Preparation of a drug-loaded cinnamaldehyde-dextran polymer self-assembled nanoparticle and its antitumor application
A kind of technology of glucan and cinnamaldehyde, which is applied in the fields of high molecular polymer and its synthesis and application
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Embodiment 1
[0028] The preparation of embodiment 1 polymer
[0029] (1) Dissolve cinnamaldehyde (5g, 1eq), trimethyl orthoformate (18.07g, 4.5eq) and pyridinium p-toluenesulfonate (1.89g, 0.2eq) in an appropriate amount of methanol, at 60°C , Reaction 3h. with saturated NaHCO 3 Quenched reaction, extracted three times with EA (ethyl acetate), combined organic layers, MgSO 4 Dry and spin dry under reduced pressure to obtain cinnamon acetal (6.45 g, 95%), which is directly carried out to the next reaction.
[0030] (2) The obtained cinnamon acetal (6.4g, corresponding to 2 equivalents of each hydroxyl group of dextran monomer), dextran (0.872g, MW=20,000), pyridinium p-toluenesulfonate (0.202 g, corresponding to each hydroxyl group of dextran monomer 0.05 equivalent), dissolved with DMSO (10ml), added activated Molecular sieve, N 2 Protected, reacted in an anhydrous and oxygen-free environment, heated at 60°C, and reacted for 60h. The molecular sieves were removed by suction filtrati...
Embodiment 2
[0033] (1) Weigh 5 mg of the polymer obtained in Example 1 and dissolve it with 1 ml of DMSO, drop it into PBS under high-speed stirring, and stir for 2 minutes to fully self-assemble and form nanoparticles. Then DLS detects its particle size, the particle size result is as follows figure 2 As shown in A, the size of nanoparticles formed by self-assembly is about 182.3nm, and its PDI value is 0.225, and the comprehensive evaluation is GOOD.
[0034] (2) Take the self-assembled nanoparticle solution, dilute it with water to 0.125mg / ml, then slowly drop it on the copper grid of the transmission electron microscope, dry it in an oven at 25°C, and then observe it under the transmission electron microscope. The result is as follows figure 2 As shown in B, nanoparticles of about 200 nm are formed.
[0035](3) Take 5 mg of cinnamaldehyde-dextran polymer, dissolve it in 1 ml of DMSO, shake for 2 minutes, and shake evenly. The DMSO solution is dropped into the PBS solution which is...
Embodiment 3
[0039] Take 5 mg of cinnamaldehyde-dextran polymer and dissolve it with 0.5 ml DMSO, and weigh 2 mg of HCPT (10-hydroxycamptothecin) and dissolve it with 0.5 ml DMSO. Mix the two evenly, drop them into 20ml of PBS that is stirring at high speed with a rubber dropper, stir for 4 hours, then dialyze in ultrapure water with a 3.5kd dialysis bag, change the water every 4 hours, and dialyze for 24 hours. Liquids are freeze-dried. The amount of drug loaded was judged by the standard curve of camptothecin. It can be detected that the entrapment rate of camptothecin is about 54%, and the entrapment amount is 0.216mg / mg. It can be seen that the nanoparticle has the ability to load drugs.
[0040] Performance Determination of Drugs for Targeted Release:
[0041] Take 3ml of the dialyzed solution (into a 1000KD dialysis bag, dialyze in 50ml of PBS (pH7.4, 5.0) at 37°C with stirring, and take out 0.3 ml (take three in parallel), measure the OD values of cinnamaldehyde and CPT at 295...
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