title: Doxorubicin hydrochloride-oleic acid conjugate loaded nanostructured lipid carriers for tumor specific drug release.
abstract: The hydrophilic drug Doxorubicin hydrochloride (DOX) paired with oleic acid (OA) was successfully incorporated into nanostructured lipid carriers (NLCs) by a high-pressure homogenization (HPH) method. Drug nanovehicles with proper physico-chemical characteristics (less than 200nm with narrow size distribution, spherical shape, layered internal organization, and negative electrical charge) were prepared and characterized by dynamic light scattering, zeta potential measurements, transmission electron microscopy, small-angle X-ray scattering and differential scanning calorimetry. The drug loading and entrapment efficiency of DOX-OA/NLCs were 4.09% and 97.80%, respectively. A pH-dependent DOX release from DOX-OA/NLCs, i.e., fast at pH 3.8 and 5.7 and sustained at pH 7.4, was obtained. A cytotoxicity assay showed that DOX-OA/NLCs had comparable cytotoxicity to pure DOX and were favorably taken up by HCT 116 cells. The intracellular distribution of DOX was also studied using a confocal laser scanning microscope. All of these results demonstrated that DOX-OA/NLCs could be a promising drug delivery system with tumor-specific DOX release for cancer treatment.
authors.affiliation: Shanghai Key Laboratory of Functional Materials Chemistry, State Key Laboratory of Bioreactor Engineering and Institute of Applied Chemistry, East China University of Science and Technology, Shanghai 200237, PR China.
authors.forename: Shuangni
authors.initials: S
authors.lastname: Zhao
authors.affiliation: State Key Laboratory of Bioreactor Engineering & Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, PR China; NTT Hi-Technology Institute, Nguyen Tat Thanh University, District 4, Ho Chi Minh City, Viet Nam.
authors.forename: Le Van
authors.initials: LV
authors.lastname: Minh
authors.affiliation: National Center for Protein Science Shanghai and Shanghai Institute of Biochemistry and Cell Biology, Shanghai 200237, PR China.
authors.forename: Na
authors.initials: N
authors.lastname: Li
authors.affiliation: Helmholtz-Zentrum Geesthacht: Centre for Materials and Coastal Research, Institute of Materials Research, Max-Planck-Strasse 1, 21502 Geesthacht, Germany.
authors.forename: Vasil M
authors.initials: VM
authors.lastname: Garamus
authors.affiliation: Helmholtz-Zentrum Geesthacht: Centre for Materials and Coastal Research, Institute of Polymer Research, Max-Planck-Strasse 1, 21502 Geesthacht, Germany.
authors.forename: Ulrich A
authors.initials: UA
authors.lastname: Handge
authors.affiliation: State Key Laboratory of Bioreactor Engineering & Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, PR China.
authors.forename: Jianwen
authors.initials: J
authors.lastname: Liu
authors.affiliation: National Center for Protein Science Shanghai and Shanghai Institute of Biochemistry and Cell Biology, Shanghai 200237, PR China.
authors.forename: Rongguang
authors.initials: R
authors.lastname: Zhang
authors.affiliation: Helmholtz-Zentrum Geesthacht: Centre for Materials and Coastal Research, Institute of Materials Research, Max-Planck-Strasse 1, 21502 Geesthacht, Germany.
authors.forename: Regine
authors.initials: R
authors.lastname: Willumeit-Römer
authors.affiliation: Shanghai Key Laboratory of Functional Materials Chemistry, State Key Laboratory of Bioreactor Engineering and Institute of Applied Chemistry, East China University of Science and Technology, Shanghai 200237, PR China. Electronic address: aihuazou@ecust.edu.cn.
authors.forename: Aihua
authors.initials: A
authors.lastname: Zou
mesh_terms: D004317:Doxorubicin / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D049329:Nanostructures / Q000737:chemistry*; D019301:Oleic Acid / Q000737:chemistry*
chemical_list: D019301:Oleic Acid; D004317:Doxorubicin
keywords: DOX; NLCs; Oleic acid; SAXS; pH-dependent drug release