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 v...

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Autores principales: Raghuvir H. Gaonkar, Soumya Ganguly, Saikat Dewanjee, Samarendu Sinha, Amit Gupta, Shantanu Ganguly, Dipankar Chattopadhyay, Mita Chatterjee Debnath
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Publicado: Nature Portfolio 2017
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spelling oai:doaj.org-article:8e11acdf92bf440ea3afa4a579a61c7a2021-12-02T12:32:16ZGarcinol loaded vitamin E TPGS emulsified PLGA nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies10.1038/s41598-017-00696-62045-2322https://doaj.org/article/8e11acdf92bf440ea3afa4a579a61c7a2017-04-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-00696-6https://doaj.org/toc/2045-2322Abstract 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.Raghuvir H. GaonkarSoumya GangulySaikat DewanjeeSamarendu SinhaAmit GuptaShantanu GangulyDipankar ChattopadhyayMita Chatterjee DebnathNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-14 (2017)
institution DOAJ
collection DOAJ
language EN
topic Medicine
R
Science
Q
spellingShingle Medicine
R
Science
Q
Raghuvir H. Gaonkar
Soumya Ganguly
Saikat Dewanjee
Samarendu Sinha
Amit Gupta
Shantanu Ganguly
Dipankar Chattopadhyay
Mita Chatterjee Debnath
Garcinol loaded vitamin E TPGS emulsified PLGA nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies
description 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.
format article
author Raghuvir H. Gaonkar
Soumya Ganguly
Saikat Dewanjee
Samarendu Sinha
Amit Gupta
Shantanu Ganguly
Dipankar Chattopadhyay
Mita Chatterjee Debnath
author_facet Raghuvir H. Gaonkar
Soumya Ganguly
Saikat Dewanjee
Samarendu Sinha
Amit Gupta
Shantanu Ganguly
Dipankar Chattopadhyay
Mita Chatterjee Debnath
author_sort Raghuvir H. Gaonkar
title Garcinol loaded vitamin E TPGS emulsified PLGA nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies
title_short Garcinol loaded vitamin E TPGS emulsified PLGA nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies
title_full Garcinol loaded vitamin E TPGS emulsified PLGA nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies
title_fullStr Garcinol loaded vitamin E TPGS emulsified PLGA nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies
title_full_unstemmed Garcinol loaded vitamin E TPGS emulsified PLGA nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies
title_sort garcinol loaded vitamin e tpgs emulsified plga nanoparticles: preparation, physicochemical characterization, in vitro and in vivo studies
publisher Nature Portfolio
publishDate 2017
url https://doaj.org/article/8e11acdf92bf440ea3afa4a579a61c7a
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