title: Garcinol loaded vitamin E TPGS emulsified PLGA nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies.
abstract: Garcinol (GAR) is a naturally occurring polyisoprenylated phenolic compound. It has been recently investigated for its biological activities such as antioxidant, anti-inflammatory, anti ulcer, and antiproliferative effect on a wide range of human cancer cell lines. Though the outcomes are very promising, its extreme insolubility in water remains the main obstacle for its clinical application. Herein we report the formulation of GAR entrapped PLGA nanoparticles by nanoprecipitation method using vitamin E TPGS as an emulsifier. The nanoparticles were characterized for size, surface morphology, surface charge, encapsulation efficiency and in vitro drug release kinetics. The MTT assay depicted a high amount of cytotoxicity of GAR-NPs in B16F10, HepG2 and KB cells. A considerable amount of cell apoptosis was observed in B16f10 and KB cell lines. In vivo cellular uptake of fluorescent NPs on B16F10 cells was also investigated. Finally the GAR loaded NPs were radiolabeled with technetium-99m with >95% labeling efficiency and administered to B16F10 melanoma tumor bearing mice to investigate the in vivo deposition at the tumor site by biodistribution and scintigraphic imaging study. In vitro cellular uptake studies and biological evaluation confirm the efficacy of the formulation for cancer treatment.
authors.affiliation: Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology, Kolkata, India.
authors.forename: Raghuvir H
authors.initials: RH
authors.lastname: Gaonkar
authors.affiliation: Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology, Kolkata, India.
authors.forename: Soumya
authors.initials: S
authors.lastname: Ganguly
authors.affiliation: Advanced Pharmacognosy Research Laboratory, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India.
authors.forename: Saikat
authors.initials: S
authors.lastname: Dewanjee
authors.affiliation: Regional Radiation Medicine Center, Thakurpukur Cancer Center and Welfare Home Campus, Kolkata, India.
authors.forename: Samarendu
authors.initials: S
authors.lastname: Sinha
authors.affiliation: Regional Radiation Medicine Center, Thakurpukur Cancer Center and Welfare Home Campus, Kolkata, India.
authors.forename: Amit
authors.initials: A
authors.lastname: Gupta
authors.affiliation: Regional Radiation Medicine Center, Thakurpukur Cancer Center and Welfare Home Campus, Kolkata, India.
authors.forename: Shantanu
authors.initials: S
authors.lastname: Ganguly
authors.affiliation: Department of Polymer Science & Technology, University College of Science & Technology, University of Calcutta, Kolkata, India.
authors.forename: Dipankar
authors.initials: D
authors.lastname: Chattopadhyay
authors.affiliation: Infectious Diseases and Immunology Division, CSIR-Indian Institute of Chemical Biology, Kolkata, India. mitacd@iicb.res.in.
authors.forename: Mita
authors.initials: M
authors.lastname: Chatterjee Debnath
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D055598:Chemical Phenomena; D004337:Drug Carriers; D065546:Drug Liberation; D004655:Emulsions / Q000737:chemistry*; D019344:Lactic Acid / Q000737:chemistry*; D008546:Melanoma, Experimental; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D051381:Rats; D017550:Spectroscopy, Fourier Transform Infrared; D013729:Terpenes / Q000737:chemistry* / Q000494:pharmacology*; D014018:Tissue Distribution; D014810:Vitamin E / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D004655:Emulsions; D013729:Terpenes; D014810:Vitamin E; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; C054597:garcinol