Division of Pharmaceutics and Translational Therapeutics, College of Pharmacy, University of Iowa, Iowa, IA, USA.
Department of Orthopaedics and Rehabilitation, University of Iowa Hospital and Clinics, University of Iowa, Iowa, IA, USA.
Int J Pharm. 2018 Mar 25;539(1-2):139-146. doi: 10.1016/j.ijpharm.2018.01.028. Epub 2018 Jan 17.
Melanoma is an incurable disease for which alternative treatments to chemotherapy alone are sought. Here, using a melanoma model, we investigated the antitumor potential of combining ultrasound (US) with poly(lactic-co-glycolic acid) (PLGA) microspheres loaded with doxorubicin (DOX). The aim was to achieve synergistic tumoricidal activity through direct and indirect US-mediated damage of tumor cells combined with sustained and potentially controllable release (when combined with US) of DOX from microspheres. An in vitro release assay demonstrated an ability of US to affect the release kinetics of DOX from DOX-loaded PLGA microspheres by inducing a 12% increase in the rate of release. In vitro viability assays demonstrated that combining US with DOX-loaded PLGA microspheres resulted in synergistic tumor cell (B16-F10 melanoma cells) killing. Melanoma-bearing mice were treated intratumorally with DOX (8 µg)-loaded microspheres and subjected to US treatment at the tumor site. This treatment could significantly extend survival (mean survival (MS) = 22.1 days) compared to untreated mice (MS = 10.4 days) and most other treatments, such as blank microspheres plus US (MS = 11.5 days) and DOX (8 µg)-loaded microspheres alone (MS = 13 days). The findings that immune checkpoint blockade did not significantly extend survival of mice treated with DOX (8 µg)-loaded microspheres plus US, and that tumor-free ("cured") mice were not protected from subsequent tumor rechallenge suggests minimal involvement of the adaptive immune response in the observed antitumor activity. Nevertheless, the synergistic increase in survival of melanoma-challenged mice treated with the combination of US and DOX-loaded microspheres implicates such a treatment methodology as a promising additional tool for combatting otherwise currently incurable cancers.
黑色素瘤是一种无法治愈的疾病,因此人们在寻找单独化疗以外的替代疗法。在这里,我们使用黑色素瘤模型,研究了将超声(US)与载多柔比星(DOX)的聚乳酸-羟基乙酸共聚物(PLGA)微球相结合的抗肿瘤潜力。目的是通过直接和间接的 US 介导的肿瘤细胞损伤以及 PLGA 微球中 DOX 的持续和潜在可控释放(与 US 联合使用时)来实现协同杀瘤活性。体外释放实验表明,US 能够通过诱导 DOX 释放率提高 12%来影响载 DOX 的 PLGA 微球的释放动力学。体外细胞活力实验表明,将 US 与载 DOX 的 PLGA 微球联合使用可协同杀伤肿瘤细胞(B16-F10 黑色素瘤细胞)。荷瘤小鼠在肿瘤内接受载 DOX(8μg)的微球治疗,并在肿瘤部位进行 US 治疗。与未治疗的小鼠(MS=10.4 天)和大多数其他治疗方法(如空白微球加 US(MS=11.5 天)和单独载 DOX(8μg)的微球(MS=13 天)相比,这种治疗方法可以显著延长生存时间(平均生存时间(MS)=22.1 天)。载 DOX(8μg)的微球加 US 治疗的小鼠接受免疫检查点阻断治疗后,其生存时间没有显著延长,无肿瘤(“治愈”)的小鼠也没有免受随后的肿瘤再挑战的保护,这表明适应性免疫反应在观察到的抗肿瘤活性中参与度较小。然而,US 联合载 DOX 微球治疗的黑色素瘤挑战小鼠的生存时间协同增加表明,这种治疗方法是对抗目前无法治愈的癌症的一种有前途的附加工具。