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Intracellular Delivery of Nanoparticles of an Antiasthmatic Drug

AAPS PharmSciTech volume 9, pages 217–223 (2008)Cite this article

Abstract

The aim of the investigation was to prepare and characterize wheat germ agglutinin(WGA)-conjugated poly(d,l-lactic-co-glycolic) acid nanoparticles encapsulating mometasone furoate (MF) as a model drug and assess changes in its fate in terms of cellular interactions. MF loaded nanoparticles were prepared using emulsion–solvent evaporation technique. WGA-conjugation was done by carbodiimide coupling method. The nanoparticles were characterized for size, zeta potential, entrapment efficiency and in-vitro drug release. The intracellular uptake of nanoparticles, drug cellular levels, and anti-proliferative activity studies of wheat germ agglutinin-conjugated and unconjugated nanoparticles were assessed on alveolar epithelial (A549) cells to establish cellular interactions. Prepared nanoparticles were spherical with 10–15 μg/mg of WGA conjugated on nanoparticles. The size of nanoparticles increased after conjugation and drug entrapment and zeta potential reduced from 78 ± 5.5% to 60 ± 2.5% and −15.3 ± 1.9 to −2.59 ± 2.1 mV respectively after conjugation. From the cellular drug concentration–time plot, AUC was found to be 0.4745, 0.6791 and 1.24 for MF, MF-nanoparticles and wheat germ agglutinin-MF-nanoparticles respectively. The in-vitro antiproliferative activity was improved and prolonged significantly after wheat germ agglutinin-conjugation. The results conclusively demonstrate improved availability and efficacy of antiasthmatic drug in alveolar epithelial cell lines. Hence, a drug once formulated as mucoadhesive nanoparticles and incorporated in dry powder inhaler formulation may be used for targeting any segment of lungs for more improved therapeutic response in other lung disorders as well.

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Acknowledgments

The authors are thankful to the Department of Science and Technology, Government of India, for providing financial support under the Women Scientist Scheme (WOS-A).We also thank Technology Information and Forecasting Council’s (TIFAC) Centre of Relevance and Excellence in New Drug Delivery System.

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Affiliations

  1. Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan, The Maharaja Sayajirao University of Baroda, Vadodara, 390001, Gujarat, India

    Naazneen Surti, Sachin Naik & Ambikanandan Misra

  2. Department of Microbiology and Biotechnology Centre, Faculty of Science, The Maharaja Sayajirao University of Baroda, Sayajigunj, Vadodara, 390002, India

    Tamishraha Bagchi

  3. Institute of Nuclear Medicine and Allied Sciences, New Delhi, India

    B. S. Dwarkanath

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  1. Naazneen Surti
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  2. Sachin Naik
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  3. Tamishraha Bagchi
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  4. B. S. Dwarkanath
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  5. Ambikanandan Misra
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Correspondence to Ambikanandan Misra.

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Surti, N., Naik, S., Bagchi, T. et al. Intracellular Delivery of Nanoparticles of an Antiasthmatic Drug. AAPS PharmSciTech 9, 217–223 (2008). https://doi.org/10.1208/s12249-008-9036-x

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  • DOI: https://doi.org/10.1208/s12249-008-9036-x

Key words

  • intracellular levels
  • mometasone furoate
  • nanoparticles
  • poly(d
  • l-lactic-co-glycolic) acid
  • sustained delivery
  • wheat germ agglutinin