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Preparation of rifampicin nano drug delivery system and application of rifampicin nano drug delivery system in prevention and treatment of Parkinson's disease

A nano-drug delivery system, rifampicin technology, applied in nano-drugs, nervous system diseases, nano-technology, etc., can solve the problems of low local aggregation concentration, poor stability, low water solubility, etc., to improve bioavailability, increase Stability, effect of increasing water solubility

Pending Publication Date: 2022-04-08
中山大学附属第八医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to the analysis, there are still the following deficiencies in the use of rifampicin in the treatment of neurological diseases: (1) rifampicin has strong fat solubility, but its water solubility is low, and its stability in internal circulation is poor; The local concentration of substantia nigra-striatum is much lower than its working concentration; 3) The peripheral toxicity of rifampicin, such as liver toxicity, limits the use of its higher concentration

Method used

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  • Preparation of rifampicin nano drug delivery system and application of rifampicin nano drug delivery system in prevention and treatment of Parkinson's disease
  • Preparation of rifampicin nano drug delivery system and application of rifampicin nano drug delivery system in prevention and treatment of Parkinson's disease
  • Preparation of rifampicin nano drug delivery system and application of rifampicin nano drug delivery system in prevention and treatment of Parkinson's disease

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Effect test

Embodiment 1

[0040] Example 1 Preparation of rifampicin nano drug delivery system (TTBZ-PEG-PCL@rif polymer micelles)

[0041] (1) Preparation of PEG-PCL@rifampicin

[0042] Such as figure 1 As shown, rifampicin is loaded in the PEG-PCL carrier by means of self-assembly (Self-assembly), and the PEG-PCL@rif (PEG-PCL@rifampin) solution is prepared, and the specific preparation method is as follows:

[0043] Weighed 1mg of rifampicin (rifampicin, rif) and 10mg of Allyl-PEG-PCL (PEG-PCL) lyophilized powder (purchased from Shunna Nano Co., Ltd.) and dissolved them in 1mL of DMF to form an organic phase, and subjected them to ultrasonication (130W ) was added dropwise into 10 mL of deionized water. Place the above-mentioned mixed solution in a dialysis bag with a molecular weight cut-off of 14,000, dialyze with water for more than 12 hours, collect the solution in the dialysis bag, and use a 0.45um microporous membrane to remove hydrophobic drug aggregates to obtain PEG- PCL@rif solution.

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Embodiment 2

[0048] Embodiment 2 TTBZ-PEG-PCL@rif (referred to as drug-loaded micelles) characterization and physical and chemical properties

[0049] (1) Determination of TTBZ-PEG-PCL@rif morphology characterization

[0050] Pipette 10 μL of drug-loaded micelles, and slowly drop them into a 200-mesh copper grid, dry naturally, and then stain the sample with 0.3% phosphotungstic acid for 1 minute. After the staining is completed, use a transmission electron microscope (TEM) to observe its appearance , particle size.

[0051] pass Figure 5 It can be seen from the transmission electron microscope (TEM) that the particle size of TTBZ-PEG-PCL@rif nanoparticles is about 100nm, and the polymer micelles are in a circular stable distribution. The stable particle size distribution provided the prerequisite for the micelles to target dopamine neuronal vesicular monoamine transporter 2 (VMAT2) through a passive targeting effect to increase the local concentration of rifampicin.

[0052] (2) 1HNMR...

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Abstract

The invention belongs to the technical field of nano drug delivery systems, and particularly relates to preparation of a rifampicin nano drug delivery system and application of the rifampicin nano drug delivery system to prevention and treatment of Parkinson's disease. Rifampicin is loaded into a PEG-PCL nano drug delivery system for the first time, and the PEG-PCL nano drug delivery system is prepared into polymeric micelles; tTBZ molecules are modified on the surface of the polymer micelle and can be specifically combined with VMAT2. Compared with a traditional rifampicin medicament type, the carrier (PEG-PCL) is weak in cytotoxicity, the micelle formed by a PEG-PCL hydrophilic block has the structural characteristics of a hydrophobic inner core and a hydrophilic outer core, the water solubility of the rifampicin is increased, and the stability of the rifampicin circulating in a body is improved; the rifampicin nano-particle has a targeting drug delivery capability, and improves the local aggregation concentration of rifampicin in dopaminergic neurons, so that the bioavailability of the drug is improved, the protection effect of the drug on neurological diseases such as Parkinson's disease is improved, and the peripheral toxic and side effects of the drug are reduced.

Description

technical field [0001] The invention belongs to the technical field of nano drug delivery system, in particular to the preparation of a rifampicin nano drug delivery system and its application in the prevention and treatment of Parkinson's disease. Background technique [0002] Rifampicin (Rif) is a semi-synthetic broad-spectrum antibacterial drug of the rifamycin class, common name: rifampicin, English name: RIFAMPICINTABLETS. As a classic, effective and safe anti-tuberculosis drug, rifampicin has antibacterial activity against a variety of pathogenic microorganisms. Rifampicin is well absorbed after oral administration, and the plasma concentration reaches its peak within 1.5 to 4 hours after taking the drug. This product is used in combination with other anti-tuberculosis drugs for the initial treatment and retreatment of various tuberculosis, including the treatment of tuberculous meningitis. In addition, rifampicin also has potential neuroprotective effects. Studies ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K47/34A61K31/496A61P25/16B82Y5/00B82Y40/00
CPCY02A50/30
Inventor 陶恩祥李耀林淡钰卜璐璐梁嫣然陈颖井秀娜彭素丹
Owner 中山大学附属第八医院