IP Library Granted Patent US 11,266,822
Granted Patent B2
US 11,266,822 · App. 16/158,942 · Granted Mar 8, 2022

Microneedle array

Inventor: Toshio Shimada (Ashigarakami-gun, JP)
Assignee: FUJIFILM Corporation
A61M37/0015A61K9/70A61K47/02A61K47/24A61K47/36A61M37/00A61M2037/003A61M2037/0023
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Quick Facts
Patent No.
US 11,266,822
App. No.
16/158,942
Granted
Mar 8, 2022
Kind
B2
Abstract

An object of the present invention is to provide a microneedle array which is capable of suppressing aggregation of liposomes in a case where a water-soluble polymer is mixed with liposomes during production of the microneedle array and is capable of localizing a drug at a tip of a needle. According to the present invention, provided is a microneedle array including: a sheet; and a plurality of needles which are present on an upper surface of the sheet, in which each needle contains a water-soluble polymer, a drug, a liposome, and a salt, a zeta potential of the liposome is −10 mV or less, the zeta potential is a zeta potential of a liquid obtained by diluting the liposome to 0.1 mg/mL with 10 mmol/L of a phosphoric acid aqueous solution having a pH of 7, and a content of the salt in a portion of each needle which contains the liposome is 2.5 mmol/g or less.

Claims (39)

1. A microneedle array comprising:

a sheet; and

a plurality of needles which are present on an upper surface of the sheet,

wherein each needle is formed from a solution which contains a water-soluble polymer, a drug, a liposome, and a salt, and the drug is localized at a tip of the needle,

a zeta potential of the liposome is −10 mV or less,

the zeta potential is a zeta potential of a liquid obtained by diluting the liposome to 0.1 mg/mL with 10 mmol/L of a phosphoric acid aqueous solution having a pH of 7,

a content of the salt in a portion of each needle which contains the liposome is 2.5 mmol/g or less,

the liposome contains an anionic compound,

the anionic compound is at least one selected from the group consisting of phosphatidylglycerol, phosphatidylserine, phosphatidic acid, a lipid containing a polyoxyethylene chain, and a saponin, and

the water-soluble polymer is at least one selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, dextran, dextrin, hydroxyethyl starch, and a cellulose derivative.

2. The microneedle array according to claim 1 ,

wherein the water-soluble polymer is electrically neutral.

3. The microneedle array according to claim 1 ,

wherein the water-soluble polymer is hydroxyethyl starch, and

the liposome contains phosphatidylcholine and distearoyl phosphatidylglycerol.

4. The microneedle array according to claim 1 ,

wherein the drug is a hormone or a vaccine.

5. The microneedle array according to claim 1 ,

wherein the salt is a salt containing at least one selected from the group consisting of a sodium ion, a potassium ion, an ammonium ion, a lithium ion, and a silver ion.

6. The microneedle array according to claim 1 , wherein the zeta potential of the liposome is from −10 mV to −100 mV.

7. The microneedle array according to claim 1 , wherein the content of the salt in a portion of each needle which contains the liposome is from 0.01 mmol/g to 2.5 mmol/g.

8. The microneedle array according to claim 1 , wherein the zeta potential of the liposome is of a value effective to suppress aggregation of liposomes.

9. The microneedle array according to claim 1 , wherein the zeta potential of the liposome is of a value effective to suppress aggregation of liposomes in a case where a water-soluble polymer is mixed with liposomes during production of the microneedle array.

10. The microneedle array according to claim 1 , wherein the zeta potential of the liposome results in suppressing aggregation of liposomes.

11. The microneedle array according to claim 1 , wherein the zeta potential of the liposome results in suppressing aggregation of liposomes in a case where a water-soluble polymer is mixed with liposomes during production of the microneedle array.

12. A microneedle array comprising:

a sheet; and

a plurality of needles which are present on an upper surface of the sheet,

wherein each needle is formed from a solution which contains a water-soluble polymer, a drug, a liposome, and a salt, and the drug is localized at a tip of the needle,

the zeta potential of the liposome is in a range from −10 mV to −100 mV and is of a value effective to suppress aggregation of liposomes,

the zeta potential is a zeta potential of a liquid obtained by diluting the liposome to 0.1 mg/mL with 10 mmol/L of a phosphoric acid aqueous solution having a pH of 7,

the content of the salt in a portion of each needle which contains the liposome is from 0.01 mmol/g to 2.5 mmol/g,

the liposome contains an anionic compound,

the anionic compound is at least one selected from the group consisting of phosphatidylglycerol, phosphatidylserine, phosphatidic acid, a lipid containing a polyoxyethylene chain, and a saponin, and

the water-soluble polymer is at least one selected from the group consisting of polyethylene glycol, polyvinylpyrrolidone, dextran, dextrin, hydroxyethyl starch, and a cellulose derivative.

13. The microneedle array according to claim 12 , wherein the water-soluble polymer is electrically neutral.

14. The microneedle array according to claim 12 , wherein the water-soluble polymer is hydroxyethyl starch, and the liposome contains phosphatidylcholine and distearoyl phosphatidylglycerol.

15. The microneedle array according to claim 12 , wherein the drug is a hormone or a vaccine.

16. The microneedle array according to claim 12 , wherein the zeta potential of the liposome results in suppressing aggregation of liposomes in a case where a water-soluble polymer is mixed with liposomes during production of the microneedle array.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 12, 2018
From: SHIMADA, TOSHIO
To: FUJIFILM CORPORATION
Reel/Frame 047151/0420 →
Priority Claims (1)
JP JP2016-081778 · Apr 15, 2016 · national
Continuity (2)
Continuation PCTJP2017014963 · Apr 12, 2017
Related Publication 20190076635A1 · Mar 14, 2019
Cited By (2)
US 12,186,515 US 12,714,838