Ocular drug delivery formulation
Inventors
Hossain, Sazzad • Kabiri, Maryam • Yadav, Vikramaditya Ganapati
Assignees
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Publication Number
US-12083229-B2
Publication Date
2024-09-10
Expiration Date
Abstract
There is provided an ocular drug delivery formulation comprising a delivery carrier comprising a cellulosic polymer and an anionic polysaccharide and nanoparticles comprising an amphiphilic non-ionizable block copolymer and a cannabinoid. The formulation has a gel point of about 30° C. to about 37° C.
Core Innovation
The disclosed invention relates to an ocular drug delivery formulation having a thermoresponsive delivery carrier and cannabinoid-loaded nanoparticles for topical ocular administration. The delivery carrier includes a cellulosic polymer and an anionic polysaccharide, and the formulation is designed to form a gel with a gel point in a target range of about 30 °C to about 34 °C.
The delivery carrier combines methyl cellulose as the cellulosic polymer and hyaluronic acid as the anionic polysaccharide. Nanoparticles are included that comprise poly(ethylene oxide-b-lactide) as an amphiphilic non-ionizable block copolymer together with a cannabinoid, where the nanoparticles have an average diameter from about 75 nm to about 250 nm.
In the disclosed embodiments, the cannabinoid may be specified from a set of cannabinoid compounds, including cannabigerolic acid (CBGA). The formulation is characterized by gel point behavior that is linked to carrier design parameters, and the resulting system is described as having enhanced transcorneal penetration and corneal and lens uptake relative to mineral oil controls.
Claims Coverage
The independent claims define an ocular drug delivery formulation with three inventive features: a thermoresponsive carrier with gel point control, cannabinoid-loaded poly(ethylene oxide-b-lactide) nanoparticles, and a specific carrier-and-nanoparticle selection defining gel point and nanoparticle size.
Thermoresponsive ocular carrier composition with gel point control
An ocular drug delivery formulation where a delivery carrier comprises from about 1 wt % to about 4 wt % of methyl cellulose and from about 0.5 wt % to about 2.5 wt % of hyaluronic acid, and wherein the formulation has a gel point from about 30 °C to about 34 °C.
Amphiphilic non-ionizable block copolymer nanoparticles encapsulating a cannabinoid
Nanoparticles comprising poly(ethylene oxide-b-lactide) as an amphiphilic non-ionizable block copolymer and a cannabinoid, wherein the average diameter of the nanoparticles is from about 75 nm to about 250 nm.
Specific carrier-and-nanoparticle selection defining gel point and nanoparticle size
An ocular drug delivery formulation comprising a delivery carrier with 2.5 wt % methyl cellulose and 1.5 wt % hyaluronic acid and nanoparticles comprising poly(ethylene oxide-b-lactide) and cannabigerolic acid (CBGA), wherein the average diameter of the nanoparticles is about 175 nm to about 200 nm and wherein the formulation has a gel point of about 32 °C.
Across the independent claims, the core coverage is a thermoresponsive ocular formulation using methyl cellulose and hyaluronic acid to achieve a gel point around 30–34 °C, combined with poly(ethylene oxide-b-lactide) nanoparticles carrying a cannabinoid, with nanoparticle average diameter constrained to about 75–250 nm or specifically about 175–200 nm alongside a gel point about 32 °C.
Stated Advantages
Enhanced transcorneal penetration.
Enhanced corneal and lens uptake versus mineral oil controls.
Documented Applications
Treatment of an eye disorder by administering an effective amount of the ocular drug delivery formulation to the eye of a subject in need.
The eye disorder is glaucoma.
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