IP Library › Granted Patent US 12,220,439
Granted Patent B2
US 12,220,439 · App. 18/129,182 · Granted Feb 11, 2025

Methods of diagnosing and treating dry eye syndrome and compositions for treating a human eye

Inventors: Scott Whitcup (Laguna Hills, CA); Orest Olejnik (Reno, NV); Michael Garst (Newport Beach, CA); Peter Simmons (Yorba Linda, CA)
Assignee: Akrivista LLC
A61K36/235A61K9/0048A61K9/1075A61K36/47A61K36/534A61K36/54A61K36/61A61K36/752A61K47/32A61K47/44A61P27/04G01N33/50
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Quick Facts
Patent No.
US 12,220,439
App. No.
18/129,182
Granted
Feb 11, 2025
Kind
B2
Abstract

In preferred embodiments the invention is directed to ocular compositions for the treatment of dry eye, methods for making such compositions, and suites comprising a plurality of different ocular compositions each having a defined composition. In preferred examples, the invention is directed to compositions comprising at least one natural oil, wherein a first member of the suite of compositions is effective in treating dry in in a first patient having a particular set of symptoms and a different second member of the suite of compositions is effective in treating dry in in a second patient having a different set of symptoms. The invention is also directed to methods of making and using the compositions, and to skin care compositions for use around the eye, such as the upper and lower eyelids having a lubricating, non-irritating base composition comprising at least one natural oil.

Claims (27)

1. A composition for applying to an eye or eyelid of a human comprising:

water;

0.1% (w/v) to 0.3% (w/v), inclusive, of a hydrophobic component, wherein the hydrophobic component comprises from about 0.05% (w/v) to about 0.25% (w/v) avocado oil and from about 0.05% (w/v) to about 0.25% (w/v) castor oil; and

hyaluronic acid.

2. The composition of claim 1 , wherein the composition comprises less than about 0.5% (w/v), less than about 0.25% (w/v), less than about 5% (w/v) hyaluronic acid.

3. The composition of claim 2 , wherein the composition comprises less than about 1% (w/v) hyaluronic acid.

4. The composition of claim 1 , further comprising one or more components from the group consisting of a surfactant, an emulsion stabilizer, a tonicity component, a buffer, a preservative, and a chelating agent.

5. The composition of claim 4 , wherein the surfactant comprises a polyoxyethylene sorbitan ester.

6. The composition of claim 5 , wherein the polyoxyethylene sorbitan ester comprises less than about 1% (w/v).

7. The composition of claim 4 , wherein the emulsion stabilizer comprises a polyacrylic acid polymer.

8. The composition of claim 4 , wherein one or more components comprises a polyoxyethylene sorbitan ester and a polyacrylic acid polymer.

9. The composition of claim 4 , wherein the tonicity component comprises glycerin.

10. The composition of claim 9 , wherein the glycerin comprises less than about 1% (w/v).

11. The composition of claim 4 , wherein the buffer comprises boric acid.

12. The composition of claim 4 , wherein the preservative comprises sodium perborate.

13. The composition of claim 4 , wherein the chelating agent comprises EDTA.

14. The composition of claim 1 , further comprising a polyoxyethylene sorbitan ester, a polyacrylic acid polymer, glycerin, boric acid, sodium perborate, and EDTA.

15. The composition of claim 1 , wherein the composition has a viscosity of less than about 20 cP.

16. The composition of claim 1 , wherein the composition is filtered.

17. A composition for applying to an eye or eyelid of a human consisting of:

water;

0.1% (w/v) to (0.3% (w/v), inclusive, of a hydrophobic component, wherein the hydrophobic component comprises from about 0.05% (w/v) to about 0.25% (w/v) avocado oil and from about 0.05% (w/v) to about 0.25% (w/v) castor oil;

less than about 5% (w/v) hyaluronic acid; less than about 1% of a polyoxyethylene sorbitan ester; less than about 1% (w/v) of a tonicity component; a buffer; a preservative;

and a chelating agent.

18. The composition of claim 17 , wherein the polyoxyethylene sorbitan ester is polysorbate 80.

19. The composition of claim 18 , wherein the composition comprises less than 0.2% polyacrylic acid polymer.

20. The composition of claim 17 , wherein the composition has a viscosity of less than about 20 cP.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 30, 2024
From: WHITCUP, SCOTT; OLEJNIK, OREST; GARST, MICHAEL; SIMMONS, PETER
To: AKRIVISTA LLC
Reel/Frame 067574/0875 →
Continuity (3)
Continuation 16638546
Provisional Application 62547553 · Aug 18, 2017
Related Publication 20230233637A1 · Jul 27, 2023
References Cited (98)
US 3278447A · McNicholas · 1966 [cited by applicant]
US 4146499A · Rosano · 1979 [cited by applicant]
US 4585656A · Rosenthal et al. · 1986 [cited by applicant]
US 5527488A · Groh · 1996 [cited by applicant]
US 5698219A · Valdivia et al. · 1997 [cited by applicant]
US 6559182B1 · Purcell · 2003 [cited by applicant]
US 6582718B2 · Kawashima et al. · 2003 [cited by applicant]
US 8909327B1 · Bosworth · 2014 [cited by applicant]
US 8957048B2 · Vehige et al. · 2015 [cited by applicant]
US 9314528B2 · Vehige et al. · 2016 [cited by applicant]
US 9345779B2 · Nakata et al. · 2016 [cited by applicant]
US 11622982B2 · Whitcup et al. · 2023 [cited by applicant]
US 11903986B2 · Whitcup et al. · 2024 [cited by applicant]
US 20030086986A1 · Bruijn et al. · 2003 [cited by applicant]
US 20030109509A1 · Gamache et al. · 2003 [cited by applicant]
US 20030223953A1 · Chong · 2003 [cited by applicant]
US 20050202097A1 · Maskin · 2005 [cited by applicant]
US 20060148686A1 · Xia et al. · 2006 [cited by applicant]
US 20060153885A1 · Korb et al. · 2006 [cited by applicant]
US 20060251685A1 · Yu et al. · 2006 [cited by applicant]
US 20070299004A1 · Acheampong et al. · 2007 [cited by applicant]
US 20100137252A1 · Matsumura et al. · 2010 [cited by applicant]
US 20100174000A1 · Sarrazin · 2010 [cited by examiner]
US 20120108658A1 · Odaka et al. · 2012 [cited by applicant]
US 20120201910A1 · Gore et al. · 2012 [cited by applicant]
US 20130090308A1 · Vehige et al. · 2013 [cited by applicant]
US 20130150324A1 · Simmons et al. · 2013 [cited by applicant]
US 20130331341A1 · Acheampong et al. · 2013 [cited by applicant]
US 20130331768A1 · Nichamin · 2013 [cited by applicant]
US 20140302146A1 · Kurose et al. · 2014 [cited by applicant]
US 20160143977A1 · Likitlersuang et al. · 2016 [cited by applicant]
US 20170014489A1 · Welch et al. · 2017 [cited by applicant]
US 20170143690A1 · Gadek et al. · 2017 [cited by applicant]
US 20180050074A1 · Whitcup et al. · 2018 [cited by applicant]
US 20200164013A1 · Whitcup et al. · 2020 [cited by applicant]
CN 1564683A · 2005 [cited by applicant]
CN 106389218 · 2017 [cited by applicant]
CN 109689161A · 2019 [cited by applicant]
EP 0480690 · 1992 [cited by applicant]
EP 2633852 · 2013 [cited by applicant]
EP 3266446 · 2018 [cited by applicant]
JP 2006233398 · 2006 [cited by applicant]
JP 2007528897 · 2007 [cited by applicant]
JP 2010520210A · 2010 [cited by applicant]
JP 2012528888 · 2012 [cited by applicant]
JP 2014528452A · 2014 [cited by applicant]
WO WO2006004577 · 2006 [cited by applicant]
WO WO2006009112 · 2006 [cited by applicant]
WO WO2008106228 · 2008 [cited by applicant]
WO WO2016085885 · 2016 [cited by applicant]
WO WO2018035469 · 2018 [cited by applicant]
Abetz et al., “Development and validation of the impact of dry eye on everyday life (IDEEL) questionnaire, a patient-reported outcomes (PRO) measure for the assessment of the burden of dry eye on patients,” Health Qual.… [cited by applicant]
Adams et al., “Inadvertent administration of Olbas oil into the eye: a surprisingly frequent presentation,” Eye, Jan. 2009, 23(1): 2 pages. [cited by applicant]
Azeez et al., “Effects of antioxidants on the oxidative stability of vegetable oil at elevated temperature,” International Journal of Applied Science and Technology, May 2013, 3(5): 9 pages. [cited by applicant]
Begley et al., “Use of the dry eye questionnaire to measure symptoms of ocular irritation in patients with aqueous tear deficient dry eye,” Cornea, 2002, 21:664-670. [cited by applicant]
Bennett et al., “Ratite oils promote keratinocyte cell growth and inhibit leukocyte activation,” Poultry science, Sep. 1, 2015, 94(9):2288-2296. [cited by applicant]
Bron et al., “Grading of corneal and conjunctival staining in the context of other dry eye tests,” Cornea, Oct. 2003, 22:7:640-650. [cited by applicant]
Corazza et al., “Doubtful value of patch testing for suspected contact allergy to ophthalmic products,” Acta dermato-venereologica, 2005, 85(1):70-71. [cited by applicant]
De Oliveira et al., “Effect of semisolid formulation of Persea americana Mill (avocado) oil on wound healing in rats,” Evidence-Based Complementary and Alternative Medicine, Jan. 1, 2013. 1-8. [cited by applicant]
Dutok et al., “Acute Toxicity and Dermal and Eye Irritation of the Aqueous and Hydroalcoholic Extracts of the Seeds of (Zapote) Pouteriamammosa (L.) Cronquist,” The Scientific World Journal, Article ID. 2015, 642906(7). [cited by applicant]
European Search Report application No. 1784222.8 PCT/US201747627, dated Apr. 6, 2020, 15 pages. [cited by applicant]
European Search Report application No. 17842221.8 PCT/US2017047627, dated Apr. 6, 2020. [cited by applicant]
European Search Report application No. 18846695.7 PCT/US2018046918, dated Apr. 28, 2021, 12 pages. [cited by applicant]
FDA.gov, [online], “FDA warns that getting alcohol-based hand sanitizer in the eyes can cause serious injury,” Nov. 2, 2021, retrieved on Jul. 26, 2022, retrieved from URL<https://www.fda.gov/drugs/drug-safety-and-avail… [cited by applicant]
FDA.gov, [online], “OTC Active Ingredients”, retrieved on Jan. 21, 2021, retrieved from www.fda.gov/downloads/aboutfda/centersoffices/officeofmedicalproductsandtobacco/cder/ucm135691.pdf, 44 pages. [cited by applicant]
Foulks et al., “New testing options for diagnosing and grading dry eye disease,” Am. J. Ophthalmol., 2014, 157:6:1122-1129. [cited by applicant]
Gao et al., “High Level of Inflammatory Cytokines in the Tears: a Bridge of Patients with Concomitant Exotropia and Dry Eye,” Oxidative Medicine and Cellular Longevity, Oct. 7, 2021, 2021: 7 pages. [cited by applicant]
Gerbacia et al., “Microemulsions: Formulation and stabilization,” J. Coll. & Interface Sci., Aug. 1973, 44:242-248. [cited by applicant]
Guillot et al., “A study of skin and eye irritation in the rabbit due to different sources of some cosmetic raw materials (Part II),” International Journal of Cosmetic Science, Feb. 1, 1979, 1(1): 27-57. [cited by applicant]
Habashy et al., “Anti-inflammatory effects of jojoba liquid wax in experimental models,” Pharm Res., 2005, 51:2:95-105. [cited by applicant]
Hysa et al., “Immunopathophysiology and clinical impact of uveitis in inflammatory rheumatic diseases: an update.” European journal of clinical investigation, Aug. 2021, 51(8):e13572, 13 pages. [cited by applicant]
Jamaicahospital.org [online], “Castor Oil,” 2015, retrieved on Feb. 28, 2023, retrieved from URL<https://jamaicahospital.org/newsletter/castor-oil/#:-:text=Castor%200i1%20is%20probably%20best,first%20before%20using%20ca… [cited by applicant]
Jeong et al., “Evaluation of acute toxicity of plant extracts, lavender, lemon eucalyptus and cassia essential oil,” The Korean Journal of Pesticide Science, English Abstract, 2010, 14(4):339-346. [cited by applicant]
Kathuria et al., “Categorization of marketed artificial tear formulations based on their ingredients: a rational approach for their use,” Journal of Clinical Medicine, Mar. 21, 2021, 10(6):1289, 11 pages. [cited by applicant]
Office action U.S. Appl. No. 15/680,998, mailed Jan. 28, 2019. [cited by applicant]
Office action U.S. Appl. No. 15/680,998, mailed Aug. 24, 2018. [cited by applicant]
Omar, “Oleuropein in olive and its pharmacological effects,” Scientia pharmaceutica, Jun. 2010, 78(2):133-154. [cited by applicant]
Ownby et al., “Expression of pro-inflammatory mediators is inhibited by an avocado/soybean unsaponifiables and epigallocatechin gallate combination,” Journal of Inflammation, Dec. 1, 2014, 11(1): 7 Pages. [cited by applicant]
Pazzoti et al., “Evaluation of oxidative stability of compound oils under accelerated storage conditions,” Brazilian Archives of Biology and Technology, Nov. 14, 2018, 61, 12 pages. [cited by applicant]
PCT International Preliminary Report on Patentability in International Appln. No. PCT/US2017/047627, dated Feb. 19, 2019, 12 pages. [cited by applicant]
PCT International Preliminary Report on Patentability in International Appln. No. PCT/US2018/046918, dated Feb. 18, 2020, 8 pages. [cited by applicant]
PCT International Search Report and Written Opinion application No. PCT/US18/46918, mailed Dec. 4, 2018. 4 pages. [cited by applicant]
PCT International Search Report and Written Opinion in International Appln. PCT/US2017/047627, dated Nov. 22, 2017, 13 pages. [cited by applicant]
PCT International Search Report and Written Opinion, application No. PCT/US/2017/047627, dated Nov. 22, 2017, 13 pages. [cited by applicant]
Pflugfelder et al., “Biological functions of tear film,” Experimental eye research, Aug. 1, 2020, 197:108115, 16 pages. [cited by applicant]
Sade de Paiva et al., “Assessing the severity of keratitis sicca with videokeratoscopic indices,” Ophthalmology, Jun. 1, 2003, 110(6):1102-1109. [cited by applicant]
Said et al., “Benefits and side effects of different vegetable oil vectors on apoptosis, oxidative stress, and P2X7 cell death receptor activation,” Investigative ophthalmology & visual science, Nov. 1, 2007, 48(11):500… [cited by applicant]
Schiffman et al., “Reliability and validity of the ocular surface disease index,” Arch. Ophthalmol. 118:615-621. [cited by applicant]
See et al., “Eyelid skin as a potential site for drug delivery to conjunctiva and ocular tissues,” International journal of pharmaceutics, Nov. 25, 2017, 533(1): 4 pages (Abstract). [cited by applicant]
Simmons et al., “Efficacy, safety, and acceptability of a lipid-based artificial tear formulation: a randomized, controlled, multicenter clinical trial,” Clinical therapeutics, Apr. 1, 2015, 37(4):858-868. [cited by applicant]
theperfumeexpert.com [online], “Kiehls Creamy Eye Treatment Review,” 2013, retrieved on Feb. 28, 2023, retrieved from URL<http://www.theperfumeexpert.com/kiehls-creamy-eye-treatment-review>, 4 pages. [cited by applicant]
Thode et al., “Current and emerging therapeutic strategies for the treatment of meibomian gland dysfunction (MGD),” Drugs, Jul. 1, 2015, 75(11):1177-1185. [cited by applicant]
Tiffany et al., “Tear film stability and tear surface tension,” Curr Eye Res., 1989, 8:5:507-15. [cited by applicant]
Tiffany, “Surface tension in tears tension superficial de la lagrima,” Arch. Soc. ESP Oftalmol., 2006; 81:363-366. [cited by applicant]
Villena et al., “Ocular inflammation models by topical application: croton-oil induced uveitis,” Current eye research, Jan. 1, 1999, 18(1):3-9. [cited by applicant]
Wikipedia.org [online], “Lotion,” 2023, retrieved on Feb. 28, 2023, retrieved from URL<https://en.wikipedia.org/wiki/Lotion>, 5 pages. [cited by applicant]
Woolf et al., “Avocado oil,” InGourmet and health-promoting specialty oils, Jan. 1, 2009, 73-125. [cited by applicant]
Yoon, “Topical biological agents targeting cytokines for the treatment of dry eye disease,” World J Ophthalmol, May 12, 2013, 3(2): 16-19. [cited by applicant]