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Novel PLGA microspheres for sustained delivery of antisense oligonucleotide

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Abstract

Novel poly(lactide-co-glycolide acid)(PLGA) microspheres were developed for sustained delivery of antisense oligonucleotide(ASO). First, a new cationic agent, polyethylenimine(PEI) conjugated to linoleic acid(LA)(PEI-LA) was synthesized by reacting PEI(M w=800) with linoleoyl chloride. Then, PEI-LA was combined with LOR-2501 to form electrostatic complexes at moderate nitrogen-to-phosphate(N/P) molar ratios which were then encapsulated into poly(lactide-co-glycolide) microspheres by a multiple emulsion-solvent evaporation technique. With an increase in ASO/PEI-LA concentration from 5% to 10%, encapsulation efficiency of ASO in the microspheres reduced from 72.14% to 57.62%, and the particle size of microspheres increased from 28.58 μm to 34.76 μm. In vitro studies show that the release profile of ASO from microspheres prepared at 7.5% ASO-PEI-LA lasted for 14 d. The novel microspheres have a potential use as a sustained release vehicle for ASO.

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Authors and Affiliations

  1. College of Life Science, Jilin University, Changchun, 130012, P. R. China

    Jing Xie, Chao-jun Jiang, Robert Jian-guang Lee, Yu-lin Zhou & Le-sheng Teng

  2. College of Pharmacy, Ohio State University, Columbus, 43210, USA

    Jing Xie, Robert Jian-guang Lee & Le-sheng Teng

  3. The Second Hospital of Jilin University, Changchun, 130041, P. R. China

    Xin Li

Authors
  1. Jing Xie
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  2. Xin Li
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  3. Chao-jun Jiang
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  4. Robert Jian-guang Lee
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  5. Yu-lin Zhou
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  6. Le-sheng Teng
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Correspondence to Le-sheng Teng.

Additional information

Supported by the National Natural Science Foundation of China(Nos.30870251, 31070309).

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Xie, J., Li, X., Jiang, Cj. et al. Novel PLGA microspheres for sustained delivery of antisense oligonucleotide. Chem. Res. Chin. Univ. 29, 1003–1005 (2013). https://doi.org/10.1007/s40242-013-3127-2

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  • DOI: https://doi.org/10.1007/s40242-013-3127-2

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