Centre for Nanosciences & Molecular Medicine, Amrita Institute of Medical Sciences & Research Centre, Amrita Vishwa Vidyapeetham, Kochi, Kerala-682041, India.
Curr Drug Deliv. 2019;16(7):654-662. doi: 10.2174/1567201816666190816102949.
Prolonged chemodrug delivery to the tumor site is a prerequisite to maintaining its localised therapeutic concentrations for effective treatment of malignant solid tumors.
The current study aims to develop implantable polymeric depots through conventional electrospinning for sustained drug delivery, specifically to the peritoneum.
Non-woven electrospun mats were fabricated by simple electrospinning of Polydioxanone solution loaded with the chemodrug, Paclitaxel. The implants were subjected to the analysis of morphology, mechanical properties, degradation and drug release in phosphate buffer and patient-derived peritoneal drain fluid samples. In vivo studies were conducted by surgical knotting of these implants to the peritoneal wall of healthy mice.
Non-woven electrospun mats with a thickness of 0.65±0.07 mm, weighing ~ 20 mg were fabricated by electrospinning 15 w/v% polymer loaded with 10 w/w% drug. These implants possessing good mechanical integrity showed a drug entrapment efficiency of 87.82±2.54 %. In vitro drug release studies in phosphate buffer showed a sustained profile for ~4 weeks with a burst of 10 % of total drug content, whereas this amounted to >60% in patient samples. Mice implanted with these depots remained healthy during the study period. The biphasic drug release profile obtained in vivo showed a slow trend, with peritoneal lavage and tissues retaining good drug concentrations for a sustained period.
The results indicate that non-woven electrospun mats developed from biodegradable Polydioxanone polymer can serve as ideal candidates for easily implantable drug depots to address the challenges of peritoneal metastasis in ovarian cancer.
将化疗药物长时间递送至肿瘤部位是维持其局部治疗浓度以有效治疗恶性实体肿瘤的前提条件。
本研究旨在通过常规静电纺丝技术开发可植入的聚合物储库,以实现化疗药物紫杉醇的持续药物递送,特别是递送至腹膜部位。
通过将载药的聚二氧杂环已酮溶液简单静电纺丝,制备出非织造型无纺静电纺丝垫。对这些植入物进行形态学、机械性能、在磷酸盐缓冲液和患者来源的腹膜引流液样本中的降解和药物释放分析。通过将这些植入物用手术结系到健康小鼠的腹膜壁上,进行体内研究。
通过将 15 w/v%的聚合物负载 10 w/w%的药物进行静电纺丝,制备出厚度为 0.65±0.07mm、重量约为 20mg 的非织造型无纺静电纺丝垫。这些具有良好机械完整性的植入物显示出 87.82±2.54%的药物包封效率。在磷酸盐缓冲液中的体外药物释放研究显示,在约 4 周的时间内呈现出持续的释放模式,其中 10%的药物呈爆发释放,而在患者样本中则超过 60%。在研究期间,植入这些储库的小鼠保持健康。体内获得的双相药物释放模式显示出缓慢的趋势,腹膜灌洗和组织在较长时间内保持良好的药物浓度。
这些结果表明,由可生物降解的聚二氧杂环已酮聚合物制成的非织造型无纺静电纺丝垫可以作为理想的可植入药物储库候选物,用于解决卵巢癌腹膜转移的挑战。