131I-Traced PLGA-Lipid Nanoparticles as Drug Delivery Carriers for the Targeted Chemotherapeutic Treatment of MelanomaReportar como inadecuado

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Nanoscale Research Letters

, 12:365

First Online: 19 May 2017Received: 13 April 2017Accepted: 12 May 2017DOI: 10.1186-s11671-017-2140-7

Cite this article as: Wang, H. & Sheng, W. Nanoscale Res Lett 2017 12: 365. doi:10.1186-s11671-017-2140-7


Herein, folic acid FA conjugated Polyd,l-lactide-co-glycolide PLGA-lipid composites FA-PL were developed as nanocarriers for the targeted delivery of insoluble anti-cancer drug paclitaxel PTX, resulting FA-PLP nanoparticles. Furthermore, I, as a radioactive tracer, was used to label FA-PLP nanoparticles FA-PLP-I to evaluate their cell uptake activity, in vivo blood circulation, and biodistribution. The FA-PLP-I nanoparticles had a spherical morphology with great stability, a narrow size distribution 165.6 and 181.2 nm, and −22.1 mV in average zeta potential. Confocal laser scanning microscopy indicated that the targeting molecule FA promotes PLP-I uptake by melanoma B16F10 cells, which was further confirmed by the cell incorporation rate via I activity detection as measured by a gamma counter. FA-PLP-I without PTX FA-PL-I shows minor cytotoxicity, good biocompatibility, while FA-PLP-I was demonstrated to have efficient cell viability suppression compared to free PTX and PLP-I. Following intravenous injection, the blood circulation half-life of free PTX t1-2 = 5.4 ± 0.23 h was prolonged to 18.5 ± 0.5 h by FA-PLP-I. Through FA targeting, the tumor uptake of FA-PLP-I was approximately 4.41- and 12.8-fold higher compared to that of PLP-I and free PTX-I, respectively. Moreover, following 40 days of treatment, FA-PLP-I showed an improved tumor inhibition effect compared to free PTX and PLP-I, with no relapse and no remarkable systemic in vivo toxicity. The results demonstrate that the I-labeled PLGA-lipid nanoparticle can be simultaneously applied for targeted drug delivery and reliable tracking of drugs in vivo.

KeywordsNanocarrier PLGA-lipid I Biodistribution Drug delivery Melanoma Electronic supplementary materialThe online version of this article doi:10.1186-s11671-017-2140-7 contains supplementary material, which is available to authorized users.

Autor: Haiyan Wang - Weizhong Sheng

Fuente: https://link.springer.com/

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