Preparation and Application of a Triblock Polymer Based on Cholesterol Polyethylene Glycol Penetrating Peptide
A technology of polyethylene glycol and cholesterol, which is applied in the direction of non-active ingredients of polymer compounds, medical preparations of non-active ingredients, drug combinations, etc., and can solve problems such as drug aggregation
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0052] Below in conjunction with specific embodiment, further illustrate the present invention. It should be understood that these embodiments are only to specifically illustrate the present invention, and are not intended to limit the scope of the present invention. In the following implementation cases, unless otherwise specified, all are conventional methods in the art or methods suggested by manufacturers. Unless otherwise defined, all professional and scientific terms used herein have the same meanings as those commonly understood by those skilled in the art. Example 1: Synthesis of penetrating peptide (WRK)-polyethylene glycol-cholesterol (WRK-PEG-Chol).
[0053] Accurately weigh 500 mg of cholesterol polyethylene glycol carboxyl (Chol-PEG2000-COOH), 114.6 mg of EDCI and 17.2 mg of NHS into a 50 mL reaction bottle, add 2 mL of DMF to dissolve, and stir the mixture at room temperature for 2 h. After the activation was completed, the W5R4K peptide was dissolved with a sm...
Embodiment 2
[0055] Embodiment 2: the synthesis of folic acid-polyethylene glycol-cholesterol (FA-PEG-Chol)
[0056] Weigh an appropriate amount of target material folic acid FA52.96g (0.12mmol), DMAP 14.64g (0.12mmol), EDCI23.04 (0.12mmol) and triethylamine (TEA), add them together and dissolve in anhydrous di Add HO-PEG2000-Chol in DMSO solution slowly and uniformly while stirring (this operation is performed under a magnetic stirrer), and the entire reaction system is protected from light. The reaction was monitored by spotting samples on a thin-layer plate. The ratio of the developing system was still dichloromethane:methanol=10:1. The developer was pre-saturated in the chromatographic tank for 15 minutes, and the 5% ethanol solution of phosphomolybdic acid was used for color development at high temperature and simultaneously used iodine vapor for color development. After the color is detected by spotting the plate and the reaction is complete, the reaction is stopped and processed. A...
Embodiment 3
[0058] Embodiment 3: the liposome preparation method of the triblock polymer modification of cholesterol polyethylene glycol penetrating peptide
[0059] Prepare the liposomes by thin film hydration-rotary evaporation method, weigh DOTAP: Chol: mPEG-Chol: FA-PEG-Chol: WRK-PEG-Chol=50:45:2:1:2 (molar ratio) In a 4mL EP tube, add an appropriate amount of chloroform to 1mL, ultrasonically dissolve, and rotate under reduced pressure at 37°C to form a film (50rpm) for 1h, remove the organic solvent, and obtain a uniform film; then add 1.5mL glucose (5%) solution, 75rpm, Hydrate at 60°C for 50min; transfer the above liquid to a 10mL EP tube, dilute to 1.5mL with glucose (5%), and sonicate with a 110W (130*85%) probe-type ultrasonic instrument in an ice-water bath at 60°C for 3min (work for 3s, interval of 3s); through a 0.45 μm water filter membrane, the resulting solution is a liposome colloid solution. The average particle size and potential were measured by the Malvern laser par...
PUM
| Property | Measurement | Unit |
|---|---|---|
| particle size | aaaaa | aaaaa |
| particle diameter | aaaaa | aaaaa |
Abstract
Description
Claims
Application Information
Login to View More