Expansile crosslinked polymersome for pH-sensitive delivery of anticancer drugs

Patent metadata

Field	Value
Publication number	US-10188606-B2
Application number	US-201715728181-A
Country	US
Kind code	B2
Filing date	Oct 9, 2017
Priority date	Oct 7, 2016
Publication date	Jan 29, 2019
Grant date	Jan 29, 2019

Abstract

This disclosure relates to polymersomes comprising a crosslinked polymer and their use as drug delivery vehicles. Specifically, polymersomes comprising a polymer of Formula I:

wherein each R is independently C 1-6 alkyl; and n is an integer between 1 and 50.

First claim

What is claimed is:

1. A polymer of Formula (I):

wherein:
each R is independently C1-6 alkyl; and
n is an integer between 1 and 50.

2. The polymer of claim 1 , wherein n is an integer between 10 and 30.

3. The polymer of claim 2 , wherein n is an integer between 15 and 25.

4. The polymer of claim 3 , wherein n is 20.

5. The polymer of claim 1 , wherein each R is methyl.

6. A polymersome comprising a polymer of Formula (I):

wherein:
each R is independently C1-6 alkyl;
n is an integer between 1 and 50.

7. The polymersome of claim 6 , wherein the polymer of Formula (I) is crosslinked.

8. The polymersome of claim 6 , wherein the polymersome further comprises a therapeutic agent.

9. The polymersome of claim 6 , wherein the polymersome further comprises a hydrophilic anticancer agent.

10. The polymersome of claim 9 , wherein the hydrophilic anticancer agent is selected from the group consisting of doxorubicin, paclitaxel, 5-fluoroucacil, 6-mercaptopurine, cyclophosphamide, bleomycin, daunorubicin, epirubicin, methotrexate, vinblastine, homoharringtonine, actinomycin-D, mitocycin-c, and etoposide.

11. The polymersome of claim 10 , wherein the hydrophilic anticancer agent is doxorubicin.

12. The polymersome of claim 6 , wherein n is an integer between 10 and 30.

13. The polymersome of claim 12 , wherein n is an integer between 15 and 25.

14. The polymersome of claim 13 , wherein n is 20.

15. The polymersome of claim 6 , wherein each R is methyl.

16. The polymersome of claim 6 , wherein the diameter of the polymersome is about 50 to about 150 nm.

17. The polymersome of claim 16 , wherein the average diameter of the polymersome is about 90 to about 120 nm.

18. A pharmaceutical composition comprising a polymersome of claim 6 , and a pharmaceutically acceptable excipient.

19. A method of treating cancer in a patient, the method comprising administering to the patient a therapeutically effective amount of a polymersome of claim 6 .

20. A method for administering a therapeutic agent to a patient in need thereof, the method comprising administering to the patient a polymersome of claim 6 .

Assignees

• Mayo Found Medical Education & Res

Inventors

• Liu Xifeng
• Yaszemski Michael J
• Lu Lichun

Classifications

• A61K9/0019

  Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00) · CPC title

• A61K9/1273 Primary

  Polymersomes; Liposomes with polymerisable or polymerised bilayer-forming substances · CPC title

• C08G65/337

  containing other elements (organic compounds containing halogens only as halides of a carboxyl group C08G65/332) · CPC title

• C08G65/3315

  aromatic · CPC title

• A61K31/704

  attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)} · CPC title