Quercetin Encapsulated Polymeric Nanomicelles Substantially Chemosensitising Antiproliferation By Branched Chain Amino Acids With Enhanced Antiinflammation Capacities: A New Strategy Against Cancer

Background Quercetin as a bioflavonoid with high anticancer potential, it has been proved to have a prospective applicability in chemotherapy for a series of cancers. PANC1, MCF7, CACO2, A375, A549 and PC3 cancer cell lines represent malignant neoplasms originating from respective pancreatic, breast, colorectal, skin, lung and prostate. The poor hydrophilicity of quercetin hinders its clinical usage in cancer therapy. Therefore, a strategy to improve the solubility of quercetin in water and/or enhance the bioavailability is desired. Aims In attempting to present positive evidences that this drug delivery system of polymeric micelles is effective; Quercetin loaded polymeric nanomicelles vs. free Quercetin were coincubated with selected 3 branched chain aminoacids (BCAAs; Val, Leu and Ile)) to examine synergy in chemosensitizing a panel of 6 cancer cell lines, thus reducing the dose used to submicro-nanomolar affinities of greater antiproliferation potencies than cisplatin’s. Results Quercetin loaded nanomicelles were proved of significantly less DPPH radical scavenging activity vs. both the antioxidative ascorbic acid and free quercetin. Unlike indomethacin; in lipopolysaccharide induced RAW264.7 macrophages inflammation; quercetin loaded nanomicelles had picomolar affinity for nitric oxide (NO) radical scavenging activity. Free quercetin posed inferior micromolar antiinflammation capacity vs. quercetin loaded nanomicelles, though more potent substantially vs. indomethacin. Remarkably nanocarrier formulation of quercetin was proved of significantly more potent antineoplastic bioactivity with micromolar affinities in the 6 cancer cell lines vs. both free quercetin’s and cisplatin’s. Exquisitely in PC3 monolayers; free quercetin was more potent than cisplatin (IC50 values (µM) 46 vs. 102; p