Multi-functional stealth nanoparticle co-loaded with VP and AQ4N and modified by cRGDfK polypeptide and application thereof
A peptide modification and nanoparticle technology, applied in the field of medicine, can solve problems such as impairing the prognosis of patients, and achieve the effects of strong in vitro targeting, enhanced anti-tumor effect, and enhanced curative effect.
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Embodiment 1c
[0036] Example 1 Construction of cRGDfK-pGO-VP-AQ4N and its therapeutic effect
[0037] (1) cRGDfK-pGO-VP-AQ4N dual-mode nano drug delivery system
[0038] Graphene oxide (GO) was synthesized according to the improved Hummers method. 0.05M NaOH was added to the GO suspension, and the water bath was sonicated for 5h to convert the ester groups, hydroxyl groups, epoxides and other groups existing on GO into carboxyl groups (-COOH) , concentrated hydrochloric acid to adjust the pH of the GO solution to 1, and wash the GO solution with double distilled water to neutrality. Catalyzed by EDC (5mM) and NHS (5mM), pGO was obtained by reacting the amino terminal of 8-arm PEG with the carboxyl group of GO. Add VP and AQ4N to the pGO solution in turn and stir overnight. The dosage of VP, AQ4N and pGO is 0.75mg / ml, 1mg / ml, 5mg / ml in turn, and the VP and AQ4N with aromatic ring molecular structure will be separated by π-π stacking effect Sequentially loaded on the surface of pGO to obtai...
Embodiment 2c
[0056] Example 2 Construction of cRGDfK-pGO-VP-AQ4N and its therapeutic effect
[0057] Graphene oxide (GO) was synthesized according to the improved Hummers method. 0.05M NaOH was added to the GO suspension, and the water bath was sonicated for 5h to convert the ester groups, hydroxyl groups, epoxides and other groups existing on GO into carboxyl groups (-COOH) , concentrated hydrochloric acid to adjust the pH of the GO solution to 1, and wash the GO solution with double distilled water to neutrality. Catalyzed by EDC (5mM) and NHS (5mM), pGO was obtained by reacting the amino terminal of 8-arm PEG with the carboxyl group of GO. Add VP and AQ4N to the pGO solution in turn and stir overnight. The dosages of VP, AQ4N and pGO are 0.5mg / ml, 1.5mg / ml, and 8mg / ml in sequence. AQ4N was sequentially loaded on the surface of pGO to obtain pGO-VP-AQ4N. Using BS3 catalysis, cRGDfK polypeptide was modified on the surface of nanoparticles to obtain cRGDfK-pGO-VP-AQ4N. The dosage of cata...
Embodiment 3c
[0059] Example 3 Construction of cRGDfK-pGO-VP-AQ4N and its therapeutic effect
[0060] Graphene oxide (GO) was synthesized according to the improved Hummers method. 0.05M NaOH was added to the GO suspension, and the water bath was sonicated for 5h to convert the ester groups, hydroxyl groups, epoxides and other groups existing on GO into carboxyl groups (-COOH) , concentrated hydrochloric acid to adjust the pH of the GO solution to 1, and wash the GO solution with double distilled water to neutrality. Catalyzed by EDC (5mM) and NHS (5mM), pGO was obtained by reacting the amino terminal of 8-arm PEG with the carboxyl group of GO. Add VP and AQ4N to the pGO solution in turn and stir overnight. The dosages of VP, AQ4N and pGO are 1.5 mg / ml, 0.8 mg / ml, and 7 mg / ml in turn. The VP with aromatic ring molecular structure and AQ4N was sequentially loaded on the surface of pGO to obtain pGO-VP-AQ4N. Using BS3 catalysis, the cRGDfK polypeptide is modified on the surface of nanopartic...
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