US 10,864,170 B2Granted

Polymeric bile acid nanocompositions targeting the pancreas and colon

AssigneeYale University

InventorsTarek M. Fahmy, Jung Seok Lee, Dongin Kim

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Abstract

Pharmaceutical composition containing poly(bile) acid (PBA) polymers for oral delivery of agent(s) show enhanced uptake by the pancreas, liver, and colon. These nanoparticles show significant retention in the pancreas and colon and are therefore useful for selective delivery. The examples demonstrate efficacy of oral administration of insulin to treat diabetes, and oral induction of tolerance by administration of insulin or ovalbumin in combination with rapamycin. Diabetic animals treated with the insulin or insulin with rapamycin showed normalization of blood glucose levels.

Claims25

Dependent claims

A formulation of nanoparticles comprising a polymeric matrix formed of polymers consisting of esterified bile acid monomers (PBA polymers),

wherein the bile acid monomers have a structure of Formula I,
wherein R1, R2, and R3 are independently hydrogen or —OH, and X is —OH or —O−,
or are selected from the group of taurine or glycine conjugates thereof consisting of glycocholic acid, taurocholic acid, glycodeoxycholic acid, taurodeoxycholic acid, taurolitholic acid, taurochenodeoxycholic acid, tauroursodeoxycholic acid, glycolithocholic acid, glycochenodeoxycholic acid;
or taurine conjugates of 3-alpha-7-alpha-12-alpha-22-xi-tetrahydroxy-5-beta-cholestan-26-oic acid or taurine conjugates of 3-alpha-12-alpha-22 xitrihydroxy-5-beta-cholestan-26-oic acid,
wherein the PBA polymers have a molecular weight between 500 Da and 250,000 Da,
wherein the nanoparticles comprise one or more therapeutic, prophylactic or diagnostic agents encapsulated within or entrapped in to the PBA polymers.

3 more elements

Dependencies are inferred from the claim text.

Facts

Application: 15/757,608Filed 2 Sep 2016 · us provisional application
Priority: 4 Sep 2015
Published: US 2018/0243226 A130 Aug 2018
Granted: 15 Dec 2020
Term ends: Not estimatedThe source records don’t support an estimate.

Classification17 codes

A61K 9/5146
Organic macromolecular compounds; Dendrimers: obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g.…
A61K 9/0053
Galenical forms characterised by the site of application: mouth and digestive tract, i.e. intraoral and peroral administration
A61K 9/0095
Galenical forms not covered by A61K9/02 - A61K9/7023: drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets…
A61K 9/08
Medicinal preparations characterised by special physical form: solutions

Family

Application62/214,648Us provisional application · filed 4 Sep 2015
US 2018/0243226 A1Pre-grant publication · published 30 Aug 2018
US 10,864,170 B2This patent

From the US filing history. Foreign family members aren’t listed.

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