Abstract
BackgroundNanoparticles have been extensively investigated for targeted delivery of anticancer drugs. Since the folate receptor is universally over-expressed on the tumor cell membrane, folic acid is often used to modify the fate of nanoparticles in biologicals.MethodsTo fabricate targetable nanoparticles, folic acid was conjugated to a pullulan backbone and poly(DL-lactide-co-glycolide) (PLGA) (abbreviated as FAPuLG) was conjugated. KB cells and NIH3T3-cell-bearing mice were prepared to prove folate receptor targeting of FAPuLG nanoparticles.Results and discussionNanoparticles of FAPuLG copolymer that self-assembled in water were small with diameters <200 nm. Doxorubicin (DOX) as a model drug was incorporated into the FAPuLG nanoparticles that were used to treat folate receptor over-expressing KB human carcinoma cells. Fluorescence microscopy revealed that DOX-incorporated FAPuLG nanoparticles induced strong red fluorescence in the KB cells in the absence of folic acid. However, fluorescence intensity was decreased by blocking folate receptors. Antitumor activity of FAPuLG nanoparticles against KB cells in vitro was also decreased by blocking folate receptors. In animal study using near-infrared dye-conjugated FAPuLG nanoparticles, fluorescence intensity was significantly higher at KB solid tumor than that of NIH3T3.ConclusionsThe results indicate that FAPuLG nanoparticles can target the folate receptor of tumor cells. FAPuLG nanoparticles are a promising candidate for active targeting of anticancer agents.
Highlights
Nanoparticles have been extensively investigated for targeted delivery of anticancer drugs
The results indicate that FAPuLG nanoparticles can target the folate receptor of tumor cells
FAPuLG nanoparticles are a promising candidate for active targeting of anticancer agents
Summary
Nanoparticles have been extensively investigated for targeted delivery of anticancer drugs. Nanoparticle-based targeted drug delivery systems have been extensively investigated for biomedical applications [1,2,3,4]. The unique features of nanoscale carriers are their huge surface area versus volume, ease of surface modification, prolonged circulation in the blood through avoidance of the reticuloendothelial system, and small size that facilitates specific interaction with cell surface receptors, enabling the targeting of specific cells or tissues having. The folate receptor is over-expressed in virtually all types of tumor cells, while being barely detectable in healthy tissues and cells [11,12,13]. Nanoparticles having folic acid as a targeting moiety facilitate accumulation of anticancer agents in tumors [14]
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