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Research Article

Design and development of a commercially viable in situ nanoemulgel for the treatment of postmenopausal osteoporosis

    Foziyah Zakir

    Department of Pharmaceutics, School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi, 110062, India

    ,
    Adil Ahmad

    Department of Pharmacognosy & Phytochemistry, School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi, 110062, India

    ,
    Uzma Farooq

    Department of Pharmaceutics, School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi, 110062, India

    ,
    Mohd Aamir Mirza

    Department of Pharmaceutics, School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi, 110062, India

    ,
    Alok Tripathi

    Endocrinology Division, Central Drug Research Institute, BS-10/1, Sec 10, Jankipuram Ext, Sitapur Road, P.O. Box 173, Lucknow, Uttar Pradesh, 226031, India

    ,
    Divya Singh

    Endocrinology Division, Central Drug Research Institute, BS-10/1, Sec 10, Jankipuram Ext, Sitapur Road, P.O. Box 173, Lucknow, Uttar Pradesh, 226031, India

    ,
    Faiyaz Shakeel

    Center of Excellence in Biotechnology Research (CEBR), Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2460, Riyadh, 11451, Saudi Arabia

    ,
    Sradhanjali Mohapatra

    Department of Pharmaceutics, School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi, 110062, India

    ,
    Farhan J Ahmad

    Department of Pharmaceutics, School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi, 110062, India

    &
    Kanchan Kohli

    *Author for correspondence: Tel.: 11 2605 9688; Fax: 11 2605 9663;

    E-mail Address: kanchankohli50@gmail.com

    Department of Pharmaceutics, School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi, 110062, India

    Published Online:https://doi.org/10.2217/nnm-2020-0079

    Aim: To investigate the potential of a thermosensitive intranasal formulation of raloxifene hydrochloride (RH) for systemic delivery with the possibility of enhanced bioavailability and anti-osteoporotic efficacy. Methods: In this work, a commercially scalable nanoemulsion in thermosensitive gel, aligned with better clinical acceptability, has been developed and evaluated. Results: A significant 7.4-fold improvement in bioavailability of RH was recorded when compared with marketed tablets. Likewise, in vivo pharmacodynamics studies suggested 162% enhanced bone density and significantly improved biochemical markers compared with per-oral marketed tablet. Conclusion: The formulation, being safe and patient compliant, successfully tuned anti-osteoporotic effects with improved therapeutic performance. Further, the work provided an exceptional lead to carry out the study in clinical settings.

    Graphical abstract

    Papers of special note have been highlighted as: • of interest; •• of considerable interest

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