Poly(caprolactone)–Pluronic– poly(caprolactone) amphiphilic copolymer nanoparticles for controlled 5-Fluorouracil delivery


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5-Fluorouracil (5-FU), a pyrimidine analogue that interferes with thymidylate synthesis, has a broad spectrum of activity against solid tumors. However, 5-FU has limitations that include a short biological half-life, incomplete and non-uniform oral absorption, toxic side effects on bone marrow and the gastrointestinal tract, and non-selective action against healthy cells. In order to prolong the circulation time of 5-FU and increase its efficacy, numerous researchers have attempted to modify its delivery by use of polymer conjugates or by incorporation of 5-FU into particulate carriers. Recently, nano-sized drug delivery systems (DDS) especially biocompatible and biodegradable polymer nanoparticles have attracted considerable interest since they can offer a suitable means of delivering small molecular weight drugs, proteins or genes to a targeted tissue or organ. PCL is a semi-crystalline, hydrophobic polymer has gained much attention as ideal material for drug delivery and other applications through the decades. However, the high degree of crystallinity and hydrophobicity, PCL degrades rather slowly and less biocompatible with soft tissue limiting its applications. Therefore, the modification of PCL is proposed. Thus, their hydrophilicity, biodegradability and mechanical properties can be improved by attaching hydrophilic moiety to the synthetic polymer. So, in this work amphiphilic triblock copolymers PCL/Pluronic/PCL (CUC series) was synthesized by Lipase B catalyzed ring-opening polymerization of -CL monomer initiated by Pluronic. Nanoparticles were prepared using prepared copolymers by solvent evaporation method. 5- Fluorouracil as a model drug was loaded in these nanoparticles to investigate the drug release behavior. The properties of the prepared nanoparticles were extensively studied by dynamic light scattering (DLS) and transmission electron microscopy (TEM). The particle sizes obtained by dynamic light scattering of these nanoparticles were in the range of 100–115 nm, and increased as the hydrophobic property of the nanoparticles increased. TEM showed that the nanoparticles were in a well-defined spherical shape with a uniform size distribution. We also investigated the entrapment and in vitro release behavior, which indicated that the release speed of 5-FU could be well-controlled and the release half-life period could reach 16.86 h, which was 26.4 times longer than that of pure 5-FU.

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Journal: TechConnect Briefs
Volume: 2, Nanotechnology 2011: Electronics, Devices, Fabrication, MEMS, Fluidics and Computational
Published: June 13, 2011
Pages: 253 - 256
Industry sector: Advanced Materials & Manufacturing
Topics: Advanced Manufacturing, Nanoelectronics
ISBN: 978-1-4398-7139-3