Geneva, Switzerland.

Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER), Sector-67, S.A.S. Nagar-160062, Punjab, India.

出版信息

Nanomedicine. 2021 Apr;33:102368. doi: 10.1016/j.nano.2021.102368. Epub 2021 Feb 3.

Abstract

The photodynamic anticancer activity of a photosensitizer can be further increased by co-administration of a flavonoid. However, this requires that both molecules must be effectively accumulated at the tumor site. Hence, in order to enhance the activity of zinc phthalocyanine (ZnPc, photosensitizer), it was co-encapsulated with quercetin (QC, flavonoid) in lipid polymer hybrid nanoparticles (LPNs) developed using biodegradable & biocompatible materials and prepared using a single-step nanoprecipitation technique. High stability and cellular uptake, sustained release, inherent fluorescence, of ZnPC were observed after encapsulation in the LPNs, which also showed a higher cytotoxic effect in breast carcinoma cells (MCF-7) compared to photodynamic therapy (PDT) alone. In vivo studies in tumor-bearing Sprague Dawley rats demonstrated that the LPNs were able to deliver ZnPc and QC to the tumor site with minimal systemic toxicity and increased antitumor effect. Overall, the photodynamic effect of ZnPc was synergized by QC. This strategy could be highly beneficial for cancer management in the future while nullifying the side effects of chemotherapy.

摘要

一种光敏剂的光动力抗癌活性可以通过联合使用类黄酮进一步提高。然而,这需要这两种分子都能有效地在肿瘤部位积累。因此,为了提高锌酞菁(ZnPc,光敏剂)的活性,它与槲皮素(QC,类黄酮)一起被包裹在使用可生物降解和生物相容材料开发并使用单步纳米沉淀技术制备的脂质聚合物杂化纳米粒子(LPNs)中。ZnPC 在 LPNs 中封装后表现出高稳定性和细胞摄取、持续释放、固有荧光,与单独的光动力疗法(PDT)相比,其对乳腺癌细胞(MCF-7)的细胞毒性作用更高。在荷瘤 Sprague Dawley 大鼠体内研究中,LPNs 能够将 ZnPc 和 QC 递送到肿瘤部位,同时具有最小的全身毒性和增强的抗肿瘤作用。总的来说,QC 协同增强了 ZnPc 的光动力效应。这种策略在未来癌症管理中可能具有很高的益处,同时消除了化疗的副作用。

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