Hawley A E, Illum L, Davis S S
Department of Pharmaceutical Sciences, University of Nottingham, University Park, UK.
FEBS Lett. 1997 Jan 6;400(3):319-23. doi: 10.1016/s0014-5793(96)01408-1.
Studies were performed to develop a sub-100 nm biodegradable colloidal system for the efficient delivery of drugs and diagnostic agents to the lymphatic system. Nanospheres of poly(lactide-co-glycolide) were prepared by interfacial polymer deposition. The nanospheres were coated with block co-polymers in order to modify their surface characteristics. Radiolabelling of the nanospheres for in vivo tracing was achieved by the incorporation of the lipophilic complex 111In-oxine during nanosphere preparation. In vitro stability of the radiolabelled nanospheres was determined in rat serum at 37 degrees C. The lymphatic distribution of the nanospheres was determined after subcutaneous administration to the rat. Lymphatic uptake of all coated systems was enhanced compared to the uncoated nanospheres, and a maximal uptake of 17% of the administered dose in the regional lymph nodes was achieved. These observations suggest that the nanospheres are suitable for diagnostic and therapeutic applications in clinical and experimental medicine.
开展了多项研究,以开发一种尺寸小于100纳米的可生物降解胶体系统,用于将药物和诊断剂高效递送至淋巴系统。通过界面聚合物沉积制备聚(丙交酯-共-乙交酯)纳米球。为了改变其表面特性,纳米球用嵌段共聚物进行了包衣。通过在纳米球制备过程中加入亲脂性络合物111In-奥克辛实现纳米球的放射性标记,用于体内追踪。在37℃的大鼠血清中测定放射性标记纳米球的体外稳定性。在大鼠皮下给药后测定纳米球的淋巴分布。与未包衣的纳米球相比,所有包衣系统的淋巴摄取均增强,区域淋巴结中摄取量最高可达给药剂量的17%。这些观察结果表明,纳米球适用于临床和实验医学中的诊断和治疗应用。