US 11,878,072 B2
Compositions and methods utilizing poly(vinyl alcohol) and/or other polymers that aid particle transport in mucus
Alexey Popov, Waltham, MA (US)
Assigned to Alcon Inc., Fribourg (CH)
Filed by Alcon Inc., Fribourg (CH)
Filed on Mar. 30, 2022, as Appl. No. 17/708,960.
Application 16/883,778 is a division of application No. 13/886,514, filed on May 3, 2013, granted, now 10,688,041, issued on Jun. 23, 2020.
Application 17/708,960 is a continuation of application No. 16/883,778, filed on May 26, 2020, granted, now 11,318,088.
Claims priority of provisional application 61/642,261, filed on May 3, 2012.
Prior Publication US 2022/0218597 A1, Jul. 14, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/00 (2006.01); A61K 47/32 (2006.01); A61K 9/10 (2006.01); A61K 9/51 (2006.01); A61K 31/56 (2006.01); A61K 9/50 (2006.01); A61K 38/00 (2006.01)
CPC A61K 9/0012 (2013.01) [A61K 9/10 (2013.01); A61K 9/5026 (2013.01); A61K 9/5138 (2013.01); A61K 31/56 (2013.01); A61K 47/32 (2013.01); A61K 38/00 (2013.01)] 19 Claims
1. A method of delivering an ophthalmic formulation across a mucosal barrier of the eye comprising:
topically administering the ophthalmic formulation to the eye, wherein the ophthalmic formulation comprises:
(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; and
wherein the coated particles have an average size of less than 1 μm.