Biodistribution of radiolabeled polyglutamic acid and PEG-polyglutamic acid nanocapsules

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• 作者：Raquel Abellan-Pose^a ; Maria Rodrí ; guez-É ; vora^b ; Sara Vicente^a ; Noemi Csaba^a ; Carmen É ; vora^b ; Maria Jose Alonso^a ; ^{mariaj.alonso@usc.es} ; Araceli Delgado^b ; ^{adelgado@ull.es}
• 关键词：AUC ; area under the curve ; Cl ; clearance ; CTAB ; hexadecyltrimethylammonium bromide ; DTPA ; diethylenetriamine pentacetic acid ; 14 ; 0 DTPA-PE ; 1 ; 2-dimyristoyl-sn-glycero-3-phosphoethanolamine-N-diethylenetriaminepentaacetic acid ; % ID ; percentage of the total injected dose ; % ID/g ; percentage of injected dose per gram of tissue ; LDA ; laser Doppler anemometry ; LE ; labeling efficiency ; MPS ; mononuclear phagocyte system ; MRT ; mean residence time ; NCs ; nanocapsules ; PCS ; photon correlation spectroscopy
• 刊名：European Journal of Pharmaceutics and Biopharmaceutics
• 出版年：2017
• 出版时间：March 2017
• 年：2017
• 卷：112
• 期：Complete
• 页码：155-163
• 全文大小：2160 K
• 卷排序：112

文摘

Recently we reported the development of 100 nm polyglutamic acid (PGA)-based nanocapsules, which were intended to carry anticancer drugs to the lymphatic system (Abellan-Pose et al., 2016). In this work, the objective was to further assess the potential “lympho-targeting” properties of radiolabeled 111In-PGA and 111In-PGA-PEG, following intravenous or subcutaneous administration. The results indicate that, following intravenous administration, both types of nanocapsules exhibit a modest accumulation in the lymph nodes (⩽2.3% ID/g). On the contrary, following subcutaneous administration, and irrespective of the presence of PEG on their surface, the nanocapsules were found to form a reservoir at the injection site, from which they drained slowly into the popliteal and the iliac lymph nodes. The significant accumulation of the radiolabeled nanocapsules in the lymph nodes was attained at 24 and 48 h post-injection, reaching values comprised between 70% and 187% ID/g in the popliteal lymph nodes. Altogether, the results led us to validate our hypothesis about the ability of the PGA and PGA-PEG nanocapsules to reach the lymphatic system, especially following subcutaneous administration.