Mitochondria-targeted polysaccharide nano preparation and preparing method thereof
A nano-preparation, mitochondrial technology, applied in non-active ingredients medical preparations, medical preparations containing active ingredients, glycopeptide ingredients, etc., can solve problems such as drug leakage, achieve increased toxicity, reasonable preparation method design, and difficult The effect of leakage
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[0040] Example 1
[0041] Dissolve 40mg of triphenylphosphine TPP in 15ml of ultrapure water, and dissolve 19mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide EDC and 12mg of N-hydroxysuccinimide NHS in 1ml of ultrapure water. Pure water was added dropwise to the TPP solution to adjust the pH 5.5, and the solution was placed on a magnetic stirrer and stirred for 40 minutes. Dissolve 22mg of n-BOC-1,6-diaminohexane hydrochloride in 5ml of water, add dropwise to the activated TPP solution, adjust the pH to 7.5, stir the reaction for 4 hours, and freeze-dried TPP-C 6 -BOC is dissolved in 20ml methanol, 2ml trifluoroacetic acid is added, the reaction is stirred for 1 hour, then transferred to eggplant-shaped flask, rotary evaporated to dryness, a yellow oily substance appears, add saturated NaHCO 3 Extract the solution with chloroform, combine the chloroform layers, and evaporate to dryness to obtain TPP-C 6 -NH 2 .
[0042] Take 40mg hyaluronic acid HA (molecular weight 150,000Da) d...
Example Embodiment
[0044] Example 2
[0045] Dissolve 40mg of triphenylphosphine TPP in 15ml of ultrapure water, and dissolve 19mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide EDC and 12mg of N-hydroxysuccinimide NHS in 1ml of ultrapure water. Pure water was added dropwise to the TPP solution to adjust the pH 5.5, and the solution was placed on a magnetic stirrer and stirred for 40 minutes. Dissolve 22mg of n-BOC-1,6-diaminohexane hydrochloride in 5ml of water, add dropwise to the activated TPP solution, adjust the pH to 7.5, stir the reaction for 4 hours, and freeze-dried TPP-C 6 -BOC is dissolved in 20ml methanol, 2ml trifluoroacetic acid is added, the reaction is stirred for 1 hour, then transferred to eggplant-shaped flask, rotary evaporated to dryness, a yellow oily substance appears, add saturated NaHCO 3 Extract the solution with chloroform, combine the chloroform layers, and evaporate to dryness to obtain TPP-C 6 -NH 2 .
[0046] Take 40mg hyaluronic acid HA (molecular weight 150,000Da) d...
Example Embodiment
[0048] Example 3
[0049] Dissolve 40mg of triphenylphosphine TPP in 15ml of ultrapure water, and dissolve 19mg of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide EDC and 12mg of N-hydroxysuccinimide NHS in 1ml of ultrapure water. Pure water was added dropwise to the TPP solution to adjust the pH 5.5, and the solution was placed on a magnetic stirrer and stirred for 40 minutes. Dissolve 22 mg of n-BOC-1,6-diaminohexane hydrochloride in 5 ml of water, add dropwise to the activated TPP solution, adjust the pH to 7.5, stir the reaction for 4 hours, and lyophilize. TPP-C after lyophilization 6 -BOC is dissolved in 20ml methanol, 2ml trifluoroacetic acid is added, the reaction is stirred for 1 hour, then transferred to eggplant-shaped flask, rotary evaporated to dryness, a yellow oily substance appears, add saturated NaHCO 3 Extract the solution with chloroform, combine the chloroform layers, and evaporate to dryness to obtain TPP-C 6 -NH 2 .
[0050] Take 40mg hyaluronic acid HA (molecu...
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