IP Library Granted Patent US 11,547,680
Granted Patent B2
US 11,547,680 · App. 17/047,421 · Granted Jan 10, 2023

Benzalkonium-embedded mesostructured silica compositions and uses of same

Inventors: Tewodros Asefa (Kendall Park, NJ); Viktor Dubovoy (Piscataway, NJ); Anjani Ganti (King of Prussia, PA); Jeffrey M. Boyd (Highland Park, NJ)
Assignee: Rutgers, The State University of New Jersey
A61K31/14A01N25/12A01N33/12A61K9/0014A61K9/1611A61K31/045A61K31/07A61K31/192A61K31/351A61K31/519A61K31/522A61K31/573A61K31/593A61K31/60A61K31/7056A61K45/06A61P31/04
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Quick Facts
Patent No.
US 11,547,680
App. No.
17/047,421
Granted
Jan 10, 2023
Kind
B2
Abstract

The present invention relates in one aspect to the discovery of novel mesoporous silica nanoparticles (MSNs) templated around and comprising benzalkonium chloride (BAC). In certain embodiments, the BAC-SiO 2 mesoporous nanoparticles are capable of sustained release of BAC under acidic conditions, thereby acting as a long release antimicrobial agent. In other embodiments, the BAC-SiO 2 mesoporous nanoparticles can be incorporated into a variety of consumer products as an antimicrobial agent additive, including for example, but not limited to, surgical dressings, bandages, deodorants, soaps, facial cleansers and industrial cleaners.

Claims (41)

1. A composition comprising mesostructured silica particles and benzalkonium chloride, wherein each of the following applies:

(a) the mesostructured silica particles comprise pores;

(b) wherein the benzalkonium chloride is the only surfactant embedded within the pores of the mesostructured silica particles;

(c) each silicon atom in the silica particles is covalently bonded only to oxygen atoms; and

(d) the silica particles are at least one selected from silica nanoparticles and silica microparticles.

2. The composition of claim 1 , wherein the composition comprises at least about 1% (w/w) benzalkonium chloride.

3. The composition of claim 2 , wherein the composition comprises at least about 30% (w/w) benzalkonium chloride.

4. The composition of claim 3 , wherein the composition comprises about 34-40% (w/w) benzalkonium chloride.

5. The composition of claim 1 , wherein at least one of the following applies:

(a) a fraction of the mesostructured silica particles have a surface area of about 1,000 m 2 /g to about 2,000 m 2 /g;

(b) the mesostructured silica particles comprise pores having an average diameter of about 10 A to about 200 A;

(c) the mesostructured silica particles comprise pores having an average volume of about 0.1 cm 3 /g to about 1.0 cm 3 /g; and

(d) the mesostructured silica particles have an average diameter of about 50 nm to about 1,000 nm.

6. The composition of claim 5 , wherein at least one of the following applies:

(a) a fraction of the mesostructured silica particles have a surface area of about 1,500 m 2 /g; and

(b) the mesostructured silica particles comprise pores having an average diameter of about 30 A to about 50 A.

7. The composition of claim 1 , further comprising at least one swelling agent.

8. The composition of claim 7 , wherein the at least one swelling agent is selected from 1,3,5-trimethylbenzene (TMB), decane, octane, 1,3,5-triisopropylbenzene, and/or hexane.

9. The composition of claim 1 , further comprising at least one additional pharmaceutical agent.

10. The composition of claim 9 , wherein the at least one pharmaceutical agent is at least one selected from an analgesic agent, an anti-inflammatory agent, an antimicrobial agent, an antiviral agent, an antifungal agent, an anti-pruritic, an antiperspirant, a sunblocking agent, a vitamin, an NSAID, a skin cleanser, a disinfectant, a corticosteroid, a protein, a peptide, and/or a hormone.

11. The composition of claim 9 , wherein the at least one pharmaceutical agent is selected from ethanol, folic acid, salicylic acid, benzoic acid, hydrocortisone, vitamin A, vitamin D, clindamycin, mupirocin, acyclovir, and/or clobetasol propionate.

12. The composition of claim 1 , which is an antimicrobial composition.

13. The composition of claim 1 , which is a pharmaceutically acceptable composition.

14. The composition of claim 13 , which is formulated for topical administration.

15. The composition of claim 13 , which is incorporated into one or more selected from a wound dressing, a lotion, an ointment, a gel, a powder, a spray, an aqueous solution, and/or an anhydrous solution.

16. The composition of claim 1 , which is formulated either:

(a) for use as a cleaning agent, a disinfecting agent, a preserving agent, a bacteriostatic agent, an antifungal agent, and/or an antiviral agent; or

(b) as part of at least one selected from an antimicrobial coating, an antifungal coating, and/or an antiviral coating.

17. A method of making a composition comprising mesostructed silica particles and a benzalkonium chloride, wherein each of the following applies: (a) the mesostructured silica particles comprise pores; (b) the benzalkonium choloride is the only surfactant embedded within the pores of the mesostructured silica particles; (c) each silicon atom in the silica particles is covalently bonded only to oxygen atoms; and (d) the silica particles are at least one selected from silica nanoparticles and silica microparticles,

the method comprising heating an aqueous solution comprising benzalkonium chloride as the only surfactant, a base, and a silica precursor, and collecting the mesostructured silica particles through at least one method selected from filtering the solution and/or centrifuging the solution.

18. The method of claim 17 , wherein at least one of the following applies:

(a) the aqueous solution is heated to about 80° C.;

(b) the aqueous solution is heated for about 5 min to about 72 h;

(c) the collected mesostructured silica particles are dried after filtration or centrifugation;

(d) the silica precursor is added dropwise to a mixture of benzalkonium chloride and the base to form the aqueous solution;

(e) the benzalkonium chloride and silica precursor are present in a molar ratio of about 1:10 to about 1:100;

the aqueous solution is alkaline;

(g) the base is at least one base selected from the group consisting of ammonium hydroxide (NH 4 OH), Na 2 CO 3 , NEt 3 , lysine, NaOH, and KOH; and

(h) the silica precursor material is at least one selected from tetraethyl orthosilicate (TEOS), sodium silicate, tetramethyl orthosilicate (TMOS), tetrapropyl orthosilicate (TPOS), tetrabutyl orthosilicate (TBOS), silicic acid, and sodium silicate.

19. The method of claim 17 , wherein the aqueous solution further comprises a silica mineralizer.

20. The method of claim 19 , wherein the silica mineralizer is a fluoride salt.

Assignments (1)
CONFIRMATORY LICENSE Recorded Jan 7, 2021
From: RUTGERS, THE STATE UNIVERSITY OF N.J.
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 054916/0960 →
Continuity (2)
Provisional Application 62665146 · May 1, 2018
Related Publication 20210137855A1 · May 13, 2021