Lysine-based polyesteramide nano drug delivery system as well as preparation method and application thereof
A technology of polyester amide and lysine, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. It can solve the problems of being unable to entrap drugs in nanoparticles and achieve good biosafety Sexuality, efficient and controllable release, enhanced utilization effect
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Embodiment 1
[0054] Embodiment 1 Preparation of a lysine-based polyester amide polymer drug carrier
[0055] 1, the preparation method of the polyester amide polymer based on lysine, comprises the following steps:
[0056] (1) Synthesis of dibasic carboxylic acid di-p-nitrophenyl ester monomer (Nx):
[0057] (a) Weigh a certain amount of p-nitrophenol, measure the same equivalent of triethylamine, add it into a single-necked flask with enough acetone, stir well at room temperature, and then store it at -78°C with dry ice and acetone Down;
[0058] (b) Measure oxalyl chloride (or succinoyl chloride or suberoyl chloride) slightly less than one-half of the p-nitrophenol equivalent and add it to an appropriate amount of acetone, mix well, and then add the triethyl chloride prepared in the previous step dropwise. In the frozen amine solution, stir at -78°C for 2h, then transfer to 25°C and stir overnight (10-16h);
[0059] (c) adding the reacted solution into a large beaker with sufficient d...
Embodiment 2
[0073] Example 2 Preparation of a lysine-based polyester amide-bovine serum albumin (BSA) nanocomposite drug delivery system (Lys-PEA@BSA)
[0074] 1, its preparation process comprises the following steps:
[0075] The polyester amide polymer aqueous solution of different lysine prepared in Example 1 was mixed with the BSA aqueous solution according to the ratio of material to protein mass ratio of 250:1, and vortexed for 5 minutes to prepare spherical nanoparticles based on Polyesteramide-BSA nanocomposite drug delivery system of lysine.
[0076] 2. Results
[0077] (1) The shape of the prepared nanoparticles was characterized by transmission electron microscopy: the nanoparticles Lys-PEA@BSA exhibited a uniform and dispersed spherical structure with a particle size of less than 100 nm.
[0078] (2) Using dynamic light scattering to characterize the stability of nanoparticles, the blank nanoparticles polyester amide polymer Lys-PEA and the drug-loaded nanoparticles Lys-PEA@...
Embodiment 3
[0080] Example 3 Preparation of a lysine-based polyester amide-insulin nanocomposite drug delivery system (Lys-PEA@INS)
[0081] 1, its preparation process comprises the following steps:
[0082] The polyester amide polymer aqueous solution of different lysine prepared in Example 1 and the insulin hydrochloric acid solution are respectively 10:1, 50:1, 100:1, 250:1, 500:1 according to the mass ratio of material to protein , mixed at a ratio of 1000:1, and vortexed for 5 minutes to prepare a lysine-based polyester amide-insulin nanocomposite drug delivery system (Lys-PEA@INS) in the form of spherical nanoparticles.
[0083] 2. Results
[0084] (1) Characterize the morphology of the prepared nanoparticles by transmission electron microscope: as image 3 As shown, the nanoparticles Lys-PEA@INS have a uniform and dispersed spherical structure with a particle size of less than 100nm.
[0085] (2) Using dynamic light scattering to characterize the stability of nanoparticles, the ...
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