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

Joshy, K.S., Susan, M. Alex, Snigdha, S., Nandakumar, Kalarikkal, Laly, A. Pothen, Sabu, Thomas
International journal of biological macromolecules 2017
alginates, antiretroviral agents, bioavailability, crosslinking, dialysis, drugs, emulsions, encapsulation, evaporation, glutamic acid, half life, hydrophobicity, nanoparticles, solvents, transmission electron microscopy
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.