title: 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.
authors.affiliation: a Centre for Bioinformatics, School of Life Sciences , Pondicherry University , Kalapet , Puducherry , India.
authors.forename: Sailu
authors.initials: S
authors.lastname: Sarvagalla
authors.affiliation: b Institute of Biotechnology and Pharmaceutical Research , National Health Research Institutes , Zhunan , Taiwan , ROC.
authors.forename: Hsing Pang
authors.initials: HP
authors.lastname: Hsieh
authors.affiliation: a Centre for Bioinformatics, School of Life Sciences , Pondicherry University , Kalapet , Puducherry , India.
authors.forename: Mohane Selvaraj
authors.initials: MS
authors.lastname: Coumar
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D064107:Aurora Kinase B / Q000037:antagonists & inhibitors; D003692:Delayed-Action Preparations; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D065546:Drug Liberation; D006801:Humans; D053758:Nanoparticles; D010755:Organophosphates / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D010330:Patents as Topic; D011108:Polymers / Q000737:chemistry*; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D011799:Quinazolines / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology
chemical_list: C520647:2-((3-((4-((5-(2-((3-fluorophenyl)amino)-2-oxoethyl)-1H-pyrazol-3-yl)amino)quinazolin-7-yl)oxy)propyl)(ethyl)amino)ethyl dihydrogen phosphate; D000970:Antineoplastic Agents; D003692:Delayed-Action Preparations; D010755:Organophosphates; D011108:Polymers; D047428:Protein Kinase Inhibitors; D011799:Quinazolines; D064107:Aurora Kinase B
keywords: AZD1152; AZD1152-hqpa; Aurora kinase inhibitor; cancer; drug delivery; nano-formulation; nano-medicine; nanoparticle; nanotechnology; therapeutic index