Process of preparing polymeric nanoparticles that chelate radioactive isotopes and have a surface modified with specific molecules targeting the psma receptor and their use
A technology of radioisotopes and nanoparticles, applied in the field of polymer nanoparticles
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Embodiment 1
[0069] Preparation of Nanoparticles with 10% Substitution of Aldehyde Groups Using Gul Targeting Agent with 90% Substitution of DAD Folding Agent (BCS277)
[0070] 1.1. Oxidation of dextran to polyaldehyde dextran (PAD)
[0071] Dextran Oxidation Reaction:
[0072] Dissolve 5.00 g of dextran in 100 ml of ultrapure water. Add 0.66 g of sodium periodate. The oxidation reaction was continued overnight at room temperature in the dark. The product was purified by dialysis in 100 times volume of ultrapure water for 72 h, wherein the water was changed at least twice. Water was removed by evaporation at 40°C.
[0073] Determination of aldehyde groups in PAD:
[0074] Add 100 μl of 0.8 mM hydroxylamine hydrochloride solution, 300 μl of 0.6M acetate buffer (pH 5.8), and 20-100 μl of PAD into a 2 ml tube, and then add ultrapure water (0-80 μl) to a total volume of 500 μl. Measurements were performed on three different PAD volumes (20, 60 and 100 μl). Preparation of control samples...
Embodiment 2
[0085] Preparation of nanoparticles with 30% substitution of aldehyde groups using Gul targeting agent with 70% substitution of DAD folding agent (BCS290)
[0086] 2.1. Oxidation of dextran to polyaldehyde dextran (PAD)
[0087] Dextran Oxidation Reaction:
[0088] Dissolve 5.00 g of dextran in 100 ml of ultrapure water. Add 0.66 g of sodium periodate. The oxidation reaction was continued overnight at room temperature in the dark. The product was purified by dialysis in 100 times volume of ultrapure water for 72 h, wherein the water was changed at least twice. Water was removed by evaporation at 40°C.
[0089] Determination of aldehyde groups in PAD:
[0090]Add 100 μl of 0.8 mM hydroxylamine hydrochloride solution, 300 μl of 0.6M acetate buffer (pH 5.8), and 20-100 μl of PAD into a 2 ml tube, and then add ultrapure water (0-80 μl) to a total volume of 500 μl. Three different PAD volumes (20, 60 and 100 μl) were tested. Preparation of control samples: Add 100 μl of 0.8 ...
Embodiment 3
[0101] Nanoparticles with 5% substitution of aldehyde groups were prepared using DAD folding agent (BCS318) with 95% substitution of Gul targeting agent.
[0102] 3.1. Oxidation of dextran to polyaldehyde dextran
[0103] Dextran Oxidation Reaction:
[0104] Dissolve 5.00 g of dextran in 100 ml of ultrapure water. Add 0.66 g of sodium periodate. The oxidation reaction was continued overnight at room temperature in the dark. The product was purified by dialysis in 100 times volume of ultrapure water for 72 h, wherein the water was changed at least twice. Water was removed by evaporation at 40°C.
[0105] Determination of aldehyde groups in PAD:
[0106] Add 100 μl of 0.8 mM hydroxylamine hydrochloride solution, 300 μl of 0.6m acetic acid buffer (pH5.8), and 20-100 μl of PAD into a 2ml test tube, and then add ultrapure water (0-80 μl) to a total volume of 500 μl. Three different PAD volumes (20, 60 and 100 μl) were tested. Prepare control samples: Add 100 μl 0.8 mM hydrox...
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