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Preparation and In Vitro/In Vivo Evaluation of Antihistaminic Ocular Inserts

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Pharmaceutical Chemistry Journal Aims and scope

The present study aims to prepare ocular inserts of cetirizine hydrochloride, an antihistamine used to treat allergic conjunctivitis, allergic rhinitis, uveitis and urticaria. Solvent casting method was used to prepare inserts of hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA) as film forming polymers, and polyethylene glycol (PG) and glycerin were used as plasticizers. Various physicochemical parameters of six ocular insert compositions were evaluated, including swelling behavior and in vitro drug release and kinetics. Formulation F4 showed results of in vitro studies in most appropriate range, with sustained drug release (99.12% at 210 min) following non-fickian diffusion. Drug – polymer compatibility study verified no chemical interaction between the drug and polymer. Therefore, formulation F4 was selected for in vivo studies in albino rabbits. The values of Cmax, AUC, and Tmax of formulation F4 were 478.70 ng/mL, 3013.58 ng/(mL h), and 2.3 h, respectively. Ocular inserts of cetirizine hydrochloride provide a valuable alternative for the treatment of ocular inflammatory diseases as these formulations ensure sustained drug release and increased residence time.

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Acknowledgments

The authors greatly appreciate the moral support of our research group.

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Conflict of Interest

The authors declare that they have no conlicts of interest to disclose.

Funding

This research received no specific grant from any funding agency in the public, commercial or not-for-profit sectors.

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Authors and Affiliations

  1. Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan

    Syed Nisar Hussain Shah & Ahmad Nawaz

  2. SNS Pharmaceutical Lab, Multan, Pakistan

    Hina Javed, Misbah Rafiq & Romana Riaz

  3. Department of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, 63100, Pakistan

    Hadia Sadaquat & Muhammad Akhtar

Authors
  1. Syed Nisar Hussain Shah
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  2. Ahmad Nawaz
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  3. Hina Javed
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  4. Misbah Rafiq
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Correspondence to Muhammad Akhtar.

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Shah, S.N.H., Nawaz, A., Javed, H. et al. Preparation and In Vitro/In Vivo Evaluation of Antihistaminic Ocular Inserts. Pharm Chem J 52, 615–622 (2018). https://doi.org/10.1007/s11094-018-1870-x

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  • DOI: https://doi.org/10.1007/s11094-018-1870-x

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