Introduction: Oxaliplatin (L-OHP) is a well-known third-generation platinum anticancer drug with severe systemic- and neuro-toxicity. The main objective of the current research was to develop a targeted long-circulating thermosensitive smart-release liposome (LCTL) system for better therapeutic efficacy and less toxicity.
Methods: The reverse-phase evaporation method (REV) was used to prepare L-OHP loaded LCTL (L-OHP/LCTL). The physical characteristics were evaluated including encapsulation efficiency (EE), size, zeta potential and stability. The release behavior, cytotoxicity and in vivo evaluation were also carried out.
Results: EE of LCTL was around 25% with a uniform size distribution, and LCTL achieved almost complete release at 42°C while it was only 10% at 37°C. Moreover, the LCTL showed significantly higher cytotoxicity at 42°C than that at 37°C. The in vivo results indicated LCTL could target tumors and enhance retention for more than 24 h, thereby enhancing anti-tumor efficacy on 4T1-bearing mice.
Discussion: These results indicated that LCTL not only possessed a prolonged circulation time but it also enhanced accumulation and achieved selective release at the tumor sites. Conclusively, LCTL could serve as a promising carrier for oxaliplatin delivery to treat solid tumors.

Keywords: delivery, oxaliplatin, thermosensitive, pharmacokinetic properties, tumor targeting


中文翻译：

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用于奥沙利铂靶向给药的长循环热敏脂质体

简介：奥沙利铂（L-OHP）是著名的第三代铂类抗癌药物，具有严重的全身和神经毒性。目前研究的主要目的是开发一种靶向长循环热敏智能释放脂质体（LCTL）系统，以提高治疗效果和降低毒性。
方法：采用反相蒸发法（REV）制备负载L-OHP的LCTL（L-OHP/LCTL）。评估了物理特性，包括封装效率 (EE)、尺寸、zeta 电位和稳定性。还进行了释放行为、细胞毒性和体内评价。
结果：LCTL 的 EE 约为 25%，粒径分布均匀，LCTL 在 42°C 时几乎完全释放，而在 37°C 时仅为 10%。此外，LCTL 在 42°C 时的细胞毒性明显高于 37°C。体内结果表明 LCTL 可以靶向肿瘤并增强保留时间超过 24 小时，从而增强对 4T1 小鼠的抗肿瘤功效。
讨论：这些结果表明，LCTL不仅具有延长的循环时间，而且还增强了积累并在肿瘤部位实现了选择性释放。最终，LCTL 可以作为奥沙利铂治疗实体瘤的有前途的载体。

关键词：递送，奥沙利铂，热敏性，药代动力学特性，肿瘤靶向