In situ self-assembly nanoparticles for Oral Docetaxel

Docetaxel (DTX) is a chemotherapy drug that can be used for different type of cancers. Due to polysorbate 80, the excipient in the formulation, acute hypertensivity reaction is observed after intravenous administration. The development of oral formulation for DTX has always been problematic as the bioavailability of the drug is shown to be low due to P-glycoprotein efflux transporters and the intestinal metabolism by CYP3A4 enzymes. The objective of this study is to develop novel DTX in situ self-assembly (ISNP) granules to enhance bioavailability of DTX for oral administration.

Method: The novel nanoformulation of DTX was developed by nanotechnology utilizing the proportional ratio of the components of D-a-tocopheryl polyethylene glycol 1000 succinate (TPGS), Miglyol 812, Aeropearl 300 and DTX. The particle size, drug loading and drug entrapment efficiency of the nanoparticles (NPs) were characterized using high-performance liquid chromatography and Delsa Nano C Particle Size Analyzer.

Results: The proportional ratio among the components, which optimized the drug loading and drug entrapment efficiency, was successfully identified. The drug loading and entrapment efficiency of DTX delivered in ISNP were 10% and 85% respectively. The particle size of DTX ISNPs was achieved to be around 150 nm with the polydispersity index less than 0.3.

Conclusion: DTX ISNPs were successfully developed with the composition that delivers the optimal drug loading and drug entrapment efficiency. Novel DTX ISNPs could enhance the absorption and bioavailability of the drug for oral administration as well as reduces the risk of acute hypersensitivity reactions, which improves patient adherence and reduces hospitalization.

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