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Compositions and methods utilizing poly(vinyl alcohol) and/or other polymers that aid particle transport in mucus

  • US 10,688,041 B2
  • Filed: 05/03/2013
  • Issued: 06/23/2020
  • Est. Priority Date: 05/03/2012
  • Status: Active Grant
First Claim
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1. An ophthalmic composition comprising:

  • (a) a plurality of mucus-penetrating coated particles,wherein each of the coated particles comprises;

    (i) a core particle comprising a pharmaceutical agent or a salt thereof, wherein the pharmaceutical agent constitutes at least about 80 wt % of the core particle; and

    (ii) a mucus penetration-enhancing coating comprising a surface-altering agent surrounding the core particle, wherein the surface-altering agent comprises a poly(vinyl alcohol) (PVA) polymer having pendant hydroxyl groups on the backbone of the PVA polymer, the PVA polymer having a molecular weight of at least about 1 kDa and less than or equal to about 1000 kDa, wherein the hydrolysis level of the PVA polymer is at least about 30% and less than about 95%, and(b) one or more pharmaceutically acceptable excipients or carriers;

    wherein the coated particles have an increased mobility in human mucus relative to uncoated particles;

    wherein the coated particles have an average size of less than 1 μ

    m; and

    wherein the ophthalmic composition is configured for delivery to an eye.

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