The delivery of aptamer modified therapeutic moieties to specific tissue sites has become one of the major therapeutic choices to reduce the toxicity of inhibitory drugs. Bearing this in mind, the current study was designed using sorafenib (SFB) encapsulated microparticles (MP) prepared with biodegradable poly (D, L-lactic-co-glycolic acid) (PLGA) copolymer. The surfaces of these microparticles were modified with RNA aptamer having a binding affinity towards ErbB3 receptors. SFB-loaded MP (MPS) were prepared by o/w solvent evaporation method and the surface was coupled with the amino group of aptamer by EDC/NHS chemistry. Physiochemical investigations were done by dynamic light scattering, scanning electron microscopy and FTIR. In vitro apoptosis assay, cell viability assay and metastatic progression showed a significant decrease (p < 0.001) in vitro cell viability for MPS and MPS-Apt as compared to MP. The synergistic combination of SFB and aptamer also decreased the metastatic progression of cells for an extended period. Microparticles were also evaluated for in vivo toxicity in female BALB/c mice. It was evident that the presence of aptamer decreased the generalized toxicity of MPS-Apt, as measured by mean body weight loss and blood profiles, keeping all the blood formed elements level within acceptable limits. The histopathological investigations showed some necrotic and pyknotic bodies. In a similar fashion, liver function test and renal function tests showed pronounced effects of formulations on vital organs.

适体修饰的治疗部分向特定组织部位的递送已成为减少抑制药物毒性的主要治疗选择之一。牢记这一点，当前的研究是使用索拉非尼（SFB）封装的微粒（MP）设计的，该微粒由可生物降解的聚（D，L-乳酸-乙醇酸共聚物）（PLGA）共聚物制备。用对ErbB3受体具有结合亲和力的RNA适体修饰这些微粒的表面。通过o / w溶剂蒸发法制备SFB负载的MP（MPS），并通过EDC / NHS化学方法将表面与适体的氨基偶联。通过动态光散射，扫描电子显微镜和FTIR进行了理化研究。体外与MP相比，MPS和MPS-Apt的细胞凋亡测定，细胞活力测定和转移进程显示体外细胞活力显着降低（p  <0.001）。SFB和适体的协同组合还降低了细胞延长的转移进程。还对微粒进行了体内评估对雌性BALB / c小鼠的毒性。明显的是，适体的存在降低了MPS-Apt的普遍毒性，这是通过平均体重减轻和血液分布测定的，将所有血液形成元素的水平保持在可接受的范围内。组织病理学检查显示有一些坏死和侏儒症尸体。肝功能测试和肾功能测试以类似的方式显示了制剂对重要器官的显着影响。