脂质体囊泡(liposomes)是临床转化最为成功的纳米载体,大多数临床用纳米药物如脂质体阿霉素(Doxil)、长春新碱脂质体制剂(Marqibo)、注射用阿糖胞苷脂质体(Depocyt)等都是基于脂质体囊泡。但是,脂质体囊泡因存在稳定性不高、靶向性修饰不易等问题,靶向纳米制剂的研制面临巨大挑战。聚合物囊泡在结构和形态上与脂质体囊泡相似,但相比脂质体囊泡,其具有更高的稳定性,且其物理性能如膜厚度、渗透性、流动性及表面功能性等都可更好调控。聚合物囊泡不但可装载疏水药物(如多西他赛、紫杉醇等),其亲水内腔可特异性地装载大量的亲水药物(如阿霉素盐酸盐、蛋白药物、核酸药物等)。我们设计了一系列基于聚肽和聚碳酸酯的多功能生物可降解聚合物囊泡体系,表面修饰上靶向分子如抗体和多肽,实现了疏水药物(如美登素和长春新碱)、小分子亲水抗癌药物(如甲氨蝶呤二钠盐和表阿霉素盐酸盐)、蛋白药物和核酸药物的高效装载,显著提高不同肿瘤(多发性骨髓瘤、白血病、卵巢癌、肺癌、黑色素瘤等)的靶向治疗效果。装载甲氨蝶呤二钠盐的囊泡可靶向到巨噬细胞,有效治疗类风湿性关节炎等免疫性疾病。
代表性论文
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