Solanesol-modified paclitaxel prodrug and preparation method and application thereof
A technology for solanesol and paclitaxel, which is applied in the field of solanesol-modified paclitaxel prodrug and its preparation field, achieves the effects of simple and easy preparation method, improved stability and simple and easy synthesis method
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Embodiment 1
[0041] Example 1: Synthesis of Ester-Linked Solanesol-Paclitaxel Prodrug (SOL-PTX)
[0042](1) Weigh 0.96g (9.59mmol) of succinic anhydride in 15mL of DMF, add 1mL of triethylamine, N 2 Under protection, solanesol (4.0g, 6.34mmol) and DMAP (0.39g, 3.19mmol) were dissolved in 20mL of anhydrous dichloromethane, and then the solution was dropped into into the above DMF solution, and stirred at room temperature for 48 h. After the reaction, the reaction solution was transferred to a separatory funnel, extracted twice with 30 mL of distilled water, and the solvent was removed by rotary evaporation. Petroleum ether: ethyl acetate = 1:1 (v:v) was used as the mobile phase to pass through the silica gel column, and the outflow of the product was monitored by TLC. The mobile phase was spin-dried and vacuum-dried to obtain the intermediate product MSS.
[0043] (2) Weigh MSS (0.63g, 0.88mmol), DCC (121mg, 0.59mmol), DMAP (108mg, 0.88mmol) and dissolve in 10mL dichloromethane, N 2 Pacli...
Embodiment 2
[0047] Example 2: Synthesis of Disulfide-Linked Solanesol-Paclitaxel Prodrug (SOL-SS-PTX)
[0048] (1) Weigh 1.31g (6.23mmol) of 3,3-dithiodipropionic acid, 1.28g (6.2mmol) of DCC and 0.2g (1.64mmol) of DMAP in 10mL of DMF, N 2 Under protection, dissolve solanesol (2.0g, 3.17mmoL) in 20mL of anhydrous dichloromethane, then drop the solution into the above solution at a rate of 2mL / min with a constant pressure dropping funnel, and stir at room temperature for 48h After the reaction, the reaction solution was transferred to a separatory funnel, extracted twice with 30 mL of distilled water, and the solvent was removed by rotary evaporation. Use petroleum ether: ethyl acetate = 1:1 (v:v) as the mobile phase to pass through the silica gel column, monitor the outflow of the product by TLC, spin the mobile phase to dryness, and dry it in vacuum to obtain the intermediate product MDPA.
[0049] (2) Weigh MDPA (0.72g, 0.88mmoL), DCC (121mg, 0.59mmoL), DMAP (108mg, 0.88mmoL) and disso...
Embodiment 3
[0053] Example 3: Preparation of solanesol-paclitaxel self-assembled prodrug nanoparticles
[0054] Precisely weigh 15 mg of the prodrug, dissolve it with 2 mL of absolute ethanol, slowly add the ethanol solution dropwise to 10 mL of deionized water under magnetic stirring, and allow it to self-assemble at room temperature to form uniform nanoparticles (SOL-PTX nanoparticles, SOL-SS-PTX nanoparticles). After stirring at room temperature for 12 hours, put it in a dialysis bag with a molecular weight cut-off of 3500kDA, dialyze with deionized water for 2 days, replace the deionized water every 6 hours to remove the organic solvent, and filter through a 0.22µm aqueous membrane to obtain the milky blue prodrug nano particle solution. Adopt dynamic light scattering method to measure its particle size and particle size distribution, the result is as follows image 3 shown. Depend on image 3 It can be seen that the particle size of the nanoparticles is about 100nm, the appearanc...
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