title: Quercetin-loaded poly (lactic-co-glycolic acid)-d-α-tocopheryl polyethylene glycol 1000 succinate nanoparticles for the targeted treatment of liver cancer.
abstract: Utilization of quercetin (QT) in clinics is limited by its instability and poor solubility. To overcome these disadvantages, we prepared QT as QT-loaded PLGA-TPGS nanoparticles (QPTN) and examined its properties and therapeutic efficacy for liver cancer. QT-loaded PLGA nanoparticles (QPN) and QT/coumarin-6-loaded PLGA-TPGS nanoparticles (QCPTN) with coumarin-6 as a fluorescent marker were also prepared to investigate the cellular uptake by HepG2 and HCa-F cells using a confocal laser scanning microscope (CLSM), and their effects on apoptosis of HepG2 cells were assessed with flow cytometry. The results measured using transmission electron microscopy, scanning electron microscopy and size analyses indicated that QPTN were stably dispersed sphere with diameter in the range of 100-200 nm. It indicated that the QT loading and encapsulation efficiency in QPTN reached 21.63% and 93.74%, respectively, and the accumulative drug release of QPTN was 85.8%, the QCPTN uptake in HCa-F and HepG2 cells were 50.87% and 61.09% using HPLC analysis, respectively. The results determined using an Annexin-PI flow cytometry indicated that QPTN could induce HepG2 cell apoptosis in a dose dependent manner. The results of histological examination and HPLC analysis confirmed that QPTN was targeted to liver cells. In vivo analysis using solid tumor-bearing mouse model indicated that QPTN could suppress tumor growth by 59.07%. Moreover, all the studied properties of QPTN were more desirable than those of QT-loaded PLGA nanoparticles (QPN). In conclusion, QPTN could be used as a potential intravenous dosage form for the treatment of liver cancer owing to the enhanced pharmacological effects of QT with increased liver targeting.
authors.affiliation: a College of Pharmacy, Dalian Medical University , Dalian , China and.
authors.forename: Xin
authors.initials: X
authors.lastname: Guan
authors.affiliation: a College of Pharmacy, Dalian Medical University , Dalian , China and.
authors.forename: Meng
authors.initials: M
authors.lastname: Gao
authors.affiliation: b College of Basic Medical Sciences, Dalian Medical University , Dalian , China.
authors.forename: Hong
authors.initials: H
authors.lastname: Xu
authors.affiliation: b College of Basic Medical Sciences, Dalian Medical University , Dalian , China.
authors.forename: Chenghong
authors.initials: C
authors.lastname: Zhang
authors.affiliation: a College of Pharmacy, Dalian Medical University , Dalian , China and.
authors.forename: Hongyan
authors.initials: H
authors.lastname: Liu
authors.affiliation: a College of Pharmacy, Dalian Medical University , Dalian , China and.
authors.forename: Li
authors.initials: L
authors.lastname: Lv
authors.affiliation: a College of Pharmacy, Dalian Medical University , Dalian , China and.
authors.forename: Sa
authors.initials: S
authors.lastname: Deng
authors.affiliation: a College of Pharmacy, Dalian Medical University , Dalian , China and.
authors.forename: Dongyan
authors.initials: D
authors.lastname: Gao
authors.affiliation: a College of Pharmacy, Dalian Medical University , Dalian , China and.
authors.forename: Yan
authors.initials: Y
authors.lastname: Tian
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry; D017209:Apoptosis / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D056945:Hep G2 Cells; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D008113:Liver Neoplasms / Q000188:drug therapy*; D051379:Mice; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011794:Quercetin / Q000008:administration & dosage* / Q000737:chemistry*; D013386:Succinates / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D013386:Succinates; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D011794:Quercetin; C000595209:polyethylene glycol 1000
keywords: HepG2 cells; PLGA-TPGS nanoparticles; liver cancer; quercetin; targeting property