Compound preparation for treating tumors and preparation method
A compound preparation and liposome technology, which can be used in anti-tumor drugs, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve adverse reactions, the effective delivery rate is less than 1%, and lipid It can reduce the toxic and side effects, improve the effectiveness of the drug, and the preparation process is simple.
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example Embodiment 1
[0075]
[0076]
[0077] Preparation Process:
[0078] Weigh 200mg of hyaluronic acid (35kDa) and dissolve in 40mL of purified water to obtain HA solution; weigh 436mg of ADH and 48mg of EDCI, and add the above HA solution under stirring conditions. The pH of the solution was adjusted to 4.75 with hydrochloric acid, and the stirring reaction was continued for 10 h. The pH of the solution was detected again, and if any change occurred, the pH was adjusted to 4.75, and the stirring reaction was continued for 2 h. The pH of the above solution was adjusted to 7.0 with sodium hydroxide solution to complete the preparation process of HA-ADH. The above HA-ADH reaction product was collected, placed in a dialysis bag with a molecular weight cut off of 3500, and dialyzed in purified water for 48 hours, and the dialysis medium was replaced every 12 hours. The dialyzed product was collected and lyophilized, and the resulting product was HA-ADH. Weigh 110 mg of HA-ADH and dissolve...
Embodiment 2
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[0083] Preparation Process:
[0084] Dissolve 30mg of soybean lecithin in 12mL of chloroform, and rotate it at 45°C for 1 hour to form a phospholipid film. Dissolve 20 mg of cytarabine in 4 mL of phosphate buffer (pH 6.8), add it to the above phospholipid film, and rotate and mix at 45° C. for 40 min. The above mixture was sonicated for 10 minutes under the condition of 200W power to complete the preparation of cytarabine liposomes.
[0085] In the cytarabine liposomes prepared in Example 2, the encapsulation efficiency of cytarabine was 23.75%, and the drug loading was 13.67%.
Embodiment 3
[0087] HA-ADH-daunorubicin 90mg
[0088] Cytarabine Liposome 4mL
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[0090] Preparation Process:
[0091] Weigh 90mg HA-ADH-daunorubicin and dissolve in 4mL purified water.
[0092] Take 4mL cytarabine liposome, add the above 4mL HA-ADH-daunorubicin dropwise, vortex and mix for 1min, and complete the HA-ADH-daunorubicin / cytarabine liposome hybrid nano Granules preparation.
[0093] In the HA-ADH-daunorubicin / cytarabine liposome hybrid nanoparticles prepared in Example 3, the total drug encapsulation efficiency was 26.46%, and the total drug loading was 5.09%.
[0094] The cytarabine liposomes prepared in Example 2 and the hybrid nanoparticles prepared in Example 3 were detected by a dynamic light scattering nanometer. The average particle size of the cytarabine liposome prepared in Example 2 and the hybrid nanoparticle prepared in Example 3 is about 100 nm, and conforms to a normal distribution, and the distribution is uniform. The cytarabine liposomes p...
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