title: Preparation, in vitro and in vivo evaluation of mPEG-PLGA nanoparticles co-loaded with syringopicroside and hydroxytyrosol.
abstract: This study investigated the therapeutic efficiency of monomethoxy polyethylene glycol-poly(lactic-co-glycolic acid) (mPEG-PLGA) co-loaded with syringopicroside and hydroxytyrosol as a drug with effective targeting and loading capacity as well as persistent circulation in vivo. The nanoparticles were prepared using a nanoprecipitation method with mPEG-PLGA as nano-carrier co-loaded with syringopicroside and hydroxytyrosol (SH-NPs). The parameters like in vivo pharmacokinetics, biodistribution in vivo, fluorescence in vivo endomicroscopy, and cellular uptake of SH-NPs were investigated. Results showed that the total encapsulation efficiency was 32.38 ± 2.76 %. Total drug loading was 12.01 ± 0.42 %, particle size was 91.70 ± 2.11 nm, polydispersity index was 0.22 ± 0.01, and zeta potential was -24.5 ± 1.16 mV for the optimized SH-NPs. The nanoparticle morphology was characterized using transmission electron microscopy, which indicated that the particles of SH-NPs were in uniformity within the nanosize range and of spherical core shell morphology. Drug release followed Higuchi kinetics. Compared with syringopicroside and hydroxytyrosol mixture (SH), SH-NPs produced drug concentrations that persisted for a significantly longer time in plasma following second-order kinetics. The nanoparticles moved gradually into the cell, thereby increasing the quantity. ALT, AST, and MDA levels were significantly lower on exposure to SH-NPs than in controls. SH-NPs could inhibit the proliferation of HepG2.2.15 cells and could be taken up by HepG2.2.15 cells. The results confirmed that syringopicroside and hydroxytyrosol can be loaded simultaneously into mPEG-PLGA nanoparticles. Using mPEG-PLGA as nano-carrier, sustained release, high distribution in the liver, and protective effects against hepatic injury were observed in comparison to SH.
authors.affiliation: College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, 150000, China.
authors.forename: Qingxia
authors.initials: Q
authors.lastname: Guan
authors.affiliation: College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, 150000, China.
authors.forename: Shuang
authors.initials: S
authors.lastname: Sun
authors.affiliation: College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, 150000, China.
authors.forename: Xiuyan
authors.initials: X
authors.lastname: Li
authors.affiliation: College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, 150000, China.
authors.forename: Shaowa
authors.initials: S
authors.lastname: Lv
authors.affiliation: College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, 150000, China.
authors.forename: Ting
authors.initials: T
authors.lastname: Xu
authors.affiliation: College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, 150000, China.
authors.forename: Jialin
authors.initials: J
authors.lastname: Sun
authors.affiliation: College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, 150000, China.
authors.forename: Wenjing
authors.initials: W
authors.lastname: Feng
authors.affiliation: College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, 150000, China.
authors.forename: Liang
authors.initials: L
authors.lastname: Zhang
authors.affiliation: College of Pharmacy, Heilongjiang University of Chinese Medicine, Harbin, 150000, China. Liyongji2009@163.com.
authors.forename: Yongji
authors.initials: Y
authors.lastname: Li
mesh_terms: D000818:Animals; D056486:Chemical and Drug Induced Liver Injury / Q000517:prevention & control; D004337:Drug Carriers / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D004353:Drug Evaluation, Preclinical; D005260:Female; D006027:Glycosides / Q000008:administration & dosage*; D056945:Hep G2 Cells; D006801:Humans; D008297:Male; D008422:Materials Testing; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D010626:Phenylethyl Alcohol / Q000008:administration & dosage / Q000031:analogs & derivatives*; D011091:Polyesters / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D011092:Polyethylene Glycols / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
chemical_list: D004337:Drug Carriers; D006027:Glycosides; D011091:Polyesters; C558447:methoxypolyethyleneglycol-poly(lactic-co-glycolic acid); C005975:3,4-dihydroxyphenylethanol; C038066:syringopicroside; D011092:Polyethylene Glycols; D010626:Phenylethyl Alcohol