Nanoparticles having paclitaxel coated with N-succinyl chitosan modified by folic acid and small molecular polypeptide and preparation method thereof
A technology of succinyl chitosan and small molecule polypeptides, which is applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., can solve NSCLC difficult to cure, toxic side effects, tumor cells, and limited anti-cancer effects. The curative effect of cancer and other issues, to achieve the effect of improving bioavailability, simple and easy to control, and low toxic and side effects
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Embodiment 1
[0028] Embodiment 1: Preparation of carrier Tat-Suc-FA nanoparticles
[0029] Prepare carrier Tat-Suc-FA nanoparticles according to the following synthetic route:
[0030]
[0031] Concrete preparation method is as follows:
[0032] ①Take 2mmol of EDC and 0.75mmol of FA in 20mL of DMSO (the concentration of FA in the system is 35mmol / L, and the concentration of EDC is 100mmol / L), and stir at room temperature until completely dissolved to obtain solution A;
[0033] ② Dissolve Suc in an acetic acid-sodium acetate buffer solution with pH=4.7, and control the concentration of Suc in the system to 1% (w / v) to obtain solution B;
[0034] ③ Add solution B to solution A, mix well, and then stir and react in a dark room at room temperature for 20 hours, then adjust the pH of the system to 9.0 with a 4% (w / w) aqueous solution of sodium hydroxide to obtain reaction material C; Wherein, the addition of solution B is to control the amount of Suc in the obtained material to be 0.2 tim...
Embodiment 2
[0040] Embodiment 2: Preparation of paclitaxel / Tat-Suc-FA nanoparticles
[0041] 1) Prepare Tat-Suc-FA nanoparticles according to the method described in Example 1;
[0042] 2) dissolving Tat-Suc-FA nanoparticles in acetic acid-sodium acetate buffer solution with pH=5.5 to prepare a nanopolymer solution with a concentration of 3 mg / mL;
[0043] 3) Paclitaxel was dissolved in deionized water to prepare a paclitaxel aqueous solution with a concentration of 2 mg / mL;
[0044] 4) Mix the nanopolymer solution obtained in step 2) with the paclitaxel aqueous solution obtained in step 3), and control the mass ratio of Tat-Suc-FA nanoparticles to paclitaxel in the obtained material to be 1.5:1, and the obtained material is carried out under ultrasonic conditions. After the assembly reaction (30 min), filter through a microporous membrane with a pore size of 0.22 μm, collect the permeate, and separate by freeze-drying to obtain paclitaxel / Tat-Suc-FA nanoparticles.
[0045] The paclitax...
Embodiment 3
[0048] Embodiment 3: Preparation of paclitaxel / Tat-Suc-FA nanoparticles
[0049] 1) the method described in embodiment 1 makes Tat-Suc-FA nanoparticles;
[0050] 2) dissolving Tat-Suc-FA nanoparticles in acetic acid-sodium acetate buffer solution with pH=5.0 to prepare a nanopolymer solution with a concentration of 5 mg / mL;
[0051] 3) Paclitaxel was dissolved in deionized water to prepare a paclitaxel aqueous solution with a concentration of 4 mg / mL;
[0052] 4) Mix the nanopolymer solution obtained in step 2) with the paclitaxel aqueous solution obtained in step 3), and control the ratio of the mass of Tat-Suc-FA nanoparticles to paclitaxel in the obtained material to be 2.0:1, and the obtained material is carried out under ultrasonic conditions. After the assembly reaction (40 min), filter with a microfiltration membrane with a pore size of 0.20 μm, collect the permeate, and separate by freeze-drying to obtain paclitaxel / Tat-Suc-FA nanoparticles.
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