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Publication Number
US-12521435-B2
Publication Date
2026-01-13
Expiration Date
Abstract
A photodynamic therapy composition, the composition includes a plurality of targeted phthalocyanine gold nanoparticle conjugates, wherein each targeted phthalocyanine gold nanoparticle conjugate includes a plurality of phthalocyanine compounds covalently coupled to a surface of the gold nanoparticle via bio-cleavable linker and a plurality of cancer or tissue targeting agents coupled to the gold nanoparticle.
Core Innovation
The invention relates to a photodynamic therapy composition comprising a plurality of targeted phthalocyanine gold nanoparticle conjugates. Each targeted phthalocyanine gold nanoparticle conjugate includes a plurality of phthalocyanine compounds covalently coupled directly to a surface of a gold nanoparticle via bio-cleavable linkers, and the surface of the gold nanoparticle is directly conjugated to the cysteine residue of the bio-cleavable linker via an Au-S bond.
The bio-cleavable linker is a lysosomal cleavable peptide having the amino acid sequence GFLGC (SEQ ID NO:1). A plurality of cancer or tissue targeting agents is coupled to the gold nanoparticle, including PSMA ligands.
The phthalocyanine compounds are linked to the Au nanoparticles such that the phthalocyanine is presented in a targeted conjugate form. The lysosomal cleavable peptide linker is designed to be cleaved to release or activate the phthalocyanine compounds in the relevant cellular compartment, and the conjugated phthalocyanine compounds are inactive prior to cleavage and then enzymatically cleaved in an endolysosomal vesicle of a targeted cancer cell.
The patent further provides a treatment method for a PSMA expressing cancer in a subject in need thereof, comprising systemically administering a therapeutically effective amount of the photodynamic therapy composition and subsequently exposing the phthalocyanine compounds to NIR light. The NIR light is sequentially administered at least three times following administration, and each NIR administration results in increased photodynamic therapy composition accumulation in the subject’s cancer cells.
Claims Coverage
The provided independent claim set includes three independent claims: a composition claim and two method claims. Across the independent claims, the inventive features center on targeted phthalocyanine-gold nanoparticle conjugates with a lysosomal cleavable peptide linker GFLGC (SEQ ID NO:1) conjugated via an Au-S bond, and on inducing cytotoxic effects by exposing the phthalocyanine to NIR light, including sequential NIR administration to increase accumulation.
Targeted phthalocyanine gold nanoparticle conjugates with lysosomal cleavable peptide GFLGC (SEQ ID NO:1) via Au-S bond
A photodynamic therapy composition comprising a plurality of targeted phthalocyanine gold nanoparticle conjugates, wherein each targeted phthalocyanine gold nanoparticle conjugate includes a plurality of phthalocyanine compounds covalently coupled directly to a surface of a gold nanoparticle via bio-cleavable linkers; wherein the bio-cleavable linker is a lysosomal cleavable peptide having the amino acid sequence GFLGC (SEQ ID NO:1); and wherein the surface of the gold nanoparticle is directly conjugated to the cysteine residue of the bio-cleavable linker via an Au-S bond.
Cancer or tissue targeting agents coupled to the gold nanoparticle in the conjugates
Each targeted phthalocyanine gold nanoparticle conjugate further includes a plurality of cancer or tissue targeting agents coupled to the gold nanoparticle, including PSMA ligands.
Systemic administration of the targeted composition and NIR-induced cytotoxic effects
A method for treating a PSMA expressing cancer in a subject in need thereof, comprising administering systemically a therapeutically effective amount of a photodynamic therapy composition including targeted phthalocyanine gold nanoparticle conjugates and exposing the phthalocyanine compounds to near infrared (NIR) light, thereby inducing the cytotoxic effects of the phthalocyanine compound.
Sequential NIR administration at least three times with increased accumulation
A method for treating a PSMA expressing cancer comprising administering systemically a photodynamic therapy composition including targeted phthalocyanine gold nanoparticle conjugates and PSMA ligands; exposing the phthalocyanine compound to near infrared (NIR) light; wherein NIR light is sequentially administered at least three times following administration; and wherein each NIR administration results in increased photodynamic therapy composition accumulation in the subject's cancer cells.
Across the independent claims, the invention covers a photodynamic therapy composition of targeted phthalocyanine gold nanoparticle conjugates where phthalocyanines are covalently coupled to Au via lysosomal cleavable peptide GFLGC (SEQ ID NO:1) linked through an Au-S bond to the cysteine residue, with cancer or tissue targeting agents including PSMA ligands, and methods of treating PSMA expressing cancer by systemically administering the composition and inducing cytotoxic effects via exposure of the phthalocyanine to NIR light, including sequential NIR exposures at least three times to increase accumulation.
Stated Advantages
NIR exposure induces cytotoxic effects of the phthalocyanine compound.
Sequential NIR administration at least three times results in increased photodynamic therapy composition accumulation in the subject’s cancer cells.
Documented Applications
Treating a PSMA expressing cancer in a subject in need thereof using a photodynamic therapy composition of targeted phthalocyanine gold nanoparticle conjugates and NIR light exposure.
Treating a PSMA expressing cancer using sequential NIR administration at least three times following administration, where each NIR administration results in increased photodynamic therapy composition accumulation in the subject’s cancer cells.
Targeting PSMA-expressing cancers, including metastatic prostate cancer, and PSMA-expressing cancer selected from the group consisting of renal carcinoma, transitional cell carcinoma of the urinary bladder, testicular embryonal carcinoma, colonic adenocarcinoma, neuroendocrine carcinoma, glioblastoma multiforme, malignant melanoma, pancreatic ductal carcinoma, non-small cell lung carcinoma, soft tissue carcinoma, breast carcinoma, and prostatic adenocarcinoma.
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