Department of Gastrointestinal Surgery, First Affiliated Hospital, Chongqing Medical University, Chongqing 400016, Chongqing, China.
BMC Biotechnol. 2011 Mar 15;11:21. doi: 10.1186/1472-6750-11-21.
Cytotoxic drugs are non-selective between normal and pathological tissue, and this poses a challenge regarding the strategy for treatment of tumors. To achieve sufficient antitumor activity for colorectal carcinoma, optimization of the therapeutic regimen is of great importance. We investigated the ability of oxaliplatin long-circulating liposomes (PEG-liposomal L-oHP) to provide an improved therapeutic index of colorectal carcinoma.
We determined that PEG- liposomes conjugated with cells at 2 h, with a mean fluorescence intensity that was enhanced upon extended induction time. The PEG-liposomal L-oHP induced a significant apoptotic response as compared with free L-oHP, 23.21% ± 3.38% vs. 16.85% ± 0.98%, respectively. Fluorescence imaging with In-Vivo Imaging demonstrated that PEG- liposomes specifically targeted tumour tissue. After intravenous injections of PEG-liposomal L-oHP or free L-oHP, the tumour volume suppression ratio was 26.08% ± 12.43% and 18.19% ± 7.09%, respectively, the percentage increased life span (ILS%) was 45.36% and 76.19%, respectively, and Bcl-2, Bax mRNA and protein expression in tumour tissue was 0.27-fold vs. 0.88-fold and 1.32-fold vs. 1.61-fold compared with free L-oHP, respectively.
The PEG-liposomal L-oHP exhibited a tendency to target tumour tissue and demonstrated a significantly greater impact on apoptosis compared to free oxaliplatin.
细胞毒性药物在正常组织和病理组织之间没有选择性，这给肿瘤的治疗策略带来了挑战。为了实现对结直肠癌的充分抗肿瘤活性，优化治疗方案非常重要。我们研究了奥沙利铂长循环脂质体（PEG-脂质体 L-oHP）在提供结直肠癌改善治疗指数方面的能力。
我们发现，PEG-脂质体与细胞在 2 小时时结合，随着诱导时间的延长，平均荧光强度增强。与游离 L-oHP 相比，PEG-脂质体 L-oHP 诱导的凋亡反应明显增加，分别为 23.21%±3.38%和 16.85%±0.98%。体内成像荧光成像显示，PEG-脂质体特异性靶向肿瘤组织。静脉注射 PEG-脂质体 L-oHP 或游离 L-oHP 后，肿瘤体积抑制率分别为 26.08%±12.43%和 18.19%±7.09%，相对存活率（ILS%）分别为 45.36%和 76.19%，肿瘤组织中 Bcl-2、BaxmRNA 和蛋白表达分别为 0.27 倍比 0.88 倍和 1.32 倍比 1.61 倍比游离 L-oHP。
PEG-脂质体 L-oHP 表现出靶向肿瘤组织的趋势，与游离奥沙利铂相比，对细胞凋亡的影响明显更大。
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