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%.

CONCLUSION:

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: Qingyong Li, Chen Liu, Xiuhua Zhao, Yuangang Zu, Ying Wang, Baoyou Zhang, Dongmei Zhao, Qi Zhao, Lin Su, Yang Gao, Baihe Sun
• Journal: International journal of nanomedicine (Int J Nanomedicine) Vol. 6 Pg. 397-405 ( 2011) ISSN: 1178-2013 [Electronic] New Zealand
• PMID: 21499429 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents, Phytogenic
• Drug Carriers
• Fluorescent Dyes
• Serum Albumin
• Folic Acid
• 10-hydroxycamptothecin
• Fluorescein-5-isothiocyanate
• Camptothecin

Topics

• Antineoplastic Agents, Phytogenic (administration & dosage, pharmacokinetics)
• Calorimetry, Differential Scanning
• Camptothecin (administration & dosage, analogs & derivatives, pharmacokinetics)
• Cell Line, Tumor
• Chemistry, Pharmaceutical
• Drug Carriers (chemistry)
• Drug Delivery Systems
• Fluorescein-5-isothiocyanate
• Fluorescent Dyes
• Folic Acid (chemistry)
• Humans
• Microscopy, Confocal
• Microscopy, Electron, Scanning
• Nanomedicine
• Nanoparticles (administration & dosage, chemistry, ultrastructure)
• Particle Size
• Serum Albumin (administration & dosage)
• X-Ray Diffraction