Compositions and methods for ophthalmic and/or other applications
First Claim
1. A topical pharmaceutical composition comprising:
- (a) a plurality of coated nanoparticles, each coated nanoparticle comprising;
(i) a core particle comprising loteprednol etabonate, wherein the loteprednol etabonate constitutes at least 80% of the core particle by weight, and(ii) a mucus penetration-enhancing coating comprising a (poly(ethylene oxide))-(poly(propylene oxide))-(poly(ethylene oxide)) triblock copolymer, wherein the poly(propylene oxide) block has a molecular weight of about 3600 Da and the poly(ethylene oxide) blocks constitute about 70 wt % of the triblock copolymer, and wherein the triblock copolymer is non-covalently adsorbed to the core particle;
(b) about 0.5% w/v to about 3% w/v glycerin; and
(c) about 0.1% w/v to about 1% w/v sodium chloridewherein the topical pharmaceutical composition comprises loteprednol etabonate at about 1% w/v in total;
wherein the topical pharmaceutical composition is a topical suspension, and wherein the ratio of the total weight of loteprednol etabonate to the total weight of triblock copolymer comprised in the topical suspension is about 2;
1, andwherein the coated nanoparticles are mucus-penetrating.
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Accused Products
Abstract
Particles, compositions, and methods that aid particle transport in mucus are provided. The particles, compositions, and methods may be used, in some instances, for ophthalmic and/or other applications. In some embodiments, the compositions and methods may involve modifying the surface coatings of particles, such as particles of pharmaceutical agents that have a low aqueous solubility. Such compositions and methods can be used to achieve efficient transport of particles of pharmaceutical agents though mucus barriers in the body for a wide spectrum of applications, including drug delivery, imaging, and diagnostic applications. In certain embodiments, a pharmaceutical composition including such particles is well-suited for ophthalmic applications, and may be used for delivering pharmaceutical agents to the front of the eye and/or the back of the eye.
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Citations
88 Claims
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1. A topical pharmaceutical composition comprising:
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(a) a plurality of coated nanoparticles, each coated nanoparticle comprising; (i) a core particle comprising loteprednol etabonate, wherein the loteprednol etabonate constitutes at least 80% of the core particle by weight, and (ii) a mucus penetration-enhancing coating comprising a (poly(ethylene oxide))-(poly(propylene oxide))-(poly(ethylene oxide)) triblock copolymer, wherein the poly(propylene oxide) block has a molecular weight of about 3600 Da and the poly(ethylene oxide) blocks constitute about 70 wt % of the triblock copolymer, and wherein the triblock copolymer is non-covalently adsorbed to the core particle; (b) about 0.5% w/v to about 3% w/v glycerin; and (c) about 0.1% w/v to about 1% w/v sodium chloride wherein the topical pharmaceutical composition comprises loteprednol etabonate at about 1% w/v in total; wherein the topical pharmaceutical composition is a topical suspension, and wherein the ratio of the total weight of loteprednol etabonate to the total weight of triblock copolymer comprised in the topical suspension is about 2;
1, andwherein the coated nanoparticles are mucus-penetrating. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31)
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32. A pharmaceutical composition comprising:
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(a) a plurality of particles of loteprednol etabonate; (b) about 0.5% w/v to about 3% w/v glycerin; (c) an ionic tonicity agent; and (d) poloxamer 407; wherein the particles of loteprednol etabonate are non-covalently coated with the poloxamer 407 to form coated nanoparticles, and wherein the coated nanoparticles are mucus-penetrating; wherein the pharmaceutical composition comprises loteprednol etabonate at about 1% w/v in total; and wherein the pharmaceutical composition is a topical suspension, and wherein the ratio of the total weight of the loteprednol etabonate to the total weight of the poloxamer 407 comprised in the topical suspension is about 2;
1. - View Dependent Claims (33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60)
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61. A pharmaceutical composition, comprising:
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(a) a plurality of coated nanoparticles, each of the coated nanoparticles comprising; (i) a core particle comprising a single pharmaceutical agent, wherein the single pharmaceutical agent is loteprednol etabonate, and wherein the loteprednol etabonate comprises at least 90 wt % of the core particle; and (ii) a coating on the core particle, the coating comprising poloxamer 407 non-covalently adsorbed to the core particle; and (b) one or more ophthalmically acceptable carriers, additives, and/or diluents; wherein the pharmaceutical composition is a topical suspension, and wherein the topical suspension comprises about 1% w/v loteprednol etabonate in total and about 0.5% w/v poloxamer 407 in total, and wherein the coated nanoparticles are mucus-penetrating. - View Dependent Claims (62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88)
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Specification