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临床使用具靶向作用的药物载体微球制剂需考虑其免疫原性,即使载体物质本身无免疫原性,但形成微球时的聚合或凝集作用有可能使其带免疫原性,因任何微粒均具佐剂性质。将丙烯酸淀粉溶液用过二硫酸铵及四甲基乙二胺聚合成微球。另选二硝基酚(DNP)作药物模型使与赖氨酸复合成赖-DNP,与蛋氨酸、丙氨酸和赖氨酸复合成蛋-丙-赖-DNP,再将此作为配体结合到上述微球上。将两种含药微球置于用大鼠肝制得的溶酶体液中,37°培养24 h,测得蛋-丙-赖-DNP 微球定量释出赖-DNP,而赖-DNP微球则无,这说明酶催化释放赖-DNP 需有肽臂存在,不
Clinically Use Targeted Drug Carrier Microspheres Formulations Considering their immunogenicity, aggregation or agglutination in the formation of microspheres may render them immunogenic, even if the carrier material itself is not immunogenic, as any particle Are adjuvant properties. Acrylic starch solution with ammonium persulfate and tetramethylethylenediamine polymerization into microspheres. In addition, dinitrophenol (DNP) was used as a drug model to complex with lysine to form -DNP, to methionine, alanine and lysine To the above microspheres. The two drug-containing microspheres were placed in lysosomal fluid prepared from rat liver and cultured at 37 ° C for 24 h. The release of L-DNP was determined by E-L-DNP microspheres and the release of L-DNP No ball, indicating that enzyme-catalyzed release of -DNP requires the presence of peptide arms, no