Lipid Colloidal Carriers for Improvement of Anticancer Activity of Orally Delivered Quercetin: Formulation, Characterization and Establishing <I>In Vitro–In Vivo</I> Advantage

Novel lipid nanocarriers, GeluPearl (GP) comprising of Precirol ATO 5 lipid nanoparticles with (GPNLC) or without oil (GPSLN), loaded with Quercetin (QR), were successfully fabricated to improve therapeutic efficacy. QR loaded GP nanoparticles were optimized to yield adequate colloidal stability, mean particle size in range of 350-380 nm and entrapment efficiency of more than 90%. GPSLN and GPNLC were characterized for morphological evaluation by virtue of cryo-TEM, surface charge, protection offered to QR against alkali mediated degradation and fluorescence studies to evaluate QR-lipid interaction. DSC analysis was performed to get insight into physical state of QR loaded in nanosystems. The in vitro release studies demonstrated sustained drug release potential of QR loaded GP. In vitro lipolysis studies confirmed that lipidic nanocarriers can improve QR solubilization. QR loaded GP nanosystems significantly (P < 0.05) reduced flank tumor volumes in C57BL/6 mice over a 22 day study period compared to QR suspension. GPSLN significantly reduced lung colonization and enhanced antimetastatic activity (P < 0.05) of drug against B16F10 melanoma cells in C57BL/6 mice as compared to QR suspension. QR loaded GPSLN and GPNLC could be effectively lyophilized without much change in particle size and drug content using 15% w/v mannitol as cryoprotectant.