Preparation and pharmacodynamics of niclosamide micelles

Niclosamide (NIC) has been found to have outstanding antitumour activity in recent years, but its clinical application has been limited by its poor water solubility. In this study, nanomicelles (PEG2K-Fmoc-Ibuprofen micelles, PEG2K-FIbu) were prepared as carriers to improve the solubility and bioavailability of NIC. Nuclear magnetic resonance (NMR) confirmed its successful preparation. The drug-carrying micelles (PEG2K-FIbu/NIC) were then prepared using a thin film dispersion method. PEG2K-FIbu and PEG2K-FIbu/NIC were analysed in detail in terms of particle size, polymer dispersion index, stability and encapsulation efficiency. Finally, the in vivo effects of PEG2K-FIbu/NIC were tested in a mouse liver cancer model. The particle size of PEG2K-FIbu was 11.11 nm. The encapsulation rate was 70.4% and the tumour inhibition rate was 55.98%. Tumours were significantly reduced and damage to the liver was greatly reduced. The histopathological sections and serum biochemical indices also showed that the symptoms were significantly improved after administration. In summary, PEG2K-FIbu/NIC is a potential drug delivery system of NIC to effectively treat liver cancer, providing an effective dosage form for NIC.