Adjei Isaac M, Peetla Chiranjeevi, Labhasetwar Vinod
Department of Molecular Medicine, Cleveland Clinic Lerner College of Medicine of Case Western Reserve University, Cleveland, OH 44106, USA.
Nanomedicine (Lond). 2014 Feb;9(2):267-78. doi: 10.2217/nnm.13.70. Epub 2013 Jun 26.
A large fraction of the administered dose of nanoparticles (NPs) localizes into nontarget tissue, which could be due to the heterogeneous population of NPs.
MATERIALS & METHODS: To investigate the impact of the above issue, we simultaneously tracked the biodistribution using optical imaging of two different sized poly(d,l-lactide co-glycolide) NPs, which also varied in their surface charge and texture, in a prostate tumor xenograft mouse model.
Although formulated using the same polymer and emulsifier concentration, small NPs were neutral (S-neutral-NPs), whereas large NPs were anionic (L-anionic-NPs). Simultaneous injection of these NPs, representing heterogeneity, shows significantly different biodistribution. S-neutral-NPs demonstrated longer circulation time than L-anionic-NPs (t1/2 = 96 vs 13 min); accounted for 75% of total NPs accumulated in the tumor; and showed 13-fold greater tumor to liver signal intensity ratio than L-anionic-NPs.
The data underscore the importance of formulating nanocarriers of specific properties to enhance their targeting efficacy.
纳米颗粒（NPs）给药剂量的很大一部分会定位于非靶组织，这可能归因于NPs的异质性群体。
为研究上述问题的影响，我们在前列腺肿瘤异种移植小鼠模型中，使用光学成像同时追踪了两种不同尺寸的聚（d，l-丙交酯乙交酯）NPs的生物分布，这两种NPs在表面电荷和质地方面也存在差异。
尽管使用相同的聚合物和乳化剂浓度进行配制，但小尺寸NPs呈中性（S-中性-NPs），而大尺寸NPs呈阴离子性（L-阴离子-NPs）。同时注射这些代表异质性的NPs，显示出明显不同的生物分布。S-中性-NPs的循环时间比L-阴离子-NPs长（t1/2 = 96分钟对13分钟）；占肿瘤中积累的总NPs的75%；并且肿瘤与肝脏的信号强度比是L-阴离子-NPs的13倍。
数据强调了配制具有特定性质的纳米载体以提高其靶向效果的重要性。
