Passive targeting antitumor prodrug of solid tumor and preparation method thereof
A solid tumor, targeted technology, applied in the field of anti-tumor drugs, can solve the problems of deposition, functional impact, not easy to degrade, etc.
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Embodiment 1
[0041] Embodiment 1 Solid tumor passive targeting anticancer prodrug P(A) of the present invention n preparation of
[0042] 1. Preparation of small molecule pectin:
[0043] Weigh 13.3g of pectin, add 1L of distilled water and stir to dissolve, adjust the pH with 5M NaOH to make the pH = 13, react at 65°C for 10h, and stop the reaction. Use concentrated hydrochloric acid to adjust the reaction solution to neutrality, filter with a millipore with a molecular weight cut-off of 30,000, and then filter the filtrate through a millipore with a molecular weight cut-off of 10,000, collect the solid with a molecular weight cut-off of 10,000 that does not pass through, and concentrate to dryness under reduced pressure. , vacuum-dried to obtain small molecule pectin with a molecular weight of 10,000 to 30,000.
[0044] 2. Loading of doxorubicin and cross-linking of small molecule pectin:
[0045] Weigh 1g of small molecule pectin doxorubicin with a molecular weight of 10,000 to 30,00...
Embodiment 2
[0056] Embodiment 2 Solid tumor passive targeting anticancer prodrug P(A) of the present invention n preparation of
[0057] 1. Preparation of small molecule pectin:
[0058] Weigh 13.3g of pectin, add 1L of distilled water and stir to dissolve, adjust the pH with 5M NaOH to make the pH = 13, react at 65°C for 10h, and stop the reaction. Use concentrated hydrochloric acid to adjust the reaction solution to neutrality, filter it with a millipore with a molecular weight cut-off of 10,000, and then dialyze the filtrate through a dialysis bag with a molecular weight cut-off of 7,000, collect the dialysate, concentrate it to dryness under reduced pressure, and dry it under vacuum to obtain a molecular weight of 7,000-10,000 small molecule pectin.
[0059] 2. Loading of doxorubicin and cross-linking of small molecule pectin:
[0060] Weigh 1g of small molecule pectin doxorubicin with a molecular weight of 7000-10000 and add it to the reaction bottle, add 100ml of water, stir to d...
Embodiment 3
[0063] Example 3 The solid tumor passive targeting anticancer prodrug P(A) of the present invention n preparation of
[0064] 1. Preparation of small molecule pectin:
[0065] Weigh 13.3g of pectin, add 1L of distilled water and stir to dissolve, adjust the pH with 5M NaOH to make the pH = 13, react at 65°C for 10h, and stop the reaction. The reaction solution was adjusted to neutrality with concentrated hydrochloric acid, filtered using a millipore with a molecular weight cut-off of 50,000, and the filtrate was dialyzed for 48 hours using a dialysis bag with a molecular weight cut-off of 20,000, and the distilled water was changed every 3 hours. The dialysate is concentrated to dryness under reduced pressure, and vacuum-dried to obtain small molecule pectin with a molecular weight of 20,000-50,000.
[0066] 2. Loading of doxorubicin and cross-linking of small molecule pectin:
[0067] Weigh 1g of small molecule pectin with a molecular weight of 20,000-50,000 and add it to ...
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