This invention relates to
albumin-bound
BODIPY derivatives, their preparation, and applications, belonging to the field of
pharmaceutical technology. The
albumin-bound
BODIPY derivative of this invention couples
BODIPY with the
albumin-free non-covalent binder 4-(p-iodophenyl)
butyric acid (IP), and can be further coupled with a
boron thiol compound (BSH). 4-(p-iodophenyl)
butyric acid has excellent albumin-
binding ability; by utilizing the EPR effect of albumin, tumor-targeted delivery of
boron-containing modules (BODIPY or BSH) can be achieved, overcoming the dependence of traditional
boron drugs 4-dihydroxyboron-L-
phenylalanine (BPA) on the LAT1
transporter protein, and exhibiting a certain degree of broad-spectrum targeting. Simultaneously, the
fluorine-18 (…) introduced into the BODIPY structure… 18 The F) atom allows for real-time monitoring of the distribution of boron-containing drugs
in vivo via PET-CT, enabling integrated diagnosis and treatment of tumors. This conjugate exhibits high safety and
low toxicity, high
in vitro cellular uptake, and
in vivo animal distribution experiments confirming its excellent
tumor targeting properties. This invention can serve as a broad-spectrum targeted boron-containing
drug in integrated BNCT diagnosis and treatment.