1. Folate-decorated PEG-PLGA nanoparticles with silica shells for capecitabine controlled and targeted delivery.
- Author
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Wei K, Peng X, and Zou F
- Subjects
- Capecitabine, Delayed-Action Preparations administration & dosage, Delayed-Action Preparations chemistry, Delayed-Action Preparations metabolism, Deoxycytidine administration & dosage, Deoxycytidine chemistry, Deoxycytidine metabolism, Fluorouracil administration & dosage, Fluorouracil chemistry, Fluorouracil metabolism, Folic Acid administration & dosage, Folic Acid metabolism, Nanoparticles administration & dosage, Nanoparticles metabolism, Polyesters administration & dosage, Polyesters metabolism, Polyethylene Glycols administration & dosage, Polyethylene Glycols metabolism, Silicon Dioxide administration & dosage, Silicon Dioxide metabolism, Deoxycytidine analogs & derivatives, Drug Delivery Systems methods, Fluorouracil analogs & derivatives, Folic Acid chemistry, Nanoparticles chemistry, Polyesters chemistry, Polyethylene Glycols chemistry, Silicon Dioxide chemistry
- Abstract
Di-block polymer of poly (lactic-co-glycolic acid)-poly (ethylene glycol) (PLGA-PEG) end-capped with capecitabine (CAP) at the hydrophobic domain and folate (FA) at hydrophilic domain were synthesized respectively. The products were extensively studied by nuclear magnetic resonance ((1)H NMR) and gel permeation chromatography (GPC) measurement. By using emulsion-solvent evaporation method, the two conjugates, drug CAP and tetramethoxysilane (TMOS) were mixed to form the CAP entrapped nanoparticles (NPs) with the FA moieties exposed on NPs surface, while simultaneously forming a cross-linked silica shell out of hydrophobic PLGA core domain. The testing results showed the CAP-loaded NPs presented suitable physical stability, favorable size around 200 nm, negative zeta potential charge (-28.43 ± 2.55 mV) and high encapsulation efficiency (69%). Both silica shell cross-linked drug-loaded NPs (SSCL NPs) and none silica shell cross-linked NPs (NSSCL NPs) provided an initial burst release and followed by a sustained two-stage release of the CAP. Straight lines approximate the steady-state for the two-stage release, and the K/K' of the two stages are 1.96304 and 1.78697 respectively suggesting the silica shell influenced the release of first stage significantly., (Copyright © 2014 Elsevier B.V. All rights reserved.)
- Published
- 2014
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