Anoxia-responsive nano drug carrier and preparation method and application thereof
Inactive Publication Date: 2019-05-21
TIANJIN UNIV
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[0003] At present, tremendous technological progress has been made in this field, however, one obstacle limiting the translation of nanomedicines to the clinic stems from the controlled release of entrapped drugs.
Liposome-encapsulated cisplatin SPI-77 showed greater intratumoral accumulation than free cisplatin, however, failed phase III clinical trials due to poor drug bioavailability upon drug release
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Embodiment 1
[0059] In this embodiment, the nano-drug is obtained by reacting 2-nitroimidazole with hyaluronic acid to obtain an amphiphilic drug carrier, and then the amphiphilic drug carrier is self-assembled with the hydrophobic drug to obtain a nano-drug.
[0060] Prepare nano-medicine by the following method, specifically comprising the following steps:
[0061] (1) Synthesis of amphiphilic drug carrier
[0062] Weigh 149.6mg of 2-nitroimidazole and dissolve it in 10mL N,N-dimethylformamide, add 280mg of potassium carbonate to the above solution, and add the solution in 1mL N,N-dimethylformamide dropwise under room temperature and magnetic stirring N-Boc-bromoethylamine solution (200mg, 400mg or 600mg) of methyl formamide, transferred to 70°C, 80°C or 90°C oil bath, and reacted for 3h, 4h or 5h. The insoluble matter was removed by suction filtration, washed with methanol, and the clear solution was concentrated by rotary evaporation to obtain an orange-yellow solid. The obtained sol...
Embodiment 2
[0067] The intermediate and final products of 2-nitroimidazole grafted on hyaluronic acid were verified by proton nuclear magnetic spectroscopy, and the results are shown in figure 1 .
[0068] figure 1 A is the NMR spectrum of 2-nitroimidazole, after reacting with N-Boc-bromoethylamine, the b position H is replaced to obtain figure 1 The NMR spectrum of B2-nitroimidazole derivatives; the activated -COOH on the hyaluronic acid and the amino group on the 2-nitroimidazole derivatives undergo a condensation reaction to obtain HA-NI, from figure 1 C It can be seen that HA-NI and figure 1 The H of B 2-nitroimidazole derivatives has a similar chemical environment.
Embodiment 3
[0070] A UV-Vis spectrophotometer was used to verify the successful grafting of 2-nitroimidazole on hyaluronic acid and the fact that both drugs were encapsulated by the amphiphilic carrier.
[0071] see results figure 2 As shown, in the ultraviolet-visible absorption spectrum, HA-NI shows the ultraviolet absorption peak of NI at 330nm, which further proves the grafting of NI on HA; the ultraviolet-visible absorption spectrum of NPs also shows that HA-NI is at 330nm, Ce6 The peak shape at 400nm and TPZ at 470nm proved that Ce6 and TPZ were simultaneously encapsulated in the HA-NI nanomedicine.
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Abstract
The invention provides an anoxia-responsive nano drug carrier and a preparation method and application thereof. The nano drug comprises a hydrophobic seed core and an amphiphilic shell, wherein the hydrophobic seed core comprises chlorin e 6 and tirazamine, and the amphiphilic shell is hydrophilic macromolecular hyaluronic acid modified by hydrophobic molecule 2-nitroimidazole, the hydrophobic seed core and the amphiphilic shell form a non-conjugated position relationship by hydrophilic and hydrophobic forces. According to the preparation method, the nano drug is finally successfully preparedby optimizing the preparation process, the particle size of the product is moderate and controllable, the nano drug is irradiated by laser for photodynamic treatment, oxygen is consumed, and hydrophobic molecules 2-nitroimidazole is transformed into hydrophilic molecules 2-aminoimidazole under the anoxic condition, and the nano drug is dissolved, the drug release is achieved, the chemotherapy toxicity of the chemotherapeutic drug tirazamine is activated under the anoxic condition, the combined treatment is synergistic, cancer cells are effectively killed, the application prospect is wide and the market value is huge.
Description
technical field [0001] The invention belongs to the technical field of nanomaterials, and relates to a hypoxia-responsive nanomedicine carrier and its preparation method and application. Background technique [0002] The incidence of breast cancer is very high among women all over the world, especially triple-negative breast cancer (MDA-MB-231), which has a particularly high mortality rate, and currently there is no effective treatment. Clinically, chemotherapy is usually used for postoperative treatment. However, chemotherapy has the disadvantages of high systemic toxicity, low uptake in lesion sites, and prone to multidrug resistance. Over the past few decades, nanomedicines have emerged as very promising tools for improving the therapeutic index of conventional chemotherapeutic drugs. The size of nano-drugs is between 1 and 100nm. Due to the high permeability and retention effect of solid tumors, the drug enrichment in tumors can be selectively realized, and at the same...
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