Preparation method of stearic acid drug-loading micro-nanoparticle loaded with drug with controllable packing degree
A technology for loading drugs and stearic acid, which is applied in the directions of pharmaceutical formulations, drug combinations, and non-active ingredients medical preparations, can solve problems such as reducing drug efficacy, affecting normal cells, and increasing toxic and side effects of patients, achieving low cost, The effect of easy availability of raw materials and controllable drug loading
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Embodiment 1
[0036] Preparation of stearic acid micro-nano system loaded with iodoplatin
[0037] Cis-diamminediiodoplatinum (cis-DIDP), also known as cis-diamminediiodoplatinum (II), is a cisplatin analogue. It is a dark yellow powder in appearance. Its molecular formula is (NH3)2PtI2 and its molecular weight is 482.96. Iodiplatin is an intermediate in the synthesis of platinum anticancer drugs such as cisplatin and oxaliplatin. According to the results of the current research on the pharmacological mechanism of platinum anticancer drugs, its effect may be due to the break of the Pt-X (X is a halogen) bond on the platinum complex, and the interaction of Pt with the DNA of the diseased site causes it to fail and cure For diseased cells, iodoplatin is used as an anticancer drug, and its mechanism of action is similar to that of cisplatin, so theoretically it should also have better anticancer properties.
[0038] However, compared with cisplatin, oxaliplatin, etc., because of its extremely uns...
Embodiment 2
[0052] Weigh 52.2 mg of soybean lecithin, 71.3 mg of stearic acid, and 41.7 mg of iodosamine platinum into a beaker, add 25 ml of chloroform to it, and ultrasonicate it for 5 minutes to fully dissolve the oil phase. Accurately weigh 225.7 mg of PEG-4000 into 25 ml of double-distilled water, and ultrasound for 5 minutes to fully dissolve the 9 mg / ml PEG-4000 solution as the water phase. Put the oil phase and water phase in a constant temperature water bath and heat to 30°C for storage. Place the water phase in a constant temperature water bath at 60℃ and stir with a magnetic stirrer with a stirring speed of 1000r / min. Slowly inject the oil phase and continue stirring for about 8 hours to completely evaporate the organic solvent and concentrate the volume to about 15ml The micro-nano emulsion formed. Quickly add 15 ml of ice water at 5°C to the obtained emulsion while it is hot, and ultrasonicate for 30 minutes in an ice water bath to obtain a suspension of stearic acid drug-loa...
Embodiment 3
[0054] Weigh 100.5 mg of soy lecithin, 140.3 mg of stearic acid and 87.4 mg of iodoamiplatin into a beaker, add 40 ml of dichloromethane to it, and ultrasound for 5 minutes to fully dissolve the oil phase. Accurately weigh 399.4 mg of PEG-4000 into 50 ml of double-distilled water, and ultrasound for 5 minutes to fully dissolve the 8 mg / ml PEG-4000 solution as the water phase. Put the oil phase and water phase in a constant temperature water bath and heat to 30°C for storage. Place the water phase in a constant temperature water bath at 60°C and stir with a magnetic stirrer with a stirring speed of 1000r / min. Slowly inject the oil phase and continue stirring for about 7 hours to completely evaporate the organic solvent and concentrate the volume to 30ml. Of micro-nano emulsions. To the obtained emulsion, quickly add 30 ml of ice water at 5°C while it is hot, and ultrasonicate in an ice water bath for 30 minutes to obtain a suspension of stearic acid drug-loaded micro-nanopartic...
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