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Compositions and methods for ophthalmic and/or other applications

  • US 10,646,437 B2
  • Filed: 05/11/2018
  • Issued: 05/12/2020
  • Est. Priority Date: 05/03/2012
  • Status: Active Grant
First Claim
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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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