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Raloxifene encapsulated spanlastic nanogel for the prevention of bone fracture risk via transdermal administration: Pharmacokinetic and efficacy study in animal model

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Abstract

This research work is to evaluate spanlastic-loaded raloxifene (RLX) nanogel administration via the transdermal route to avoid its hepatic metabolism and to enhance the bioavailability for better management of osteoporosis. RLX-loaded spanlastic nanogel was prepared and characterized for its viscosity, pH, spreadability, and texture profile. The formulation was applied on the skin surface of the animal for pharmacokinetic evaluation, and later, the efficacy of the formulation was assessed in ovariectomized female Wistar rats. The nanogel was obtained with a viscosity (2552.66 ± 30.61 cP), pH (7.1 ± 0.1), and spreadability (7.1 ± 0.2 cm). The texture properties, cohesiveness, and adhesiveness of the nanogel showed its suitability for transdermal application. Nanogel showed no sign of edema and erythema in the skin irritation test which revealed its safety for transdermal application. The t1/2 obtained for RLX-spanlastic nanogel (37.02 ± 0.59 h) was much higher than that obtained for RLX-oral suspension (14.43 h). The relative bioavailability was found to be 215.96% for RLX-spanlastic nanogel, and the drug and formulation did not show any toxicity in any of the vital organs, as well as no hematological changes occurring in blood samples. In microarchitectural measurement, RLX-spanlastic nanogel exhibited no unambiguous deviations along with improved bone mineral density compared to the RLX suspension treated group. Transdermal administration of RLX-spanlastic nanogel showed significant improvement of drug bioavailability (approx. twice to oral administration) without any toxic effect in the treated rats. Hence, spanlastic nanogel could be a better approach to deliver RLX via transdermal route for the management of osteoporosis.

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Availability of data and materials

The datasets generated during and/or analyzed during the current study are available from the corresponding author on reasonable request.

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Acknowledgements

Author, Mohd. Danish Ansari acknowledges Hamdard National Foundation (HNF), New Delhi for its support during the period.

Funding

Author Mohd. Danish Ansari received Hamdard National Foundation (HNF), New Delhi, for its support during the research work.

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Authors and Affiliations

  1. Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard (Deemed University), M. B. Road, 110062, New Delhi, India

    Mohd Danish Ansari, Jayamanti Pandit, Ayesha Waheed, Rao Nargis Jahan, Iram khan, Mohd Aqil & Yasmin Sultana

  2. Department of Pharmacology, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India

    Sadat Shafi, Divya Vohora & Shreshta Jain

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  1. Mohd Danish Ansari
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Contributions

Mohd. Danish Ansari: writing, concept, and methodology; Sadat Shafi: methodology; Jayamanti Pandit: final draft and review; Ayesha Waheed: methodology and writing; Rao Nargis Jahan: evaluation and methodology; Iram Khan: methodology and writing; Divya Vohora: evaluation and methodology; Shreshta Jain: methodology and evaluation; Mohd. Aqil: reviewing and concept; Yasmin Sultana: supervision, evaluation, and final draft.

Corresponding author

Correspondence to Yasmin Sultana.

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Approval for conducting animal study was approved by Institutional Animal Ethics Committee, Jamia Hamdard, New Delhi, and the approval no. for animal protocol is 1725.

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Ansari, M.D., Shafi, S., Pandit, J. et al. Raloxifene encapsulated spanlastic nanogel for the prevention of bone fracture risk via transdermal administration: Pharmacokinetic and efficacy study in animal model. Drug Deliv. and Transl. Res. 14, 1635–1647 (2024). https://doi.org/10.1007/s13346-023-01480-y

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