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Galactose Decorated Acid-Labile Nanoparticles Encapsulating Quantum Dots for Enhanced Cellular Uptake and Subcellular Localization

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ABSTRACT

Purpose

Biodegradable polymers containing acid-labile segments and galactose grafts were formulated into nanoparticles in current study, and enhanced cellular uptake and subcellular distribution were clarified.

Methods

Quantum dots (QDs) was utilized as an imaging agent and a model of bioactive substances, and entrapped into nanoparticles of around 200 nm through a nanoprecipitation process.

Results

The acid-labile characteristics of QDs-loaded nanoparticles were approved by the hemolysis capability, the degradation behaviors of matrix polymers, and the fluorescence decay of entrapped QDs after incubation into buffer solutions of different pH values. The galactose grafts increased the acid-lability, due to the hydrophilic moieties on the acid-labile segments, and enhanced uptake efficiency of over 50 % was found after 4 h incubation with HepG2 cells, due to the galactose-receptor mediated endocytosis. The acid-lability led to an efficient endosomal escape of QDs-loaded nanoparticles into cytoplasm.

Conclusions

The integration of acid-lability, targeting effect, and full biodegradable backbone into nanoparticle matrices constitutes a promising platform for intracellular delivery of bioactive substances for disease diagnosis, imaging and treatment.

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ACKNOWLEDGMENTS & DISCLOSURES

This work was supported by National Natural Science Foundation of China (30570501, 20774075, and 51073130), and Fundamental Research Funds for the Central Universities (SWJTU11CX126 and SWJTU11ZT10).

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Authors and Affiliations

  1. Key Laboratory of Advanced Technologies of Materials Ministry of Education of China, School of Materials Science & Engineering, Southwest Jiaotong University, Chengdu, 610031, People’s Republic of China

    Xiaojun Cai, Xiaohong Li, Yaowen Liu, Guannan Wu, Yuancong Zhao & Fang Chen

  2. National Engineering Research Center for Biomaterials, Sichuan University, Chengdu, 610064, People’s Republic of China

    Zhongwei Gu

Authors
  1. Xiaojun Cai
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  2. Xiaohong Li
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  3. Yaowen Liu
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  4. Guannan Wu
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  5. Yuancong Zhao
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  6. Fang Chen
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  7. Zhongwei Gu
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Correspondence to Xiaohong Li or Zhongwei Gu.

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Cai, X., Li, X., Liu, Y. et al. Galactose Decorated Acid-Labile Nanoparticles Encapsulating Quantum Dots for Enhanced Cellular Uptake and Subcellular Localization. Pharm Res 29, 2167–2179 (2012). https://doi.org/10.1007/s11095-012-0745-1

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  • DOI: https://doi.org/10.1007/s11095-012-0745-1

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