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A kind of pH-sensitive and active oxygen-sensitized pluronic polymer and its preparation method and application

A Pluronic and polymer technology, which is applied in the directions of organic active ingredients, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. problem, to achieve the effect of improving stability

Active Publication Date: 2021-04-06
ANHUI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, its reversal performance is related to its hydrophilic-hydrophobic ratio (HLB). If the hydrophilicity is strong, the reversal effect will be low (for example, pluronic127 basically has no reversal performance), and it is also easy to cause the assembled blank micelles to be intolerant to dilution; if the hydrophobicity is strong, the reversal effect will be low. High performance, but also high toxicity

Method used

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  • A kind of pH-sensitive and active oxygen-sensitized pluronic polymer and its preparation method and application
  • A kind of pH-sensitive and active oxygen-sensitized pluronic polymer and its preparation method and application
  • A kind of pH-sensitive and active oxygen-sensitized pluronic polymer and its preparation method and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] A pH-sensitive and active oxygen-sensitized pluronic polymer, the structure of which is shown in formula VI:

[0057]

Embodiment 2

[0059] Preparation method of pH-sensitive and active oxygen-sensitized pluronic polymer:

[0060] The synthetic route of pH-sensitive and ROS-sensitized pluronic polymers is as follows:

[0061]

[0062] The preparation method of the pH-sensitive and active oxygen-sensitized pluronic polymer comprises the following steps:

[0063] Preparation of the compound shown in S1, formula III:

[0064] To a 100mL round-bottomed reaction flask, add Plavonic P123 (10g, 1.7mmol) shown in formula I, 2,2,2-trifluoro-N-(2-methoxy-[1,3 ]-dioxolane-4-methyl)acetamide (2.35g, 10.25mmol), pyridinium p-toluenesulfonate (Py-PTSA) (8.54mg, 0.034mmol), vacuumize with oil pump, 120°C oil bath Under the condition of reaction 8h. After the reaction is over, let it stand until it returns to room temperature. Dissolve the reactants with dichloromethane and dilute with 0.5% NaHCO 3 solution and saturated brine for extraction, the lower organic phase was collected, and rotary evaporated to obtain th...

Embodiment 3

[0073] Preparation of blank micelles and their particle size and morphology:

[0074] 1. Preparation of pranik P123 blank micelles:

[0075] Weigh 30mg of Pluronic P123 into a 25mL round-bottom bottle, add 1mL of anhydrous dichloromethane, spin steam at 50°C for 30min, and then put it in a 60°C oven to dry overnight; then put the round-bottom bottle into a 50°C water bath Hydrate and heat for 15 minutes, add 10 mL of deionized water (pH 7.4) at 50 °C to the bottle, stir and vortex quickly, filter the solution with a 0.22 μm filter head, and obtain a milky white or transparent micellar emulsion, which is Pluronic P123 blank micelles.

[0076] The particle size distribution and morphology of the nanomicelles were detected by DLS and transmission electron microscopy, and the particle size distribution is shown in Figure 3a As shown, the topographic feature map is shown as Figure 3c .

[0077] Depend on Figure 3a , Figure 3c It can be seen that the blank micelles of Plur...

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Abstract

The invention discloses a pH-sensitive and active oxygen-sensitized Planic polymer. The structure of the polymer is shown in formula VI: at the same time, the invention also discloses the preparation method of the above-mentioned polymer, which specifically includes step S1: shown in formula III Preparation of compound; step S2: preparation of compound shown in formula IV; step S3: preparation of pH-sensitive and active oxygen-sensitized pluronic polymer shown in formula VI; at the same time, the present invention combines the polymer prepared above with antitumor Drug compounding is applied to the drug delivery system, and the above-mentioned polymer is prepared into drug-loaded micelles. The above-mentioned polymer disclosed in the present invention uses Pluronic P123 as the core, and is designed according to the principle of drug combination. On both sides of Pluronic P123 Orthoester and vitamin E succinate groups are sequentially combined at the end of the chain. The polymer prepared by using the above drug combination theory not only shows significant reversal of multidrug resistance of tumor cells but also has ideal drug release. relatively stable.

Description

technical field [0001] The invention belongs to the technical field of preparation of pluronic polymer carriers, and in particular relates to a pH-sensitive and active oxygen-sensitized pluronic polymer, a preparation method and application thereof. Background technique [0002] Drug chemotherapy has been one of the main means of clinical treatment of cancer. However, traditional small-molecule anticancer drugs are often metabolized quickly in the body and have short half-lives, which eventually lead to lower drug accumulation in tumor sites and lower therapeutic effects. In order to obtain a better antitumor effect, it is often necessary to repeat the administration several times clinically. This will not only increase the cost of the patient, but the side effects of the drug will also bring serious negative effects to the patient, such as hair loss, loss of appetite, and weight loss. In addition, long-term administration of single-drug chemotherapy can also cause drug re...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G65/332C08G65/337C08G65/333A61K31/704A61K47/10A61P35/00
Inventor 唐汝培程旭杨霞
Owner ANHUI UNIVERSITY
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