IP Library › Granted Patent US 8,062,663
Granted Patent B2
US 8,062,663 · App. 12/466,011 · Granted Nov 22, 2011

Methods and compostions for enhancing transdermal drug delivery

Assignee: National Health Research Instittues
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Quick Facts
Patent No.
US 8,062,663
App. No.
12/466,011
Granted
Nov 22, 2011
Kind
B2
Abstract

Methods and compositions for enhancing transdermal delivery of a bioactive agent. The method contains the step of applying to a skin tissue an effective amount of a composition comprising: (a) a drug vehicle; (b) a bioactive agent encapsulated within the drug vehicle; (c) a plurality of proteolytic enzyme molecules conjugated onto the surface of the drug vehicle; and (d) a pharmaceutically acceptable carrier, for a period of time effective to deliver the bioactive agent across the skin tissue at a desired dosage.

Claims (34)

1. A method for enhancing delivery of a bioactive agent across a skin tissue comprising the step of:

applying an effective amount of a composition comprising:

a) a liposome;

b) a bioactive agent encapsulated within the liposome;

c) a plurality of proteolytic enzyme molecules conjugated onto the surface of the liposome; and

d) a pharmaceutically acceptable carrier,

for a period of time effective to deliver the bioactive agent across the skin tissue at a desired dosage.

2. The method of claim 1 , wherein the composition further comprises a nanoparticle enclosed in the liposome, wherein the bioactive agent is encapsulated within the nanoparticle within the liposome.

3. The method of claim 2 , wherein the nanoparticle is formed from poly(lactic-co-glycolic acid) (PLGA) or hydro-gel.

4. The method of claim 1 , wherein the proteolytic enzyme is papain.

5. The method of claim 4 , wherein the concentration of papain is less than 93, or less than 50, 40 or 30 μg/ml.

6. The method of claim 1 , wherein the proteolytic enzyme is a selected from the group consisting of papain, pancreatin, ficin, bromelain, elastase, pepsin, hyaluronidase, streptokinase, streptodornase, trypsin, chymotrypsin, α-chymotrypsin, α-amylase, deoxyribonuclease, collagenase, sutilain and any combination thereof.

7. The method of claim 1 , wherein the bioactive agent comprises two or more than two types of bioactive agents.

8. The method of claim 7 , wherein the two or more than two types of bioactive agents comprises at least one type of hydrophilic bioactive agent.

9. The method of claim 1 , wherein the bioactive agent is a hormone.

10. A composition for transdermal administration of a bioactive agent comprising:

a) a liposome;

b) a bioactive agent encapsulated within the liposome;

c) a plurality of proteolytic enzyme molecules conjugated onto the surface of the liposome; and

d) a pharmaceutically acceptable carrier,

wherein the proteolytic enzyme is selected from the group consisting of papain, pancreatin, ficin, bromelain, elastase, pepsin, hyaluronidase, streptokinase, streptodornase, trypsin, chymotrypsin, α-chymotrypsin, α-amylase, deoxyribonuclease, collagenase, sutilain and any combination thereof.

11. The composition of claim 10 , wherein the enzyme is papain.

12. The composition of claim 11 , wherein the concentration of papain is less than 93, or less than 50, 40 or 30 μg/ml.

13. The composition of claim 10 , wherein the composition further comprises a nanoparticle enclosed within the liposome, and wherein the bioactive agent is encapsulated within the nanoparticle within the liposome.

14. The composition of claim 13 , wherein the nanoparticle is formed from poly(lactic-co-glycolic acid) (PLGA) nanoparticle or hydro-gel.

15. A composition for transdermal administration of a bioactive agent comprising:

a) a liposome;

b) a bioactive agent encapsulated within the liposome;

c) a plurality of papain molecules conjugated onto the surface of the liposome; and

d) a pharmaceutically acceptable carrier.

16. The composition of claim 15 , wherein the concentration of papain is less than 93, or less than 50, 40 or 30 μg/ml.

17. The composition of claim 15 , wherein the composition further comprises a nanoparticle enclosed within the liposome, and wherein the bioactive agent is encapsulated within the nanoparticle within the liposome.

18. The composition of claim 17 , wherein the nanoparticle is formed from poly(lactic-co-glycolic acid) (PLGA) nanoparticle or hydro-gel.

19. The method of claim 15 , wherein the bioactive agent comprises two or more than two types of bioactive agents.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 14, 2009
From: WANG, YU-JING; WANG, YU-CHAO; WU, YI-TING; TAI, LIN-AI; LO, LEU-WEI; YANG, CHUNG-SHI
To: NATIONAL HEALTH RESEARCH INSTITUTES
Reel/Frame 022685/0813 →
Continuity (2)
Provisional Application 61055784 · May 23, 2008
Related Publication 20090291133A1 · Nov 26, 2009