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Mitochondria targeted external medicinal preparation

A technology for topical drugs and mitochondria, which is applied in the direction of drug combination, drug delivery, and medical preparations of non-active ingredients. Permeability, promote release, help transdermal absorption effect

Active Publication Date: 2020-12-08
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the commonly used transdermal preparations often have two major defects, (1) the transdermal performance of the preparation is poor, and the drug stays more on the surface of the skin to affect the final drug effect; (2) the drug lacks intracellular secondary targeting , cannot function at a specific site of action

Method used

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  • Mitochondria targeted external medicinal preparation
  • Mitochondria targeted external medicinal preparation
  • Mitochondria targeted external medicinal preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1 Preparation of Peptide Dendrimers

[0060] 1. In the present invention, the mitochondrial targeting phospholipid is a drug carrier peptide dendrimer (G2), and its structural formula is:

[0061]

[0062] Its preparation method is as follows:

[0063] 1) Amidation reaction of lysine and BOC-protected arginine

[0064] According to lysine, BOC protection of arginine, condensing agent [equimolar 1-hydroxybenzotriazole (HOBT) and benzotriazole-N,N,N',N'-tetramethyluronium hexafluoro Phosphate (HBTU)], the molar ratio of the organic base is 1:3:3:1, and the metering of lysine, BOC protected arginine, HOBT, HBTU, DIPEA and DMF.

[0065] Add the above-mentioned raw materials into a branch bottle under ice bath and nitrogen protection, then add an organic base and anhydrous dimethylformamide to dissolve the solid drug, stir and react for 24-48 hours, then extract the reaction solution with ethyl acetate, and with saturated NaHCO 3 , dilute hydrochloric acid, sa...

Embodiment 2

[0091] Dissolve 2 mg of the drug carrier peptide dendrimer (G2) prepared in Example 1, 6 mg of soybean lecithin, 0.5 mg of cholesterol, 1 mg of Tween 80, 1 mg of sodium deoxycholate and 1 mg of coenzyme Q10 in 25 mL of chloroform-methanol mixed solvent medium (the volume ratio of chloroform to methanol is 2:1), and then the solvent was removed by rotary evaporation under reduced pressure to obtain a dry lipid film, which was hydrated with 2 mL of deionized water, ultrasonicated in a water bath at 50°C for 15 min, followed by ultrasonic probe for 5 min, Obtain liposome solution. Then centrifuge at a speed of 3500r / min for 3min to remove free coenzyme Q10, and the obtained supernatant is the mitochondria-targeted liposome loaded with coenzyme Q10.

[0092] Dissolve 6 mg of soybean lecithin, 0.5 mg of cholesterol, 1 mg of Tween 80, 1 mg of sodium deoxycholate and 1 mg of coenzyme Q10 in 25 mL of chloroform-methanol mixed solvent (the volume ratio of chloroform and methanol is 2:1...

Embodiment 3

[0098] The poloxamer solution, chitosan solution and liposome solution are miscible, and the ratio of 30% poloxamer 188 and 30% poloxamer 407 to 1% low-density chitosan and liposome is 4 : 0.5: 0.5 (v: v: v), the viscous transparent fluid prepared according to this ratio forms a gel at 37°C, but cannot form a gel at room temperature and low temperature, and has heat sensitivity. The gel phase transition diagram is shown in figure 2 .

[0099] The mitochondrial targeting liposomes loaded with coenzyme Q10, the liposomes loaded with coenzyme Q10 plus surfactant, the ordinary liposomes loaded with coenzyme Q10, the mitochondrial targeted liposomes loaded with Dil, and Dil-loaded surfactant liposomes and Dil-loaded ordinary liposomes with prepared 30% poloxamer 188 and 30% poloxamer 407, 1% low-density chitosan according to poloxamer: lipid Body: Chitosan ratio 8:1:1 (v:v:v) mixed, at 37 ℃ to form the corresponding liposome gel.

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Abstract

The invention discloses a mitochondria targeted external medicinal preparation which comprises a drug, a drug carrier and an auxiliary material. The drug carrier is mitochondria targeted phospholipid,and a hydrophilic head part of the phospholipid is connected with (3-propyl carboxyl) triphenylphosphine, arginine, lysine or dendritic polypeptide molecules consisting of arginine and / or lysine through an amido bond or an ester bond. Drug-loaded lipidosome prepared from the drug carrier carries positive charges, is easy to take in by cells, and can be targeted to mitochondria under the drive ofa transmembrane potential, so that the drug is released and gradually gathered in the mitochondria, and the drug effect can be further taken in the mitochondria.

Description

technical field [0001] The invention belongs to the field of drug delivery systems, and relates to a mitochondria-targeted external drug preparation, which is suitable for skin care and prevention and treatment of skin diseases. Background technique [0002] The skin is the largest organ of the human body. As the first physiological defense line of the human body, it is always involved in the functional activities of the body and maintains the unity of opposites between the body and the natural environment. The application of external preparations is mostly divided into two categories, one is the treatment of skin diseases, and the other is daily skin care. At present, the commonly used transdermal preparations often have two major defects, (1) the transdermal performance of the preparation is poor, and the drug stays more on the surface of the skin to affect the final drug effect; (2) the drug lacks intracellular secondary targeting , can not play a role in a specific site...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K9/127A61K47/24A61K47/42A61K47/36A61K47/10A61K45/00A61K31/122A61P17/00A61P17/16
CPCA61K9/0014A61K9/06A61K9/127A61K31/122A61K45/00A61K47/10A61K47/24A61K47/36A61K47/42A61P17/00A61P17/16
Inventor 姜雷涂家生庄融
Owner CHINA PHARM UNIV
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