Bioactive components conjugated to dissolvable substrates of microneedle arrays

Patent metadata

Field	Value
Publication number	US-10737083-B2
Application number	US-201916283667-A
Country	US
Kind code	B2
Filing date	Feb 22, 2019
Priority date	Mar 18, 2015
Publication date	Aug 11, 2020
Grant date	Aug 11, 2020

Abstract

Microneedle arrays and methods of forming the same can include one or more bioactive components bonded to a biocompatible material such that the one or more bioactive components are cleavable in vivo to release the bioactive component from the biocompatible material.

First claim

We claim:

1. A dissolvable microneedle array for transdermal insertion into a patient comprising:
a substrate comprising a biocompatible material that forms base portion and a plurality of microneedles extending from the base portion; and
one or more bioactive components conjugated to the biocompatible material,
wherein the one or more bioactive components are cleavable in vivo to release the bioactive component from the biocompatible material, or the bioactive component retains function when conjugated to the biocompatible material, and
wherein the one or more bioactive components are bonded to the biocompatible material by a disulfide bond.

2. The microneedle array of claim 1 , wherein the biocompatible material is carboxymethylcellulose.

3. The microneedle array of claim 1 , wherein the one or more bioactive components are cleavable in vivo in response to pH, temperature, or both.

4. The microneedle array of claim 1 , wherein the one or more bioactive components comprise Doxorubicin.

5. The microneedle array of claim 4 , wherein the amount of Doxorubicin ranges from about 1 to 1000 μg for chemotherapy.

6. The microneedle array of claim 1 , wherein the one or more bioactive components are in a higher concentration in the plurality of microneedles than in the base portion.

7. The microneedle array of claim 6 , wherein substantially all of the one or more bioactive components are located in the plurality of microneedles so that the base portion is substantially formed without any bioactive components contained therein, the one or more bioactive components are locally concentrated in the plurality of microneedles so that the one or more bioactive components are generally present only in an upper half of respective microneedles in the microneedle array, and each microneedle comprises a plurality of layers of the biocompatible material.

8. The microneedle array of claim 1 , wherein the one or more bioactive components comprise at least two different bioactive components conjugated to the biocompatible material.

9. The microneedle array of claim 8 , wherein the at least two different bioactive components are selected from the group consisting of a chemotherapeutic agent, an adjuvant, and a chemo attractant for a cancer chemo immunotherapy application.

10. The microneedle array of claim 1 , wherein the one or more bioactive component comprises at least one viral vector.

11. The microneedle array of claim 10 , wherein the at least one viral vector comprises an adenovector.

12. A dissolvable microneedle array for transdermal insertion into a patient comprising:
a substrate comprising a biocompatible material that forms base portion and a plurality of microneedles extending from the base portion; and
a first bioactive component conjugated to the biocompatible material, the bioactive component being Doxorubicin,
wherein the first bioactive component is cleavable in vivo to release the first bioactive component from the biocompatible material, or the first bioactive component retains function when conjugated to the biocompatible material, and
wherein the first bioactive component is bonded to the biocompatible material by a disulfide bond.

13. The microneedle array of claim 12 , wherein the biocompatible material is carboxymethylcellulose.

14. The microneedle array of claim 12 , wherein the first bioactive components is cleavable in vivo in response to pH, temperature, or both.

15. The microneedle array of claim 12 , wherein the amount of Doxorubicin ranges from about 1 to 1000 μg for chemotherapy.

16. The microneedle array of claim 12 , further comprising a second bioactive component.

17. The microneedle array of claim 16 , wherein the second bioactive component is selected from the group consisting of Poly-IC or Poly-ICLC.

18. The microneedle array of claim 16 , wherein the second bioactive component is also conjugated to the biocompatible material.

19. The microneedle array of claim 16 , wherein the second bioactive component is mixed into the biocompatible material.

Assignees

• Univ Of Pittsburgh—Of The Commonwealth System Of Higher Education

Inventors

• Falo Jr Louis D
• Erdos Geza

Classifications

• A61M2037/0023

  Drug applicators using microneedles · CPC title

• B29L2031/753

  Medical equipment; Accessories therefor (bloodbags, medical bags B29L2031/7148; artificial eyes B29L2011/0008) · CPC title

• B29K2001/08

  Cellulose derivatives · CPC title

• A61M2037/0053

  Methods for producing microneedles · CPC title

• B29C39/123

  Making multilayered articles · CPC title