Unlock instant, AI-driven research and patent intelligence for your innovation.

Brain-targeted nano-drug delivery system and preparation method thereof

A nano-drug and delivery system technology, applied in the field of biomedicine, can solve the problems of difficulty in crossing the blood-brain barrier, low bioavailability, short half-life, etc., achieving good biocompatibility and biodegradability, great development potential, delayed release effect

Active Publication Date: 2021-05-04
JINAN UNIVERSITY
View PDF5 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Rifampicin (RIF) is a semi-synthetic broad-spectrum antibiotic with anti-β-amyloid, anti-inflammation, anti-apoptosis, and neuroprotective effects, because of its strong hydrophobicity, high toxicity, short half-life, The characteristics of low bioavailability and difficulty crossing the blood-brain barrier make it difficult to be applied to the treatment of AD

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Brain-targeted nano-drug delivery system and preparation method thereof
  • Brain-targeted nano-drug delivery system and preparation method thereof
  • Brain-targeted nano-drug delivery system and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Take 2100mg PLA-PEG-NH 2and 100 mg DTPA were dissolved in 10 ml DMSO. After adding about 1ml of triethylamine dropwise, react at 45°C for 12h. After the reaction, the reaction solution was dialyzed for 24 hours with a dialysis bag with a molecular weight cut-off of 3500 Da, during which the water was changed 6 times. Finally, the dialysate in the bag was freeze-dried to obtain PLA-PEG-DTPA. figure 1 PLA-PEG-NH 2 and the infrared spectrum of PLA-PEG-DTPA. figure 2 for PLA-PEG-DTPA 1 H NMR spectrum.

Embodiment 2

[0087] Take 200mg of gadolinium chloride hexahydrate and 100mg of PLA-PEG-DTPA prepared in Example 1 and dissolve them in a mixed solvent of 15ml of water / dioxane (1:2v / v). Then the pH value of the mixed raw material solution was adjusted to 6.0-6.5 with 0.1M NaOH solution, and the reaction mixture was stirred at 50° C. for 4 h. Then, the reaction mixture was dialyzed for 24 h with a dialysis bag with a molecular weight cut-off of 1000 Da, during which the water was changed 6 times. Freeze-dry the dialysate in the bag to obtain PLA-PEG-Gd. image 3 It is the morphology (A) and particle size distribution (B) of PLA-PEG-Gd. Figure 4 Magnetic resonance imaging properties of PLA-PEG-Gd.

Embodiment 3

[0089] 100 mg each of PLA-PEG-Gd and PLA-PEG-Mal prepared in Example 2 were dissolved in tetrahydrofuran and set aside. Take rifampicin 100mg and dissolve in tetrahydrofuran, set aside. The rifampicin solution was added dropwise to the PLA-PEG-Mal mixture of the above two PLA-PEG-Gd on an ultrasonic cell pulverizer while ultrasonicating, and ultrasonically dispersed for 15 minutes. The ratio of PLA-PEG-Gd and PLA-PEG-Mal is 1:1, and rifampicin with the same quality as PLA-PEG-Gd is added. The above mixture of rifampin and polymer was added dropwise to 25 mL of water under the condition of ultrasound, and the ice bath was sonicated for 30 minutes. The ultrasonic solution was transferred to a 3500Da dialysis bag for dialysis in an ice bath for 24 hours, during which the water was changed 6 times. The dialysate in the bag was freeze-dried to obtain RIF@PLA-PEG-Gd / Mal.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Particle sizeaaaaaaaaaa
Concentrationaaaaaaaaaa
Login to View More

Abstract

The invention relates to a brain-targeted nano-drug delivery system and a preparation method thereof, and belongs to the technical field of biological medicines. According to the invention, RVG29 is coupled to the surfaces of PLA-PEG nano-particles by introducing a binding site Mal group; rifampicin and gadolinium nano-particles are loaded at the same time, so that a novel brain-targeted nano-drug delivery system is constructed; the system has good biocompatibility, brain targeting property and drug controlled release property; rifampicin can be promoted to penetrate through a blood-brain barrier; aggregation of medicines in the animal brain is realized; the bioavailability of the medicines is improved; and meanwhile, the nano delivery system can reduce deposition of A beta in brain tissues of a mouse suffering from the Alzheimer disease and reduce apoptosis of neurons, so that cognitive impairment of the mouse is improved, and an efficient and safe strategy is provided for diagnosis and treatment of the Alzheimer disease. The brain-targeted nano-drug delivery system disclosed by the invention has potential application prospects in the fields of neurodegenerative diseases and elderly medicine.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a brain-targeted nano drug delivery system and a preparation method thereof. Background technique [0002] Alzheimer's disease (Alzheimer disease, AD) is a neurodegenerative disease, the main pathological features are Aβ (β-amyloid protein) deposition and hyperphosphorylation of Tau protein. So far, no effective drugs have been developed to treat AD from the etiology. Rifampicin (RIF) is a semi-synthetic broad-spectrum antibiotic with anti-β-amyloid, anti-inflammation, anti-apoptosis, and neuroprotective effects, because of its strong hydrophobicity, high toxicity, short half-life, Due to its low bioavailability and difficulty crossing the blood-brain barrier, it is difficult to be applied to the treatment of AD. In recent years, functional nanomaterials have been used in the treatment of neurodegenerative diseases due to their good biocompatibility and drug del...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/496A61K47/34A61K47/42A61P25/28A61K49/12A61K49/14
CPCA61K31/496A61K47/34A61K47/42A61P25/28A61K49/12A61K49/14
Inventor 毕伟朱丽红周锐意
Owner JINAN UNIVERSITY