Targeted drug delivery system for brain glioma as well as preparation method and use thereof
A glioma and nano-drug delivery system technology is applied to the glioma targeted drug delivery system modified by nucleic acid aptamer AS1411 and the field of preparation thereof, and can solve the problem of low drug loading, neurotoxicity and side effects, and excipients. Problems such as large injection dose to achieve the effect of inhibiting tumor growth and enhancing the inhibitory effect
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[0049] Example 1
[0050] Preparation of polyglutamic acid PGG:
[0051] 1) The sodium polyglutamate cPGA-Na (molecular weight 35000, 10g), tert-butyl glutamate hydrochloride H-Glu (otBu) 2 ·HCl (38.3g, 0.148mol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC·HCl (37.0g, 0.193mol), 1-hydroxybenzo Triazole HOBt (10.6g, 0.074mol) was dissolved in 500mL of anhydrous N,N-dimethylformamide DMF, magnetically stirred at 700rpm at 25°C for 24h, and protected by argon. The reacted solution was slowly poured into 3L of deionized water, a white precipitate was deposited, filtered, washed with 250mL of deionized water 3 times, and freeze-dried for 15 hours to obtain a white solid.
[0052] 2) Transfer the product (60 g) obtained in step 1) to a 1 L round bottom flask, add 480 mL of trifluoroacetic acid TFA, and magnetically stir at 700 rpm at 25° C. for 4 hours. TFA was removed by vacuum rotary evaporation at 40°C to obtain a yellow oil. After repeating this step twice, 800 mL o
Example Embodiment
[0053] Example 2
[0054] Preparation of polyglutamic acid PGG-PTX:
[0055] Polyglutamine glutamic acid PGG (10g), add 500mL anhydrous N,N-dimethylformamide DMF, 25℃, 700rpm magnetic stirring for 30min until completely dissolved, then add 1-(3-dimethylaminopropyl) Yl)-3-ethylcarbodiimide hydrochloride EDC·HCl (9.4g, 0.049mol) and 4-lutidine (2.6g), and continue to stir for 15 min. Add paclitaxel PTX (5.4g) into the reaction flask and stir it magnetically at 700rpm at 25℃ for 26-28h. After the reaction is complete, slowly pour the reaction solution into 1.5L hydrochloric acid aqueous solution (0.2M) in an ice bath environment, and a white precipitate separates out at 5000rpm After centrifugation for 10 min, the white precipitate obtained was dissolved in 1.5L of sodium bicarbonate (0.5M) aqueous solution, and then transferred to a dialysis bag (with a molecular weight cut-off of 10000) for 24 hours, during which all deionized water was replaced every 4 hours. When the resistivity of
Example Embodiment
[0057] Example 3
[0058] Preparation of aptamer AS1411 modified polyglutamine glutamate-paclitaxel covalent bond AS1411-PGG-PTX:
[0059] 1) Take 8mg (10nmol) of polyglutamine glutamate-paclitaxel covalent bond PGG-PTX and dissolve in 1mL of 2-(N-morpholine) ethanesulfonic acid buffer solution MES buffer (pH 6.0, 0.1M) , Where the concentration of PGG-PTX is 10μM. Then add 200mM 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride EDC·HCl and 200mM N-hydroxysuccinimide NHS successively, and stir with magnetic force at 400rpm at 25℃. After 30 minutes, the carboxyl groups on the surface of PGG-PTX are activated, and the mixed solution changes from transparent and clear to white and turbid.
[0060] 2) Transfer the solution obtained in step 1) to a 4mL ultrafiltration tube (molecular weight cut-off: 30000), and wash with DNA / RNase-free distilled water DNase / RNase free water to remove EDC / NHS. The amount of DNase / RNase free water is 4mL / Time, centrifugal force is 2500g
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