Preparation method and application of cyclosporine A-loaded efficient brain-targeted drug delivery system

A technology of drug delivery system and loading ring, which is applied in the direction of cardiovascular system diseases, non-effective ingredients of polymer compounds, cyclic peptide ingredients, etc., can solve the problems of cell damage in ischemic areas, blood-brain barrier damage, etc., and reduce nerve cell damage , the effect of protecting the blood-brain barrier

A technology of drug delivery system and loading ring, which is applied in the direction of cardiovascular system diseases, non-effective ingredients of polymer compounds, cyclic peptide ingredients, etc., can solve the problems of cell damage in ischemic areas, blood-brain barrier damage, etc., and reduce nerve cell damage , the effect of protecting the blood-brain barrier

CN112675149AActive Publication Date: 2021-04-20AIR FORCE MEDICAL UNIV
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  • Preparation method and application of cyclosporine A-loaded efficient brain-targeted drug delivery system
  • Preparation method and application of cyclosporine A-loaded efficient brain-targeted drug delivery system
  • Preparation method and application of cyclosporine A-loaded efficient brain-targeted drug delivery system

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Embodiment Construction

[0023] 1 Research Methods

[0024] 1.1 Preparation and characterization of CsA@Fn

[0025] (1) Preparation of CsA@Fn by solvent-based denaturation / renaturation self-assembly method: Utilizing the characteristics of ferritin denaturation in acetone and renaturation in water, CsA@Fn was prepared by solvent evaporation method. Weigh 50 mg of ferritin, add it to 50 ml of mixed solvent (acetone: water = 55:45), seal and stir at room temperature for 30 minutes to denature ferritin; weigh 150 mg of CsA, dissolve it in 0.5 ml of acetone, and add it to the above ferritin solution , sealed and stirred at room temperature for 10 minutes to fully mix ferritin and CsA evenly; add the above solution to an evaporating dish, stir at room temperature to promote the volatilization of acetone, and after 10 hours, use a microporous filter membrane with a pore size of 0.22 μm to remove the unwrapped ferritin CsA in, that is, CsA@Fn.

[0026] (2) Characterization of particle size and potential of...

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Abstract

The invention relates to the field of biological pharmacy, and discloses a preparation method and application of a cyclosporine A-loaded efficient brain-targeted drug delivery system. The drug delivery system is composed of CsA and Fn; by utilizing the characteristic that ferritin is denatured in acetone and can be renatured in water, the CsA is wrapped in a cage structure (CsA(at)Fn) of the Fn through a solvent evaporation method; the CsA(at)Fn can be mediated by transferrin receptors on the surfaces of brain capillary endothelial cells to penetrate through a blood brain barrier and be accumulated in an ischemic area; on one hand, the CsA(at)Fn van protect the integrity of the blood brain barrier and reduce accumulation of inflammatory factors in a cerebral ischemic area; and on the other hand, the CsA(at)Fn taken by neuronal cells can inhibit the opening of mitochondrial permeability conversion pores of the neuronal cells, reduce the release of mitochondrial ROS and cytochrome C, inhibit the apoptosis of the neuronal cells and play a role in neuroprotection.

Description

technical field [0001] The invention relates to the field of biopharmaceuticals, in particular to a novel high-efficiency targeted drug delivery system for treating cerebral ischemia / reperfusion injury. Background technique [0002] Ischemic stroke is one of the leading causes of disability and death. At present, the main treatment for ischemic stroke is to restore cerebral blood perfusion in the ischemic area as soon as possible, but when the ischemic brain tissue is reperfused with blood, it will cause a series of re-injuries. The mechanism of cerebral ischemia / reperfusion injury is complex, including many pathophysiological changes, such as energy metabolism disorder, oxidative stress, excitatory amino acid toxicity, and inflammatory injury. The latest research shows that mitochondria play an important role in cerebral ischemia / reperfusion injury. During cerebral ischemia, the supply of oxygen and glucose in the cerebral ischemic tissue is insufficient, and the synthesi...

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Application Information

Patent Timeline
20 Apr 2021
Publication
CN112675149A
IPC
A61K9/51; A61K47/42; A61K38/13; A61P9/10
Inventors
周四元; 刘道洲