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Highly loaded nanoparticulate carrier using an hydrophobic antisense oligonucleotide complex

Stein, Cy A.
Published in European Journal of Pharmaceutical Sciences. 1999, vol. 9, no. 2, p. 163-170
Abstract Antisense oligonucleotides, and particularly those with phosphorothioate backbones, have emerged as potential gene specific therapeutic agents and are currently undergoing evaluation in clinical trials for a variety of diseases. In the area of HIV-1 therapeutics, targeting of oligonucleotides to infected cells, such as macrophages, would be highly desirable. The present study was designed to prepare and characterize oligonucleotide-loaded nanoparticles for this purpose. Due to their hydrophilic characteristics, oligonucleotides are difficult to entrap in polymeric particles. Here, the oligonucleotides were first complexed with cetyltrimethylammonium bromide. The oligonucleotide-loaded nanoparticles were prepared by the emulsification-diffusion method and subsequently purified. In comparison with previous studies, a high oligonucleotide-loading was achieved; 2.5, 5 and 10% oligonucleotide loading were assessed. If the initial oligonucleotide content was 4%, this method produced a final oligonucleotide loading of 1.9% with an entrapment efficiency of 47%. The integrity of the oligonucleotide and of the polymer, in the final freeze-dried product, was retained.
Keywords NanoparticleAntisense oligonucleotidePoly-(DL-lactic acid)Drug deliveryBiodegradable polymerHIV-1
PMID: 10620729
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Research group Technologie pharmaceutique
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BERTON, Myriam et al. Highly loaded nanoparticulate carrier using an hydrophobic antisense oligonucleotide complex. In: European Journal of Pharmaceutical Sciences, 1999, vol. 9, n° 2, p. 163-170. doi: 10.1016/s0928-0987(99)00049-4 https://archive-ouverte.unige.ch/unige:84283

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Deposited on : 2016-06-07

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