Preparation, characterization and targeting of micronized 10-hydroxycamptothecin-loaded folate-conjugated human serum albumin nanoparticles to cancer cells

被引：45

作者：

Li, Qingyong ^{[1
]}

Liu, Chen ^{[1
]}

Zhao, Xiuhua ^{[1
]}

Zu, Yuangang ^{[1
]}

Wang, Ying ^{[1
]}

Zhang, Baoyou ^{[1
]}

Zhao, Dongmei ^{[1
]}

Zhao, Qi ^{[1
]}

Su, Lin ^{[1
]}

Gao, Yang ^{[1
]}

Sun, Baihe ^{[1
]}

机构：

[1] NE Forestry Univ, Minist Educ, Key Lab Forest Plant Ecol, Harbin 150040, Heilongjiang, Peoples R China

来源：

INTERNATIONAL JOURNAL OF NANOMEDICINE | 2011年 / 6卷

关键词：

nanoparticle-coated; desolvation technique; 10-hydroxycamptothecin; human serum albumin; folate; targeted delivery; DRUG-DELIVERY SYSTEM; EVALUATION IN-VITRO; BSA NANOPARTICLES; RECEPTOR; RELEASE; MICROSPHERES; CAMPTOTHECIN; MICELLES; STABILIZATION; STABILITY;

D O I：

10.2147/IJN.S16144

中图分类号：

TB3 [工程材料学];

学科分类号：

0805 ; 080502 ;

摘要：

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 mu g.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.

引用

页码：397 / 405

页数：9

共 39 条

[1] Conjugation of folate via gelonin carbohydrate residues retains ribosomal-inactivating properties of the toxin and permits targeting to folate receptor positive cells [J].