Reductive and pH dual responsive nano micelle and preparation method and application thereof
A nanomicelle, responsive technology, applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problems of inability to release the drug and low efficacy, and improve the curative effect. , Overcome the effect of being easily leaked
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Embodiment 1
[0021] Embodiment 1: the synthesis (Mn=1000Da) of polycaprolactone diol
[0022]
[0023] Polycaprolactone diol (PCL) is based on caprolactone (ε-CL) as the starting material and dithioethylene glycol (HES) in stannous octoate (Sn(Oct) 2 ) catalyzed by ring-opening polymerization.
[0024] The specific operation is as follows:
[0025] Under nitrogen protection, add 42.1mL toluene, HES (0.102g, 0.6590mmol), Sn(Oct.) 2 (0.081g, 0.1997mmol), ε-CL (7.22g, 63.27mmol), and then the reactor was sealed and removed from the glove box, and placed in an oil bath at 100°C to continue the polymerization reaction for 24h. After the reaction was completed, the reaction solution was concentrated and precipitated in glacial ether, filtered, and vacuum-dried for 24 hours to obtain the product PCL-SS-PCL. Yield: 85.1%.
Embodiment 2
[0026] Embodiment 2: the synthesis (Mn=5000Da) of polymer PEtOz-OH
[0027]
[0028] The preparation of polyoxazoline PEtOz-OH, a capped hydrophilic segment polymer, said polyoxazoline is a polymer, and its synthesis is under the protection of nitrogen, the ring-opening polymerization of methyl p-toluenesulfonate 2-ethyl-2 - Oxazolines. The specific operation is as follows:
[0029] Methyl p-toluenesulfonate (0.34g, 1.834mmol) and 2-ethyl-2-oxazoline (10g, 100.9mmol) were added to dry acetonitrile, and the mixture was heated to 100°C and stirred for 24h. After the reaction was completed, cool to room temperature, add 0.1 mL KOH (1N) and stir at room temperature for 4 h, then settle and separate with glacial ether. The polymer PEOZ-OH was purified by dialysis with deionized water (MWCO:3500g / mol) for two days, during which the dialysis medium was changed, and finally the product PEtOz-OH was obtained by freeze-drying. Yield: 87.6%.
Embodiment 3
[0030] Embodiment 3: the synthesis of polymer PEtOz-PU(SS)-PEtOz
[0031]
[0032] The preparation method of the amphiphilic polyurethane comprises the following steps: firstly reacting polycaprolactone diol and diisocyanate at 65 DEG C to synthesize a polyurethane prepolymer, and then capping with terminal hydroxyl polyoxazoline at room temperature to obtain a final product.
[0033] The specific operation is as follows:
[0034] Under the protection of nitrogen, 1 g, that is, 1 mmol of polycaprolactone diol was azeotroped with toluene and dissolved in 10 mL of anhydrous DMF, and then CDI (1.05 mmol, 0.214 g) was added, and stirred and reacted at 65 ° C for 24 h. Polyoxazoline (0.1 mmol, 0.5 g) was dissolved in 5 mL of anhydrous DMF, dropped into the above solution in an ice-water bath, and reacted at room temperature for 48 h. After the reaction, concentrate and settle in methanol / glacial ether, and vacuum-dry to obtain PEtOz-PU(SS)-PEtOz; the ratio of methanol / glacial e...
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