Encapsulation of zidovudine in PF-68 coated alginate conjugate nanoparticles for anti-HIV drug delivery

[Display omitted] •Amide derivative of alginate was developed with Glutamic acid.•This biocompatible alginate derivative was used as a carrier of antiviral drug zidovudine.•The nanoparticles were stable and biocompatible with spherical morphology.•A slow release of zidovudine was exhibited in phosph...

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Veröffentlicht in:International journal of biological macromolecules 2018-02, Vol.107 (Pt A), p.929-937
Hauptverfasser: Joshy, K.S., Susan, M. Alex, Snigdha, S., Nandakumar, Kalarikkal, Laly, A. Pothen, Sabu, Thomas
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Sprache:eng
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Zusammenfassung:[Display omitted] •Amide derivative of alginate was developed with Glutamic acid.•This biocompatible alginate derivative was used as a carrier of antiviral drug zidovudine.•The nanoparticles were stable and biocompatible with spherical morphology.•A slow release of zidovudine was exhibited in phosphate buffered saline of pH7.4.•The nanoparticles were non-toxic and efficient internalization were observed in glioma cells. Retroviral drug delivery faces many challenges due to its low bioavailability, short half life and hydrophobicity. In this study, the anti viral drug zidovudine (AZT) was encapsulated inside the amide functionalised alginate nanoparticles (AZT-GAAD NPs) using emulsion solvent evaporation method. The amide derivative of alginate was prepared by coupling reaction with d,l glutamic acid using carbodiimide activation chemistry. The stabilizer, PF-68 was integrated during the preparation of nanoparticles. The alginate nanoparticles were prepared via chemical cross linking. The novelty of this work imparts the absence of chemical cross-linking for the preparation of nanoparticles.The resulting nanoparticles had spherical shape with an average size of 432±11.9nm as confirmed by TEM images. The nanoparticles had a loading efficacy of 29.5±3.2% obtained by dialysis method. The release of AZT in PBS(pH-7.4) was studied and a slow and sustained release of AZT was observed. The nanoparticles were found to be biocompatible and in vitro cellular internalization studies indicated significantly higher internalization efficiency. All these results suggested that (AZT-GAAD NPs) can function as a promising delivery vectors for efficient antiviral drug delivery.
ISSN:0141-8130
1879-0003
DOI:10.1016/j.ijbiomac.2017.09.078