Nanoparticle-insulin and insulin analogue compositions

摘要

The present invention relates to insulin- and insulin analog-carrying nanoparticles formulated together with or for use with free insulin or with an insulin analog, such as a rapidly-acting insulin analog. The compositions of the present invention find use in medicine, particularly in glycemic control, e.g. for controlling blood glucose levels in diabetic subjects. Nanoparticle compositions of the invention, formulated together with or for use with free insulin or with an insulin analog, comprise a nanoparticle comprising a core comprising a metal and/or a semiconductor; and a corona comprising a plurality of ligands covalently linked to the core, wherein said plurality of ligands comprise at least one carbohydrate moiety; and at least one insulin peptide and/or insulin analog peptide that is non-covalently bound to the corona.

主权项

1. A pharmaceutical composition comprising:
(i) a free insulin analogue peptide selected from the group consisting of: insulin lispro, insulin aspart, and insulin glulisine; and (ii) a plurality of nanoparticles, each of said nanoparticles comprising:
(a) a core comprising a metal and/or a semiconductor;(b) a corona comprising a plurality of ligands covalently linked to the core, wherein at least one of said ligands comprises a carbohydrate moiety; and(c) at least one insulin non-covalently bound to the corona,wherein the molar ratio of free insulin analogue peptide to the nanoparticle-bound insulin is in the range 1:1 to 100:1, and wherein the nanoparticle-bound insulin induces an increase in plasma adrenalin concentration and/or plasma growth hormone concentration upon administration to a mammalian subject.