Department of Chemical Engineering, Curtin University, Sarawak 98009, Malaysia; Curtin Sarawak Research Institute, Curtin University, Sarawak 98009, Malaysia.
Department of Chemical Engineering, Curtin University, Sarawak 98009, Malaysia; Curtin Sarawak Research Institute, Curtin University, Sarawak 98009, Malaysia.
Biomed Pharmacother. 2018 May;101:996-1002. doi: 10.1016/j.biopha.2018.03.052. Epub 2018 Mar 22.
Targeted drug delivery is a promising strategy to promote effective delivery of conventional and emerging pharmaceuticals. The emergence of aptamers as superior targeting ligands to direct active drug molecules specifically to desired malignant cells has created new opportunities to enhance disease therapies. The application of biodegradable polymers as delivery carriers to develop aptamer-navigated drug delivery system is a promising approach to effectively deliver desired drug dosages to target cells. This study reports the development of a layer-by-layer aptamer-mediated drug delivery system (DPAP) via a w/o/w double emulsion technique homogenized by ultrasonication or magnetic stirring. Experimental results showed no significant differences in the biophysical characteristics of DPAP nanoparticles generated using the two homogenization techniques. The DPAP formulation demonstrated a strong targeting performance and selectivity towards its target receptor molecules in the presence of non-targets. The DPAP formulation demonstrated a controlled and sustained drug release profile under the conditions of pH 7 and temperature 37 °C. Also, the drug release rate of DPAP formulation was successfully accelerated under an endosomal acidic condition of ∼pH 5.5, indicating the potential to enhance drug delivery within the endosomal micro-environment. The findings from this work are useful to understanding polymer-aptamer-drug relationship and their impact on developing effective targeted delivery systems.
靶向药物递送是一种很有前途的策略，可以促进传统和新兴药物的有效递送。适体作为优于靶向配体的出现，可将活性药物分子特异性地导向所需的恶性细胞，为增强疾病治疗创造了新的机会。将可生物降解的聚合物作为递送载体来开发适体导航药物递送系统是一种很有前途的方法，可以有效地将所需的药物剂量递送到靶细胞。本研究通过 w/o/w 双乳液技术并通过超声处理或磁搅拌来报告层状适体介导的药物递送系统（DPAP）的开发。实验结果表明，两种均化技术产生的 DPAP 纳米颗粒的物理特性没有显著差异。在存在非靶标物的情况下，DPAP 制剂表现出针对其靶受体分子的强靶向性能和选择性。DPAP 制剂在 pH 7 和 37°C 的条件下表现出控制和持续的药物释放曲线。此外，DPAP 制剂的药物释放率在约 pH 5.5 的内体酸性条件下成功加速，表明有可能增强内体微环境中的药物递送。这项工作的结果有助于理解聚合物-适体-药物的关系及其对开发有效靶向递送系统的影响。
