Nanoformulation of paclitaxel to enhance cancer therapy

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Journal titleJournal of Biomaterials Applications
Pages298307; # of pages: 10
SubjectCancer Chemotherapy; Nanoformulation; Paclitaxel; Pluronic copolymers; water-soluble; Chemotherapy; Copolymers; Diseases; Drug delivery; Enzyme inhibition; Loading; Nanoparticles; Synthesis (chemical); Toxicity; Hydrogels; nanocarrier; paclitaxel; phosphate buffered saline; poloxamer; sorbitan palmitate; antineoplastic activity; aqueous solution; article; cancer cell culture; cancer therapy; cell killing; cell strain MCF 7; cell viability; controlled study; cytotoxicity; drug delivery system; drug distribution; drug efficacy; drug formulation; drug solubility; drug structure; drug uptake; HeLa cell; high performance liquid chromatography; IC 50; in vitro study; nanoencapsulation; nanopharmaceutics; nanotoxicology; particle size; physical chemistry; proton nuclear magnetic resonance; scanning electron microscopy; toxicity testing; transmission electron microscopy
AbstractPaclitaxel is a microtubule inhibitor causing mitotic arrest and is widely used in cancer chemotherapy. However, its poor water solubility restricts its direct clinical applications. In this article, we report paclitaxel-loaded nanoparticles that are water soluble and that can improve the drug's bio-distribution and therapeutic efficacy. Paclitaxel-loaded nanoparticles were synthesized by using Pluronic copolymers (F-68 and P-123) and surfactant (Span 40) as nanocarrier. The toxicity and cellular uptake of paclitaxel-loaded nanoparticles were evaluated. The paclitaxel-loaded nanoparticles can completely disperse into phosphate buffer saline to produce a clear aqueous suspension. Based on HPLC analysis, the drug-loading rate is 9.0 ± 0.1% while drug encapsulation efficiency is 99.0 ± 1.0%. The cytotoxicity assay was performed using breast cancer MCF-7 and cervical cancer Hela cells. For MCF-7 cells, the half maximal inhibitory concentrations (IC50) of paclitaxel-loaded nanoparticles and paclitaxel are 8.5 ± 0.3 and 14.0 ± 0.7 ng/mL at 48 hours and 3.5 ± 0.4 and 5.2 ± 0.5 ng/mL at 72 hours across several runs. IC50 of paclitaxel-loaded nanoparticles and paclitaxel for Hela cells are 5.0 ± 0.3 and 8.0 ± 0.3 ng/mL at 48 hours and 2.0 ± 0.1 and 6.5 ± 0.3 ng/mL at 72 hours. In-vitro studies show that the drug's nanoformulation gives obvious enhancements in the drug's efficiency at killing cancer cells over paclitaxel alone. Materials of the nanocarrier used for nanoformulation are approved with low toxicity according to the result of cell studies. Conclusion: paclitaxel-loaded nanoparticles greatly improved the physicochemical properties of paclitaxel without modifying its chemical structure, allowing for deep-site cancer drug delivery and enhancing the drug therapeutic efficiency. © 2012 The Author(s).
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AffiliationNational Research Council Canada (NRC-CNRC); National Institute for Nanotechnology (NINT-INNT)
Peer reviewedYes
NPARC number21269660
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Record identifiera7598d29-2a77-4590-b984-33995bdeea61
Record created2013-12-13
Record modified2016-05-09
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