iMed.UL - Research Institute for Medicines and Pharmaceutical Sciences, School of Pharmacy, Lisbon, Portugal.
Nanomedicine. 2012 Oct;8(7):1208-15. doi: 10.1016/j.nano.2011.12.007. Epub 2011 Dec 27.
Lung cancer remains a leading cause of death due to the low efficacy of chemotherapy, mainly related to the administration route used. Therefore, alternative administration routes are needed. Paclitaxel (PTX) is an insoluble anticancer drug active against solid tumors, such as those found in lung cancer, that has stimulated an intense research effort over recent years. Solid lipid nanoparticles (SLNs) are potential carriers for poorly soluble drugs, being biodegradable systems that served as alternatives to the usual colloidal carriers. That system was used to deliver PTX to the lungs and seem to fulfill the requirements for an optimum particulate carrier. Furthermore, PTX-loaded SLN pulmonary administration provided a target administration, which is expected to avoid high concentration of the drug at nontarget tissues, reducing toxicity, and increasing the drug's therapeutic index. The rationale of this study was to deliver a colloidal system to the lung lymphatics through a pulmonary route for cancer therapy.
Paclitaxel-loaded solid lipid nanoparticles were used to target tumors in a murine lung cancer model enabling high PTX concentration in the target with reduced systemic toxicity and increased therapeutic index.
由于化疗效果不佳,肺癌仍是主要死亡原因,主要与所用的给药途径有关。因此,需要替代给药途径。紫杉醇(PTX)是一种对实体瘤(如肺癌)有效的不溶性抗癌药物,近年来已激发了大量的研究工作。固体脂质纳米粒(SLN)是对疏水性药物有潜在作用的载体,是可生物降解的系统,可作为常规胶体载体的替代品。该系统被用于将 PTX 递送至肺部,并似乎符合最佳颗粒载体的要求。此外,负载 PTX 的 SLN 肺部给药提供了靶向给药,有望避免药物在非靶向组织中的高浓度,降低毒性,并提高药物的治疗指数。本研究的原理是通过肺部途径将胶体系统递送至肺淋巴管,用于癌症治疗。
紫杉醇负载的固体脂质纳米粒被用于靶向小鼠肺癌模型中的肿瘤,使目标组织中 PTX 浓度升高,全身毒性降低,治疗指数增加。