Sustained release anticancer agent carrying angiogenesis inhibitor and cytotoxic drug
A new blood vessel, inhibitor technology, applied in the field of sustained release agent, sustained release injection and sustained release implant, can solve the problems of systemic toxicity and drug resistance limit application
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Embodiment 1
[0112] Put 80mg of polyphenylpropane (p-CPP: 20:80 of sebacic acid (SA)) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 10mg Nedaplatin and 10 mg marimastat were re-shaken and spray-dried to prepare microspheres for injection containing 10% nedaplatin and 10% marimastat. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 220cp-460cp (at 20°C-30°C). The drug release time of the sustained-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.
Embodiment 2
[0114] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the contained anticancer active ingredients and their weight percentages are:
[0115] (a) 20% marimastat, SU5416, SU6668, fumagillin or TNP-470;
[0116] (b) 20% heptaplatin, nedaplatin, melphalan, 4H-cyclophosphamide peroxide, 2'-hydroxypaclitaxel, 10-deacetylpaclitaxel, 7-epi-paclitaxel, vinorelbine, tamoxicil Fen, methotrexate, doxorubicin, epirubicin, actinomycin D, tamustine, amustine, semustine, or ramustine; or
[0117] (c) 2-40% marimastat, SU5416, SU6668, fumagillin or TNP-470 and 2-40% heptaplatin, nedaplatin, melphalan, 4H-peroxycyclophosphamide, 2'-hydroxy-paclitaxel, 10-deacetyl-paclitaxel, 7-epi-paclitaxel, vinorelbine, tamoxifen, methotrexate, doxorubicin, epirubicin, actinomycin D, tamustine, a A combination of mustin, semustine, or ramustine.
Embodiment 3
[0119] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 65,000 into a container, add 100 ml of dichloromethane, dissolve and mix well, add 15 mg of fumagillin and 15 mg of tamustine, and re-shake Dry in vacuo to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make micropowder containing 15% fumagillin and 15% tamustine, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding Suspension-type sustained-release injection with a viscosity of 300cp-400cp (at 20°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.
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