# US 2014/0170229 A1 · Polymeric nanoparticles for photosensitizers > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2014/0170229 A1 - Document ID: US20140170229A1 - Status: Published application - Kind: A1 - Application number: 14/236,212 - Filed: 2011-08-11 - Published: 2014-06-19 - Earliest claimed: 2011-08-11 - Assignees: Quest Pharmatech Inc. - Inventors: Azita Haddadi; Ragupathy Madiyalakan; Thomas Woo - Web page: https://patentgrep.com/patent/US20140170229A1 ## CPC - A61K 41/0057: {Photodynamic therapy with a photosensitizer, i.e. agent able to produce reactive oxygen species upon exposure to light or radiation, e.g. UV or visible light; photocleavage of nucleic acids with an agent} - A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)} - A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)} - A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} - A61K 9/5153: {Polyesters, e.g. poly(lactide-co-glycolide)} - A61K 31/122: having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin - A61P 35/00: Antineoplastic agents - C07C 49/84: containing ether groups, [IMAGE cpc-sch-C07C-0958.gif] groups,[IMAGE cpc-sch-C07C-0959.gif] groups, or[IMAGE cpc-sch-C07C-0960.gif] groups - Y10S 977/773: Nanoparticle, i.e. structure having three dimensions of 100 nm or less - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS - Y10S: TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS ## 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. ## Claims ### Claim 1 A biodegradable polymeric nanoparticle comprising an inner core formed of a photodynamic agent capable of being activated to generate cytotoxic singlet oxygen for anti-cell proliferation activity. ### Claim 2 (depends on 1) The nanoparticle of claim 1, wherein the polymer is selected from the group consisting of polyglycolic acid, polylactic acid or a poly(lactide-co-glycolide). ### Claim 3 (depends on 2) The nanoparticle of claim 2, wherein the polymer comprises poly(lactic-co-glycolic acid). ### Claim 4 (depends on 3) The nanoparticle of claim 3, wherein the polymer comprises poly(lactic-co-glycolic acid) having an ester-terminus. ### Claim 5 (depends on 3) The nanoparticle of claim 3, wherein the polymer comprises poly(lactic-co-glycolic acid) having a free carboxylic acid terminus. ### Claim 6 (depends on 1) The nanoparticle of claim 1, wherein the photodynamic agent comprises hypocrellin B, or a derivative thereof. ### Claim 7 (depends on 6) The nanoparticle of claim 6, wherein the hypocrellin B, or derivative thereof, comprises a compound having the structure of SL052. ### Claim 8 (depends on 6) The nanoparticle of claim 6, wherein the hypocrellin B, or derivative thereof, comprises a compound having the structure of SL017. ### Claim 9 (depends on 1) The nanoparticle of claim 1, wherein the nanoparticles have an average diameter that is approximately 100-400 nm. ### Claim 10 (depends on 9) The nanoparticle of claim 9, wherein the nanoparticles have an average diameter of approximately 200 nm. ### Claim 11 (depends on 1) The nanoparticle of claim 1, wherein the nanoparticle is activated by means selected from the group consisting of photodynamic (PDT) therapy and/or hydrogen peroxide. ### Claim 12 (depends on 1) A pharmaceutical composition comprising the nanoparticle of claim 1 capable of anti-cell proliferation activity, and a pharmaceutically acceptable carrier. ### Claim 13 (canceled) ### Claim 14 (depends on 17) The method of claim 17, further comprising an activation means selected from the group consisting of photodynamic (PDT) therapy and/or hydrogen peroxide. ### Claim 15 (depends on 14) The method of claim 14, wherein the nanoparticle is used to contact the target tissue systemically, topically, or a combination thereof. ### Claim 16 (depends on 1) A method of manufacturing a pharmaceutical composition capable of being activated to generate cytotoxic levels of singlet oxygen at a target tissue, wherein the composition comprises the nanoparticles of claim 1, and a pharmaceutically acceptable carrier. ### Claim 17 (depends on 1) A method of delivering a photosensitizing agent capable of being activated to produce cytotoxic singlet oxygen to a target tissue, the method comprising: contacting the tissue with an effective amount of the biodegradable polymeric nanoparticle of claim 1, wherein the nanoparticle is capable of being internalized by the target tissue.