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Comparing different sterol containing solid lipid nanoparticles for targeted delivery of quercetin in hepatocellular carcinoma.
J Liposome Res. 2014 Sep; 24(3):191-203.JL

Abstract

Quercetin (QT) is a potential chemotherapeutic drug with low solubility that seriously limits its clinical use. The aim of this study was enhancing cellular penetration of QT by sterol containing solid lipid nanoparticles (SLNs) which make bilayers fluent for targeting hepatocellular carcinoma cells. Three variables including sterol type (cholesterol, stigmasterol and stigmastanol), drug and sterol content were studied in a surface response D-optimal design for preparation of QT-SLNs by emulsification solvent evaporation method. The studied responses included particle size, zeta potential, drug loading capacity and 24 h release efficiency (RE24%). Scanning electron and atomic force microscopy were used to study the morphology of QT-SLNs and their thermal behavior was studied by DSC analysis. Cytotoxicity of QT-SLNs was determined by MTT assay on HepG-2 cells and cellular uptake by fluorescence microscopy method. Optimized QT-SLNs obtained from cholesterol and QT with the ratio of 2:1 that showed particle size of 78.0 ± 7.0 nm, zeta potential of -22.7 ± 1.3 mV, drug loading efficiency of 99.9 ± 0.5% and RE24 of 56.3 ± 3.4%. IC50 of QT in cholesterol SLNs was about six and two times less than free QT and phytosterol SLNs, respectively, and caused more accumulation of QT in HepG2 cells. Blank phytosterol SLNs were toxic on cells.

Authors+Show Affiliations

Department of Pharmaceutics, Faculty of Pharmacy and Novel Drug Delivery Systems Research Center, Isfahan University of Medical Sciences , Isfahan , Islamic Republic of Iran.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

24354715

Citation

Varshosaz, Jaleh, et al. "Comparing Different Sterol Containing Solid Lipid Nanoparticles for Targeted Delivery of Quercetin in Hepatocellular Carcinoma." Journal of Liposome Research, vol. 24, no. 3, 2014, pp. 191-203.
Varshosaz J, Jafarian A, Salehi G, et al. Comparing different sterol containing solid lipid nanoparticles for targeted delivery of quercetin in hepatocellular carcinoma. J Liposome Res. 2014;24(3):191-203.
Varshosaz, J., Jafarian, A., Salehi, G., & Zolfaghari, B. (2014). Comparing different sterol containing solid lipid nanoparticles for targeted delivery of quercetin in hepatocellular carcinoma. Journal of Liposome Research, 24(3), 191-203. https://doi.org/10.3109/08982104.2013.868476
Varshosaz J, et al. Comparing Different Sterol Containing Solid Lipid Nanoparticles for Targeted Delivery of Quercetin in Hepatocellular Carcinoma. J Liposome Res. 2014;24(3):191-203. PubMed PMID: 24354715.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Comparing different sterol containing solid lipid nanoparticles for targeted delivery of quercetin in hepatocellular carcinoma. AU - Varshosaz,Jaleh, AU - Jafarian,Abbas, AU - Salehi,Golnaz, AU - Zolfaghari,Behzad, Y1 - 2013/12/20/ PY - 2013/12/21/entrez PY - 2013/12/21/pubmed PY - 2015/4/10/medline KW - Cholesterol KW - hepatocellular carcinoma KW - phytosterols KW - quercetin KW - solid lipid nanoparticles SP - 191 EP - 203 JF - Journal of liposome research JO - J Liposome Res VL - 24 IS - 3 N2 - Quercetin (QT) is a potential chemotherapeutic drug with low solubility that seriously limits its clinical use. The aim of this study was enhancing cellular penetration of QT by sterol containing solid lipid nanoparticles (SLNs) which make bilayers fluent for targeting hepatocellular carcinoma cells. Three variables including sterol type (cholesterol, stigmasterol and stigmastanol), drug and sterol content were studied in a surface response D-optimal design for preparation of QT-SLNs by emulsification solvent evaporation method. The studied responses included particle size, zeta potential, drug loading capacity and 24 h release efficiency (RE24%). Scanning electron and atomic force microscopy were used to study the morphology of QT-SLNs and their thermal behavior was studied by DSC analysis. Cytotoxicity of QT-SLNs was determined by MTT assay on HepG-2 cells and cellular uptake by fluorescence microscopy method. Optimized QT-SLNs obtained from cholesterol and QT with the ratio of 2:1 that showed particle size of 78.0 ± 7.0 nm, zeta potential of -22.7 ± 1.3 mV, drug loading efficiency of 99.9 ± 0.5% and RE24 of 56.3 ± 3.4%. IC50 of QT in cholesterol SLNs was about six and two times less than free QT and phytosterol SLNs, respectively, and caused more accumulation of QT in HepG2 cells. Blank phytosterol SLNs were toxic on cells. SN - 1532-2394 UR - https://www.unboundmedicine.com/medline/citation/24354715/Comparing_different_sterol_containing_solid_lipid_nanoparticles_for_targeted_delivery_of_quercetin_in_hepatocellular_carcinoma_ L2 - https://www.tandfonline.com/doi/full/10.3109/08982104.2013.868476 DB - PRIME DP - Unbound Medicine ER -