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Development and characterization of gel-in-water nanoemulsion as a novel drug delivery system

The effective delivery of anti-cancer drugs with minimal side effects and better therapeutic efficacy has remained an active area of research for many decades. Organogels have gained attention in recent years as potential drug delivery systems due to their high bioavailability, no first-pass metabol...

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Published in:Materials Science & Engineering C 2021-05, Vol.124, p.112076-112076, Article 112076
Main Authors: Fardous, Jannatul, Omoso, Yuji, Joshi, Akshat, Yoshida, Kozue, Patwary, Md Kawchar Ahmed, Ono, Fumiyasu, Ijima, Hiroyuki
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container_title Materials Science & Engineering C
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creator Fardous, Jannatul
Omoso, Yuji
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Yoshida, Kozue
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Ono, Fumiyasu
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description The effective delivery of anti-cancer drugs with minimal side effects and better therapeutic efficacy has remained an active area of research for many decades. Organogels have gained attention in recent years as potential drug delivery systems due to their high bioavailability, no first-pass metabolism and rapid action. Considering this, in the current study an organogel based nanoemulsion was developed aiming to effectively deliver hydrophobic drugs via encapsulation within in situ gellable organogel droplets, termed as gel-in-water (G/W) nanoemulsion. G/W nanoemulsion was prepared using a combination of lipiodol and organogelator 12-hydroxystearic acid (12-HSA) as inner gel phase; dispersed in water by ultrasonication and stabilized with polyoxyethylene hydrogenated castor oil (HCO-60) as a surfactant. The prepared nanoemulsion showed high drug loading efficiency (≈97%) with a mean diameter of 206 nm. Lower polydispersity index (PdI) value (≈0.1) suggests monodispersed nature of G/W nanoemulsion in the continuous phase. G/W nanoemulsion was found stable over six months in terms of particle size, zeta potential and pH at different storage temperatures. There was no cytotoxic effect of prepared G/W nanoemulsion on primary hepatocytes in vitro. In contrast, paclitaxel-loaded G/W showed a significant decrease in melanoma cell growth (*p 
doi_str_mv 10.1016/j.msec.2021.112076
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Organogels have gained attention in recent years as potential drug delivery systems due to their high bioavailability, no first-pass metabolism and rapid action. Considering this, in the current study an organogel based nanoemulsion was developed aiming to effectively deliver hydrophobic drugs via encapsulation within in situ gellable organogel droplets, termed as gel-in-water (G/W) nanoemulsion. G/W nanoemulsion was prepared using a combination of lipiodol and organogelator 12-hydroxystearic acid (12-HSA) as inner gel phase; dispersed in water by ultrasonication and stabilized with polyoxyethylene hydrogenated castor oil (HCO-60) as a surfactant. The prepared nanoemulsion showed high drug loading efficiency (≈97%) with a mean diameter of 206 nm. Lower polydispersity index (PdI) value (≈0.1) suggests monodispersed nature of G/W nanoemulsion in the continuous phase. G/W nanoemulsion was found stable over six months in terms of particle size, zeta potential and pH at different storage temperatures. There was no cytotoxic effect of prepared G/W nanoemulsion on primary hepatocytes in vitro. In contrast, paclitaxel-loaded G/W showed a significant decrease in melanoma cell growth (*p &lt; 0.05) both in vitro and in vivo. Our results support the hypothesis that organogel based nanoemulsions can be a promising drug delivery system. [Display omitted] •Gel-in-water (G/W) nanoemulsion was developed for hydrophobic drug delivery.•12-HSA forms the inner gel phase of G/W and ensures high encapsulation efficiency.•G/W was found biocompatible to primary rat hepatocytes in vitro.•Paclitaxel loaded G/W showed cytotoxicity against cancer both in vitro and in vivo.</description><identifier>ISSN: 0928-4931</identifier><identifier>EISSN: 1873-0191</identifier><identifier>DOI: 10.1016/j.msec.2021.112076</identifier><identifier>PMID: 33947568</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Anticancer properties ; Antitumor agents ; Bioavailability ; Castor oil ; Chemotherapy ; Cytotoxicity ; Drug delivery ; Drug Delivery Systems ; Emulsions ; Gel-in-water ; Hepatocytes ; Hydrophobic drug ; Hydrophobicity ; Materials science ; Melanoma ; Metabolism ; Nanoemulsion ; Nanoemulsions ; Nanoparticles ; Organogel ; Paclitaxel ; Particle Size ; Polydispersity ; Polyoxyethylene ; Side effects ; Stability ; Surface-Active Agents ; Water ; Zeta potential</subject><ispartof>Materials Science &amp; Engineering C, 2021-05, Vol.124, p.112076-112076, Article 112076</ispartof><rights>2021 Elsevier B.V.</rights><rights>Copyright © 2021 Elsevier B.V. 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subjects Anticancer properties
Antitumor agents
Bioavailability
Castor oil
Chemotherapy
Cytotoxicity
Drug delivery
Drug Delivery Systems
Emulsions
Gel-in-water
Hepatocytes
Hydrophobic drug
Hydrophobicity
Materials science
Melanoma
Metabolism
Nanoemulsion
Nanoemulsions
Nanoparticles
Organogel
Paclitaxel
Particle Size
Polydispersity
Polyoxyethylene
Side effects
Stability
Surface-Active Agents
Water
Zeta potential
title Development and characterization of gel-in-water nanoemulsion as a novel drug delivery system
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