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Lactosaminated-N-succinyl chitosan nanoparticles for hepatocyte-targeted delivery of acyclovir

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Abstract

The present study discusses lactose-acyclovir-N-succinyl chitosan nanoparticles (Lac-N-Suc-CSNP) using lactose as an asialoglycoprotein receptor (ASGPR) ligand for hepatic parenchymatic cells targeting. For this purpose, N-succinyl chitosan nanoparticles (N-Suc-CSNP) were prepared previously by ionotropic gelation method and lactose was conjugated to the free amino terminal group of chitosan. Lactose conjugation with N-Suc-CSNP was confirmed by FT-IR and zeta potential measurements. The Lac-N-Suc-CSNP obtained were characterized for their morphology, particle size, polydispersity index, and zeta potential. The Lac-N-Suc-CSNP showed spherical in shape with 220.3 ± 5.0 nm size range, +4.1 ± 0.2 mV zeta potential, 62.5 ± 1.2 % acyclovir entrapment efficiency and showed 27.3 ± 0.9 % cumulative acyclovir release up to 72 h. The acyclovir concentration from Lac-N-Suc-CSNP was found to be 19.9 ± 1.62 μg/g after 24 h administration revealed remarkably targeting potential to the hepatocytes and keep at a high level during the experiment. These results suggest that Lac-N-Suc-CSNP are potentially vector for hepatocytes targeting.

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Abbreviations

ASGPR:

Asialoglycoprotein receptor

N-Suc-CSNP:

N-succinyl chitosan nanoparticles

Lac-N-Suc-CSNP:

Lactosaminated-N-succinyl chitosan nanoparticles

PDI:

Poly dispersity index

FITC:

Fluorescein isothiocyanate

TEM:

Transmission electron microscopy

FT-IR:

Fourier-transform infrared spectroscopy

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Acknowledgments

The author Nivrati Jain thanks to All India Council for Technical Education, New Delhi, India for providing financial assistance. Nivrati Jain offer his sincere thanks to AIIMS, New Delhi for providing the facilities for conducting TEM study of developed formulation. NIPER Chandigarh for particle size and zeta potential analysis, Department of Chemistry Dr. H. S. Gour University, Sagar (MP) for providing IR facilities. The authors thank Ipca Pvt. Limited, Mumbai for supplying gift samples of Acyclovir to carry out the work. The authors would also like to thank Institutional Animal Ethical Committee, ADINA Institute of Pharmaceutical Sciences, Sagar for permission of in vivo studies.

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Authors and Affiliations

  1. ADINA Institute of Pharmaceutical Sciences, Sagar, 470002, Madhya Pradesh, India

    Nivrati Jain, Vaibhav Rajoriya, Prateek Kumar Jain & Ashish Kumar Jain

  2. Pharmaceutics Division, ADINA Institute of Pharmaceutical Sciences, Opposite J.L. Nehru Agriculture Research Centre, Bhopal Road, Sagar, 470002, Madhya Pradesh, India

    Ashish Kumar Jain

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  1. Nivrati Jain
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  2. Vaibhav Rajoriya
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  3. Prateek Kumar Jain
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  4. Ashish Kumar Jain
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Correspondence to Ashish Kumar Jain.

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Jain, N., Rajoriya, V., Jain, P.K. et al. Lactosaminated-N-succinyl chitosan nanoparticles for hepatocyte-targeted delivery of acyclovir. J Nanopart Res 16, 2136 (2014). https://doi.org/10.1007/s11051-013-2136-x

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