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Amphotericin b polypeptide hydrogel drug-loading system for the treatment of fungal infections

A technology for amphotericin and fungal infection, applied in antifungal agents, dipeptide components, pharmaceutical formulations, etc., can solve the problems of low biocompatibility, clinical toxicity and side effects of bioavailability, improve the transport efficiency in vivo, improve Biocompatibility, the effect of reducing clinical toxic and side effects

Active Publication Date: 2021-02-23
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to provide three amphotericin B (abbreviated as AmB) polypeptide hydrogels for the treatment of fungal infections in view of the low biocompatibility, bioavailability and clinical side effects of amphotericin B currently used in clinical practice. Glue nano drug loading system

Method used

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  • Amphotericin b polypeptide hydrogel drug-loading system for the treatment of fungal infections
  • Amphotericin b polypeptide hydrogel drug-loading system for the treatment of fungal infections
  • Amphotericin b polypeptide hydrogel drug-loading system for the treatment of fungal infections

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Weigh about 1.2g of 2-chlorotrityl chloride resin (1.0~1.2mmol / g) into the solid-phase synthesis tube, add 15mL of dichloromethane (DCM for short), swell for 20 minutes, filter, wash with DCM for 2min× 5 times. Add the first amino acid, 15mL DCM and N,N-diisopropylethylamine (DIPEA for short) to the above-mentioned solid-phase synthesis tube according to the dosage in Table 1, shake for 2 hours and drain, and wash with DCM for 2min×5 times. Add 10 mL of DCM / methanol / DIPEA (80:15:5) mixture to block the activated sites of the resin, shake for 15 min x 2 times, then drain, and wash with N,N-dimethylformamide (DMF) for 2 min x 5 times. Add 10 mL of 20% piperidine / DMF (V / V) solution and shake for 5 minutes to drain, add 10 mL of this solution and shake for 30 minutes, wash with DMF for 2 minutes x 5 times.

[0035] Add the second amino acid, 2-(7-azobenzotriazole)-tetramethyluronium hexafluorophosphate (referred to as HBTU) and 1-hydroxybenzotriazole (referred to as HOBT),...

Embodiment 2

[0040] According to the Nap-FFDKY compound prepared in Example 1, weigh 132.9 mg of the Nap-FFDKY compound and 92.41 mg of amphotericin B and dissolve them completely in 5 ml of DMF, add 41.25 μL of DIPEA, stir overnight in the dark, add glacial ether to disperse and extract, The solid was obtained by centrifugation, and was purified by HPLC after adding DMF to dissolve, and the purification conditions were as follows: the chromatographic column adopts Phenomenex Luna C 18 (50×300 mm, 10 μm), the mobile phase is methanol:water (55:45, V / V), the detection wavelength is 280 nm, and the flow rate is 15 ml / min. After preparation, the components were combined, concentrated by rotary evaporation, and freeze-dried to obtain the pure Nap-AmB product with a yield of about 69.1%.

Embodiment 3

[0042] According to the Npx-FFDKY compound prepared in Example 1, weigh 139.6 mg Npx-FFDKY and 92.41 mg amphotericin B and dissolve them completely in 5 ml DMF, add 41.25 μL DIPEA, stir overnight in the dark, add glacial ether to disperse and extract, and separate The obtained solid was purified by HPLC after adding DMF for dissolution, and the purification conditions were as follows: the chromatographic column adopts Phenomenex Luna C 18 (50×300 mm, 10 μm), the mobile phase is methanol:water (45:55, V / V), the detection wavelength is 280 nm, and the flow rate is 15 ml / min. After preparation, the components were combined, concentrated by rotary evaporation, and freeze-dried to obtain pure Npx-AmB with a yield of about 53.5%.

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Abstract

The invention belongs to the field of biological technology, and in particular relates to three amphotericin B polypeptide hydrogel nano drug-carrying systems for treating fungal infections. The invention uses the polypeptide hydrogel with great potential for clinical application, and covalently binds amphotericin B, a small-molecule hydrophobic antibacterial drug, to form an amphotericin B polypeptide hydrogel nanometer drug-loading system. The prepared nano drug loading system has high drug loading capacity, high biocompatibility and high stability, and at the same time has slow and controlled drug release behavior, easy degradation of polypeptide carrier, reduced clinical toxic and side effects and obvious antifungal effect. Amphotericin B polypeptide hydrogel nano-drug delivery system can be stored and used in the form of lyophilized powder, or diluted with water for injection for intravenous injection, or mixed with other excipients to make tablets, pills, and granules or capsules. The amphotericin B polypeptide hydrogel nano drug-loading system is suitable for the field of antifungal and fungal infectious disease treatment, and has a good application prospect.

Description

technical field [0001] The invention belongs to the field of biotechnology, and relates to a novel amphotericin B polypeptide hydrogel nano drug loading system. In particular, it relates to three amphotericin B polypeptide hydrogel nano drug loading systems for treating fungal infections. Background technique [0002] Amphotericin B is a class of polyene macrolide antibiotics produced by Streptomyces nodosum, and it is mainly used clinically for deep fungal infections. Amphotericin B can specifically bind to ergosterol on the fungal cell membrane, and inhibit the growth of fungi by affecting the permeability of the cell membrane. It is clinically used to treat severe deep fungus-induced visceral or systemic infections. Although amphotericin B is effective and no obvious drug resistance has been found so far, it can cause strong nephrotoxicity, and long-term use will cause damage to the kidney and circulatory system. The clinical symptoms are proteinuria, low Potassium, ane...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/64A61K9/06A61K31/7048A61K38/05A61P31/10
CPCA61K9/06A61K31/7048A61K38/05A61K2300/00
Inventor 舒畅丁黎李腾飞
Owner CHINA PHARM UNIV
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