1. Synthesis and Characterization of Hybrid Polymer/Lipid Expansile Nanoparticles: Imparting Surface Functionality for Targeting and Stability.
- Author
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Stolzoff M, Ekladious I, Colby AH, Colson YL, Porter TM, and Grinstaff MW
- Subjects
- Antineoplastic Agents chemistry, Antineoplastic Agents pharmacokinetics, Cell Line, Tumor, Cell Survival drug effects, Chemistry, Pharmaceutical, Drug Delivery Systems, Folic Acid chemistry, HeLa Cells, Humans, Paclitaxel chemistry, Particle Size, Surface Properties, Antineoplastic Agents chemical synthesis, Folic Acid pharmacokinetics, Lipids chemistry, Nanoparticles chemistry, Paclitaxel pharmacokinetics, Polyethylene Glycols chemistry
- Abstract
The size, drug loading, drug release kinetics, localization, biodistribution, and stability of a given polymeric nanoparticle (NP) system depend on the composition of the NP core as well as its surface properties. In this study, novel, pH-responsive, and lipid-coated NPs, which expand in size from a diameter of approximately 100 to 1000 nm in the presence of a mildly acidic pH environment, are synthesized and characterized. Specifically, a combined miniemulsion and free-radical polymerization method is used to prepare the NPs in the presence of PEGylated lipids. These PEGylated-lipid expansile NPs (PEG-L-eNPs) combine the swelling behavior of the polymeric core of expansile NPs with the improved colloidal stability and surface functionality of PEGylated liposomes. The surface functionality of PEG-L-eNPs allows for the incorporation of folic acid (FA) and folate receptor-targeting. The resulting hybrid polymer/lipid nanocarriers, FA-PEG-L-eNPs, exhibit greater in vitro uptake and potency when loaded with paclitaxel compared to nontargeted PEG-L-eNPs.
- Published
- 2015
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