title: Preparation and evaluation of paclitaxel-loaded nanoparticle incorporated with galactose-carrying polymer for hepatocyte targeted delivery.
abstract: OBJECTIVE
  Paclitaxel-loaded poly(lactic-co-glycolic acid) (PLGA) nanoparticles incorporated with galactose-carrying polymer poly(vinyl benzyllactonamide) (PVLA) were prepared to facilitate the hepatocyte cell targeted delivery of paclitaxel via ligand-receptor mediated endocytosis. The factors impacting nanoparticle properties, drug release and cellular uptake efficiency were evaluated in vitro.
  
  
  METHODS
  Paclitaxel-loaded nanoparticles incorporated with PVLA were prepared by emulsion solvent evaporation method with polyvinyl alcohol (PVA) as co-emulsifier. The presence of PVLA on the particle surface was investigated through the change of ζ potential and surface hydrophobicity. Cellular uptake and cytotoxic activity, involving factors concerned with them, were evaluated by HepG2 cells in vitro.
  
  
  RESULTS
  The presence of PVLA led to the increase of ζ potential, reduction of the particle surface hydrophobicity, slight promotion of paclitaxel encapsulation efficiency and more homogeneous particle size, but excessive PVLA accelerated the burst release. With enhanced attachment and cellular uptake efficiency, the PVLA incorporated nanoparticles exhibited significant cytotoxicity to HepG2 cells, and particles with higher PVLA-to-PLGA ratio, although had larger size and almost the same cellular uptake efficiency, performed much higher cytotoxic activity due to the larger drug capacity and faster release rate.
authors: Department of Chemical Engineering, Tsinghua University, Beijing, P.R. China.
authors: Yujie
authors: Y
authors: Wang
authors: Guoqiang
authors: G
authors: Jiang
authors: Tingting
authors: T
authors: Qiu
authors: Fuxin
authors: F
authors: Ding
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004339:Drug Compounding; D016503:Drug Delivery Systems; D045703:Emulsifying Agents / Q000737:chemistry; D004705:Endocytosis / Q000187:drug effects; D005690:Galactose / Q000737:chemistry; D056945:Hep G2 Cells; D022781:Hepatocytes / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D007785:Lactose / Q000031:analogs & derivatives* / Q000737:chemistry; D008113:Liver Neoplasms / Q000188:drug therapy*; D053758:Nanoparticles / Q000737:chemistry*; D017239:Paclitaxel / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D010316:Particle Size; D011137:Polystyrenes / Q000737:chemistry*; D011142:Polyvinyl Alcohol / Q000737:chemistry; D012995:Solubility; D013499:Surface Properties
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D045703:Emulsifying Agents; D011137:Polystyrenes; D011142:Polyvinyl Alcohol; C074112:poly-N-4-vinylbenzyllactonamide; D007785:Lactose; D017239:Paclitaxel; D005690:Galactose