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

• Published in: Nanomedicine Vol. 33; p. 102368
• Main Authors: Thakur, Neeraj S., Mandal, Narattam, Patel, Gopal, Kirar, Seema, Reddy, Y. Nikhileshwar, Kushwah, Varun, Jain, Sanyog, Kalia, Yogeshvar N., Bhaumik, Jayeeta, Banerjee, Uttam C.
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.04.2021
• Subjects: Animals; Antineoplastic Agents - administration & dosage; Antineoplastic Agents - chemistry; Biocompatible Materials - administration & dosage; Biocompatible Materials - chemistry; Biomaterials; Cell Membrane Permeability; Delayed-Action Preparations; Drug Liberation; Fluorescence imaging; Humans; Hybrid nanoparticles; Isoindoles - administration & dosage; Isoindoles - chemistry; Liposomes - chemistry; MCF-7 Cells; Molecular Targeted Therapy; Nanoparticles - chemistry; Neoplasms - drug therapy; Neoplasms - radiotherapy; Organometallic Compounds - administration & dosage; Organometallic Compounds - chemistry; Photochemotherapy - methods; Photosensitizing Agents - administration & dosage; Photosensitizing Agents - chemistry; Quercetin - administration & dosage; Quercetin - chemistry; Rats; Rats, Sprague-Dawley; Reactive Oxygen Species - metabolism; Synergistic PDT; Targeted delivery; Zinc Compounds - administration & dosage; Zinc Compounds - chemistry; Synergistic PDT; Hybrid nanoparticles; Fluorescence imaging; Targeted delivery; Biomaterials
• ISSN: 1549-9634; 1549-9642
• DOI: 10.1016/j.nano.2021.102368

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. Highly hydrophobic photosensitizers could be efficiently delivered at the targeted tumor site using hybrid nanoparticles. Moreover, co-administration of the flavonoids (namely quercetin) synergizes the anticancer photodynamic effect of the administered photosensitizer. This combinatorial nanomedicine could have highly beneficial in cancer management. [Display omitted]