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Enhancement of ocular efficacy of aceclofenac using biodegradable PLGA nanoparticles: formulation and characterization

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Abstract

In the present study, an effort was made to design poly (D, L-lactide-co-glycolide) acid nanoparticles of aceclofenac by direct precipitation method. The nanoparticles were found to have adequate particle size range for ocular administration of 162.6 to 244.13 nm with nearly spherical shape and with zeta potential of − 21.5 to − 25.5 mV. Drug entrapment efficiency of nanoparticle formulations ranged from 42.9 to 92.68%. Differential scanning calorimetric (DSC) and powder X-ray diffraction (PXRD) studies depicted that the drug incorporated in nanoparticles was found to be in amorphous state. Moreover, nanoparticles showed prolonged in vitro drug release profile and followed Higuchi-square-root release kinetics. Nanoparticles showed two folds higher permeation than aqueous solution of aceclofenac. Nanoparticles were well tolerated with no signs of corneal damage in in vitro transcorneal permeation studies. The formulation was quite stable. In vivo ocular anti-inflammatory study in the rabbit eyes confirmed better efficacy of nanoparticles as compared with the aqueous solution and its potential application in ocular inflammatory conditions.

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Acknowledgements

Authors are thankful to Govt. of NCT, New Delhi, India for providing fellowship to Rajesh Katara and Ranbaxy Laboratories Ltd. (Gurgaon, India) for gifting aceclofenac bulk drug. Thanks are also due to the National Institute of Immunology (New Delhi, India) for gifting PLGA and SAIF at AIIMS (New Delhi) for TEM.

Author information

Author notes

  1. Sameer Sachdeva

    Present address: Amneal Pharmaceuticals, 1 New England Ave, Piscataway, NJ, 08854, USA

  2. Dipak K. Majumdar

    Present address: School of Pharmaceutical Sciences, Apeejay Stya University, Gurgaon, India

Authors and Affiliations

  1. Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences and Research, (Formerly College of Pharmacy), University of Delhi, Pushp Vihar, Sector III, New Delhi, 110017, India

    Rajesh Katara, Sameer Sachdeva & Dipak K. Majumdar

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  1. Rajesh Katara
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Correspondence to Rajesh Katara.

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Authors Rajesh Katara, Sameer Sachdeva, and Dipak K Majumdar declare that they have no conflict of interest.

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All institutional and national guidelines for the care and use of laboratory animals were followed.

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Katara, R., Sachdeva, S. & Majumdar, D.K. Enhancement of ocular efficacy of aceclofenac using biodegradable PLGA nanoparticles: formulation and characterization. Drug Deliv. and Transl. Res. 7, 632–641 (2017). https://doi.org/10.1007/s13346-017-0416-1

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  • DOI: https://doi.org/10.1007/s13346-017-0416-1

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