A kind of pH sensitive mixed micelles and its preparation method and application
A mixed micellar and sensitive technology, applied in the direction of pharmaceutical formulations, drug combinations, organic active ingredients, etc., can solve the problems of multidrug resistance, low bioavailability of chemotherapy drugs, etc., and achieve long drug circulation time and good size Tissue retention, effect of prolonging action time
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Embodiment 1
[0045] figure 1 It is a schematic diagram of the pH-sensitive polymer prodrug of the embodiment of the present invention. From figure 1 It can be seen that the pH-sensitive mixed micelles of the present invention have a double-layer structure, the outer layer is PEG with good hydrophilicity, the inner layer is hydrophobic drug DOX, and TPGS is also connected to it by amphiphilicity.
[0046] (a) Preparation of pH-sensitive polymeric prodrugs
[0047] With 20 mL of anhydrous DCM (dichloromethane) as the solvent and 694 μL of TEA as the catalyst, 2.00 g of mPEG with a molecular weight of 2000 was dissolved and then added TEA dropwise, and 1.0078 g of chloroformic acid was dissolved in 10 mL of anhydrous DCM as the solvent. After the phenyl phenyl ester was dissolved, it was added dropwise at 0°C, and reacted at 30°C for 24 hours. The solution was rotary evaporated at 28°C to remove DCM, anhydrous ether was added, the precipitated white substance was collected, reprecipitated ...
Embodiment 2
[0054] The particle size distribution characterization of the polymer prodrug and a pH-sensitive mixed micelle, the specific steps are as follows:
[0055] The polymer prodrug was made into a solution with a concentration of 500 μg / mL, and the polymer prodrug and TPGS were mixed at a molar ratio of 3:1. Measurement. The results of polymer prodrug testing are as follows: image 3 Shown in A, the average particle diameter of this polymer prodrug micelle is 204 nm, and PDI is 0.232; The detection result of mixed micelle is as follows image 3 As shown in B, the particle size distribution is uniform, the average particle size is 144 nm, and the PDI is 0.187. The particle size distribution of this mixed micelle is narrow, and it is significantly different from the particle size of the polymer prodrug, which indicates that a new Micellar rather than physical mixing of polymeric prodrug and TPGS.
Embodiment 3
[0057] Morphological characterization of polymer prodrugs and a pH-sensitive mixed micelle, the specific steps are as follows:
[0058] The polymer prodrug and a pH-sensitive mixed micelle were formulated into a 100 μg / mL solution with distilled water, dropped onto the copper grid, and dried overnight (14 hours). The morphology was observed with a transmission electron microscope. From the results of transmission electron microscopy, we can see that the polymer prodrug presents a spherical morphology with good monodispersity ( Figure 4 A), pH-sensitive mixed micelles exhibit a spherical structure with good monodispersity ( Figure 4 B).
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