Therapeutic polymeric nanoparticles and the methods of making and using thereof: a patent evaluation of WO2015036792

ABSTRACT

Evaluation of the patent application WO2015036792 claiming therapeutic polymeric nanoparticles loaded with AZD1152-hqpa (aurora kinase inhibitor), and methods of making and using same for the treatment of cancer, is described. The claimed polymeric nano-formulations containing hydrophobic acid significantly improved the pharmacokinetic profiles (slow/sustained drug release profile) of the drug AZD1152-hqpa, as compared to the control agent (AZD1152). Drug efficacy and tolerability were also improved, and toxicity decreased in in vivo animal experiments, resulting in a better therapeutic index for the nano-formulation. Hence, the nano-formulated AZD1152-hqpa could be tested in the clinic at a dose level similar to, or higher than, that used for AZD1152, with lower incidence of toxicity.

KEYWORDS:

• Aurora kinase inhibitor
• drug delivery
• AZD1152
• AZD1152-hqpa
• nanoparticle
• nanotechnology
• cancer
• nano-medicine
• nano-formulation
• therapeutic index

Article highlights

• Nano-formulations containing hydrophobic acid (e.g. cholic acid, sulfo succinic acid) significantly improved drug loading and/or releasing profiles of AZD1152-hqpa.

• The claimed AZD1152-hqpa nano-formulations have equivalent or improved tumor inhibition efficacy at a lower dose, compared to the control agent (AZD1152).

• Nano-formulated AZD1152-hqpa results in lower bone marrow toxicity, as compared to the control agent.

• Nano-fomulated AZD1152-hqpa could be tested in the clinics with a wider safety margin and more convenient dosing schedule due to improved therapeutic index and slow/sustained drug release.

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Declaration of interest

This work was supported by grants (SR/FT/LS-64/2011) of Science & Engineering Research Board, Govt. of India for MS Coumar. S Sarvagalla gratefully acknowledges the Department of Biotechnology, Govt. of India, for a Junior Research Fellowship (DBT-JRF/2012-13/80). HP Hsieh acknowledges financial support from National Health Research Institutes, Taiwan. The authors, MS Coumar and S Sarvagalla are employees of Pondicherry University, India, and HP Hsieh is employee of National Health Research Institutes, Taiwan. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.