Biodistribution and pharmacokinetics of EGFR-targeted thiolated gelatin nanoparticles following systemic administration in pancreatic tumor-bearing mice.
Biodistribution and pharmacokinetics of EGFR-targeted thiolated gelatin nanoparticles following systemic administration in pancreatic tumor-bearing mice.
复制标题
胰腺肿瘤小鼠全身给药后 EGFR 靶向硫醇化明胶纳米颗粒的生物分布和药代动力学。
DOI：
10.1021/mp400054e
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发表时间：
2013
影响因子：
4.9
通讯作者：
Amiji,Mansoor
中科院分区：
文献类型：
--
作者：
Xu,Jing;Gattacceca,Florence;Amiji,Mansoor
本研究旨在评价表皮生长因子受体（EGFR）靶向巯基化B型明胶纳米颗粒在皮下人胰腺癌（Panc-1）荷瘤雌性SCID Beige小鼠体内的定性和定量生物分布。EGFR靶向纳米颗粒在肿瘤块中显示出优先和持续的积累，特别是在早期时间点。在研究过程中，PEG修饰的和EGFR靶向的纳米颗粒观察到更高的血液浓度和更高的肿瘤蓄积（PEG修饰和EGFR靶向纳米颗粒的AUClast：血液中分别为17.38和19.56%ID/mL·h，肿瘤中分别为187和322%ID/g·h）（AUClast：血液中10.71%ID/mL·h，肿瘤中138%ID/g·h）。EGFR靶向纳米颗粒显示出几乎两倍于PEG修饰或未修饰的纳米颗粒的肿瘤靶向效率，突出了主动靶向策略的功效。总之，本研究表明，EGFR靶向和PEG修饰的纳米颗粒是皮下Panc-1肿瘤异种移植模型中特异性全身递送的合适载体。
The objective of this study was to evaluate qualitative and quantitative biodistribution of epidermal growth factor receptor (EGFR)-targeted thiolated type B gelatin nanoparticlesin vivoin subcutaneous human pancreatic adenocarcinoma (Panc-1) bearing female SCID Beige mice. EGFR-targeted nanoparticles showed preferential and sustained accumulation in the tumor mass, especially at early time points. Higher blood concentrations and higher tumor accumulations were observed with PEG-modified and EGFR-targeted nanoparticles during the study (AUClast: 17.38 and 19.56%ID/mL·h in blood, 187 and 322%ID/g·h in tumor for PEG-modified and EGFR-targeted nanoparticles, respectively), as compared to control, unmodified particles (AUClast: 10.71%ID/mL·h in blood and 138%ID/g·h in tumor). EGFR-targeted nanoparticles displayed almost twice tumor targeting efficiency than either PEG-modified or the unmodified nanoparticles, highlighting the efficacy of the active targeting strategy. In conclusion, this study shows that EGFR-targeted and PEG-modified nanoparticles were suitable vehicles for specific systemic delivery in subcutaneous Panc-1 tumor xenograft models.