Polymeric nanoparticles for photosensitizers
Inventors
Haddadi, Azita • Madiyalakan, Ragupathy • Woo, Thomas
Assignees
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Publication Number
US-8916205-B2
Publication Date
2014-12-23
Expiration Date
Abstract
Biodegradable polymeric nanoparticles comprising an inner core formed of a photodynamic agent capable of being activated to generate cytotoxic singlet oxygen are prepared. These nanoparticles have anti-cell proliferation activity and are useful in treating both cancerous and non-cancerous conditions including actinic keratosis, psoriasis and acne vulgaris. Preferably, the photodynamic agent is a hypocrellin B derivative while the polymeric nanoparticle comprises polyglycolic acid, polylactic acid or poly(lactide-co-glycolide). Hypocrellin-comprising nanoparticles are demonstrated to be activated by light or hydrogen peroxide.
Core Innovation
The invention provides singlet oxygen for anti-cell proliferation activity topically to target tissue by contacting the tissue with a biodegradable polymeric nanoparticle. The nanoparticle comprises an inner core formed of a photodynamic agent selected from hypocrellin B, hypocrellin B derivatives, or a combination thereof, and a polymer selected from polyglycolic acid, polylactic acid, or poly(lactic-co-glycolic acid).
In addition to contacting the tissue with the biodegradable polymeric nanoparticle, the method includes contacting the tissue with hydrogen peroxide. The photodynamic agent provided in the inner core is associated with generation of singlet oxygen for anti-cell proliferation activity in the target tissue, and the document states that these nanoparticles are internalized by tissue and can be activated to generate cytotoxic singlet oxygen.
The document describes therapeutic uses including anti-cell proliferation for cancer and non-cancer conditions such as actinic keratosis, psoriasis, and acne. It also describes pharmaceutical compositions and use methods in which the biodegradable polymeric nanoparticles and hydrogen peroxide are employed for the stated singlet-oxygen related anti-cell proliferation activity.
Claims Coverage
The independent claim is directed to a topical method for providing singlet oxygen for anti-cell proliferation activity using a biodegradable polymeric nanoparticle with a photodynamic-agent inner core and hydrogen peroxide. The claim set includes refinements of the nanoparticle polymer end groups and nanoparticle average diameter constraints in dependent claims.
Topical singlet oxygen provision with biodegradable polymeric nanoparticles and hydrogen peroxide
A method for providing singlet oxygen for anti-cell proliferation activity topically to target tissue by contacting the tissue with an effective amount of a biodegradable polymeric nanoparticle comprising an inner core formed of a photodynamic agent selected from the group consisting of hypocrellin B, hypocrellin B derivatives, or a combination thereof, and a polymer selected from the group consisting of polyglycolic acid, polylactic acid or poly(lactic-co-glycolic acid); and contacting the tissue with hydrogen peroxide.
Photodynamic-agent nanoparticle polymer with ester-terminated poly(lactic-co-glycolic acid)
The method uses, as the polymer component, poly(lactic-co-glycolic acid) having an ester-terminated end group.
Photodynamic-agent nanoparticle polymer with COOH-terminated poly(lactic-co-glycolic acid)
The method uses, as the polymer component, poly(lactic-co-glycolic acid) having a free carboxylic acid terminus.
Nanoparticle average diameter in the 100–400 nm range
The method is performed using nanoparticles having an average diameter of approximately 100–400 nm.
Nanoparticle average diameter of approximately 200 nm
The method is performed using nanoparticles having an average diameter of approximately 200 nm.
Overall, the claim coverage centers on a topical singlet-oxygen providing method that combines a biodegradable polymeric nanoparticle having a photodynamic-agent inner core (hypocrellin B or hypocrellin B derivatives) with hydrogen peroxide, with further dependent refinements to poly(lactic-co-glycolic acid) end-group chemistry and nanoparticle average diameter constraints.
Stated Advantages
Provides singlet oxygen for anti-cell proliferation activity topically to target tissue.
Documented Applications
Anti-cell proliferation activity for cancer therapy.
Treatment of actinic keratosis using hydrogen peroxide activation.
Treatment of psoriasis.
Treatment of acne.
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