title: Preparation, characterization and targeting of micronized 10-hydroxycamptothecin-loaded folate-conjugated human serum albumin nanoparticles to cancer cells.
abstract: BACKGROUND
  The purpose of this study was to develop a method for targeted delivery of 10-hydroxycamptothecin (HCPT)-loaded nanoparticles (NPs) to cancer cells.
  
  
  METHODS
  We first used a supercritical antisolvent process to prepare micronized HCPT (nHCPT), and then folate-conjugated human serum albumin (HSA) nHCPT-loaded NPs (FA-HSA-nHCPT-NPs) were prepared using a NP-coated method combined with a desolvation technique. The amount of folate conjugation was 16 μg · mg(-1) HSA.
  
  
  RESULTS
  The particle size of the spherical nHCPT microparticles obtained was 118.5 ± 6.6 nm. The particle size and zeta potential of the FA-HSA-nHCPT-NPs were 233.9 ± 1.2 nm and -25.23 ± 2.98 mV, respectively. The FA-HSA-nHCPT-NPs exhibited a smooth surface and a distinct spherical shape, and the results of differential scanning calorimetry and X-ray diffraction indicated that the FA-HSA-nHCPT-NPs presented in a nanostructured amorphous state. The FA-HSA-nHCPT-NPs showed sustained-release characteristics for 120 hours in vitro, with a drug-loading content of 7.3% and an encapsulating efficiency of 79.1%.
  
  
  CONCLUSIONS
  The FA-NPs were effective delivery systems for uptake by SGC7901 cells compared with folate-free NPs. These results suggest that a NP-coated method combined with a desolvation technique is effective for preparing NPs with drugs having poor solubility in water and most organic solvents, using albumin as the wall material. FA-HSA-NPs are a stable delivery system and have the potential for targeted delivery of anticancer drugs.
authors.affiliation: Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin, Heilongjiang, People's Republic of China.
authors.forename: Qingyong
authors.initials: Q
authors.lastname: Li
authors.forename: Chen
authors.initials: C
authors.lastname: Liu
authors.forename: Xiuhua
authors.initials: X
authors.lastname: Zhao
authors.forename: Yuangang
authors.initials: Y
authors.lastname: Zu
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.forename: Baoyou
authors.initials: B
authors.lastname: Zhang
authors.forename: Dongmei
authors.initials: D
authors.lastname: Zhao
authors.forename: Qi
authors.initials: Q
authors.lastname: Zhao
authors.forename: Lin
authors.initials: L
authors.lastname: Su
authors.forename: Yang
authors.initials: Y
authors.lastname: Gao
authors.forename: Baihe
authors.initials: B
authors.lastname: Sun
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D002166:Camptothecin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D016650:Fluorescein-5-isothiocyanate; D005456:Fluorescent Dyes; D005492:Folic Acid / Q000737:chemistry; D006801:Humans; D018613:Microscopy, Confocal; D008855:Microscopy, Electron, Scanning; D050997:Nanomedicine; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry / Q000648:ultrastructure; D010316:Particle Size; D012709:Serum Albumin / Q000008:administration & dosage*; D014961:X-Ray Diffraction
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D005456:Fluorescent Dyes; D012709:Serum Albumin; D005492:Folic Acid; C028098:10-hydroxycamptothecin; D016650:Fluorescein-5-isothiocyanate; D002166:Camptothecin