Hydrophobic IR-780 Dye Encapsulated in cRGD-Conjugated Solid Lipid Nanoparticles for NIR Imaging-Guided Photothermal Therapy

This is high demand to enhance the accumulation of near-infrared theranostic agents in the tumor region, which is favorable to the effective phototherapy. Compared with indocyanine green (a clinically applied dye), IR-780 iodide possesses higher and more stable fluorescence intensity and can be utilized as an imaging-guided PTT agent with laser irradiation. However, lipophilicity and short circulation time limit its applications in cancer imaging and therapy. Moreover, solid lipid nanoparticles (SLNs) conjugated with c­(RGDyK) was designed as efficient carriers to improve the targeted delivery of IR-780 to the tumors. The multifunctional cRGD-IR-780 SLNs exhibited a desirable monodispersity, preferable stability and significant targeting to cell lines overexpressing α_<i>v</i>β₃ integrin. Additionally, the in vitro assays such as cell viability and in vivo PTT treatment denoted that U87MG cells or U87MG transplantation tumors could be eradicated by applying cRGD-IR-780 SLNs under laser irradiation. Therefore, the resultant cRGD-IR-780 SLNs may serve as a promising NIR imaging-guided targeting PTT agent for cancer therapy

Aptamer-Modified Temperature-Sensitive Liposomal Contrast Agent for Magnetic Resonance Imaging

A novel aptamer modified thermosensitive liposome was designed as an efficient magnetic resonance imaging probe. In this paper, Gd-DTPA was encapsulated into an optimized thermosensitive liposome (TSL) formulation, followed by conjugation with AS1411 for specific targeting against tumor cells that overexpress nucleolin receptors. The resulting liposomes were extensively characterized <i>in vitro</i> as a contrast agent. As-prepared TSLs-AS1411 had a diameter about 136.1 nm. No obvious cytotoxicity was observed from MTT assay, which illustrated that the liposomes exhibited excellent biocompatibility. Compared to the control incubation at 37 °C, the liposomes modified with AS1411 exhibited much higher T₁ relaxivity in MCF-7 cells incubated at 42 °C. These data indicate that the Gd-encapsulated TSLs-AS1411 may be a promising tool in early cancer diagnosis

Poly(glycerol) Used for Constructing Mixed Polymeric Micelles as <i>T</i>₁ MRI Contrast Agent for Tumor-Targeted Imaging

There was much interest in the development of nanoscale delivery vehicles based on polymeric micelles to realize the diagnostic and therapeutic applications in biomedicine. Here, with the purpose of constructing a micellar magnetic resonance imaging (MRI) contrast agent (CA) with well biocompatibility and targeting specificity, two types of amphiphilic diblock polymers, mPEG–PG­(DOTA­(Gd))-<i>b</i>-PCL and FA-PEG-<i>b</i>-PCL, were synthesized to form mixed micelles by coassembly. The nanostructure of the resulting micellar system consisted of poly­(caprolactone) (PCL) as core and poly­(glycerol) (PG) and poly­(ethylene glycol) (PEG) as shell, simultaneously modified with DOTA­(Gd) chelates and folic acid (FA), which afforded functions of MRI contrast enhancement and tumor targeting. The mixed micelles in aqueous solution presented a hydrodynamic diameter of about 85 nm. Additionally, this mixed micelles exhibited higher <i>r</i>₁ relaxivity (14.01 mM^–1 S^1–) compared with commercial Magnevist (3.95 mM^–1 S^1–) and showed negligible cytotoxicity estimated by WST assay. In vitro and in vivo MRI experiments revealed excellent targeting specificity to tumor cells and tissue. Furthermore, considerably enhanced signal intensity and prominent positive contrast effect were achieved at tumor region after tumor-bearing mice were intravenously injected with the mixed micelles. These preliminary results indicated the potential of the mixed micelle as <i>T</i>₁ MRI CA for tumor-targeted imaging