A combined drug-loaded micelle targeting integrin receptors and its preparation method
An integrin receptor, drug-carrying micelle technology, which can be used in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of low drug loading in the micelle system, and achieve The effect of increasing drug loading and improving therapeutic index
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Embodiment 1
[0041] Example 1 Preparation of amphiphilic block copolymer Pluronic-COOH with active group carboxyl
[0042] Put 0.01MPluronic and 400ml acetone in a round-bottomed flask, slowly heat up until the solution is clear, let it cool to room temperature, add 17ml Jones reagent, magnetically stir overnight at room temperature, add 5mL isopropanol to quench the reaction. Add 12.6g of activated carbon and continue to stir for 2h, heat to 40°C, suction filter while hot to obtain a clear solution, evaporate under reduced pressure to obtain a white viscous substance, add precooled n-hexane to precipitate a solid, and dry in vacuo to obtain carboxylated Pluronic ( Pluronic-COOH). The purity of the product was analyzed by gel permeation chromatography (GPC). 1 The molecular weight of the product was calculated from the peak area ratio of the proton in the methylene group in the H-NMR spectrum.
Embodiment 2
[0043] Embodiment 2 prepares Pluronic-DOX
[0044] Weigh 7.4 mM of Pluronic-COOH in the above Example 1, and dissolve it in 20 ml of N,N-dimethylformamide at room temperature. Add 1 g EDC and 2 g NHS to the solution of Pluronic-COOH. After reacting for 15 minutes, 2.8ml of 2-mercaptoethanol, 3.48g of DOX and 10mg of triethylamine were added, and stirring was continued at room temperature for 12 hours under nitrogen protection. After the reaction, dialyze with deionized water in the dark for 2 days (MWCO3500), and freeze-dry the concentrated solution to obtain Pluronic-DOX. pass 1 The product was verified by H-NMR spectrum; the absorbance was measured by UV-Vis spectrophotometry, and the molar connection rate of DOX was calculated.
Embodiment 3
[0045] Embodiment 3 prepares the amphiphilic copolymer modified with RGD peptide
[0046] (1) Preparation of Pluronic-NHS by activating the carboxyl group with NHS:
[0047] Weigh 0.053mM of Pluronic-COOH, 22mg of DCC and 12.2mg of NHS in the above-mentioned Example 1 and dissolve them in 5ml of chloroform, and react at room temperature for 24h under the protection of nitrogen. After the reaction was completed, the solvent was removed under reduced pressure and precipitated with cold ether. The precipitate was vacuum-dried to constant weight to obtain Pluronic-NHS. The product is verified by 1H-NMR spectrum;
[0048] (2) Preparation of c(RGDyK)-Pluronic by cyclic RGD peptide (c(RGDyK)) modified amphiphilic copolymer;
[0049] Dissolve 0.0053mM of Pluronic-COOH in (1) above in 1ml of N,N-dimethylformamide to obtain solution A; dissolve 6.3mg (0.01mM) of c(RGDyK) peptide in 0.1M HEPES to obtain Solution B. Solution B was added dropwise to solution A, and the pH value was ad...
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