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Preclinical Investigation of Transdermal Route for Enhanced Bio-performance of Duloxetine HCl

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Abstract

The aim of the study was to develop and optimise drug-in-adhesive (DIA) transdermal patch of duloxetine HCl for enhanced drug delivery. DIA patch so developed reduced the dose and dosing frequency by enhancing bio-performance of the drug. A transdermal DIA patch having Duro-Tak 87–2287 as DIA polymer and Transcutol P as permeation enhancer loaded with 40% drug previously complexed with MeβCD duly characterised (FTIR, DSC, and SEM) was developed for in vivo study. Pharmacokinetic parameters of developed formulation were assessed and compared with oral route of administration. Among various permeation enhancers (PEs), Transcutol P exhibited most enhanced permeation (ER ≈ 1.99) in terms of flux and Q24 compared to control group having. Mean of maximum plasma concentration (Cmax) and area under time-concentration curve (AUC0–72) in Wistar rats (n = 6) for transdermal patch (10 mg/kg) was found to be 70.31 ± 11.2 ng/ml and 2997.29 ± 387.4 ng/ml*h, respectively, and were considerably higher than oral dose of DLX (20 mg/kg and 10 mg/kg). Albeit, T1/2 was higher in case of transdermal delivery, but this was due to sustained behaviour of delivery system. These findings highlight the significance of both inclusion complexation and transdermal delivery of DLX using DIA patch for efficient drug absorption.

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Data Availability

The datasets supporting study are available from the corresponding author on reasonable request.

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Acknowledgements

Authors are thankful to Cyclolabs, Budapest, Hungary, for providing gratis samples of different cyclodextrin derivatives and department of SAIF/CIL, Panjab University Chandigarh, for carrying out different analyses. Department of Pharmaceutics, NIPER, Mohali is acknowledged for extending spray drying facility.

Funding

This work was supported by University Grants Commission (UGC, India) through award letter (F1-17.1/2014–15/RGNF-2014–15-SC-HAR-68055) sanctioned to first author.

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Authors and Affiliations

  1. University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh-160014, India

    Rajiv Kumar, V. R. Sinha & Amita Sarwal

  2. Chandigarh College of Pharmacy, Landran-140307, Mohali, India

    Rajiv Kumar

  3. Institute of Pharmaceutical Sciences, Kurukshetra University, Kurukshetra-136119, India

    Lalita Dahiya

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  1. Rajiv Kumar
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  2. V. R. Sinha
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  3. Lalita Dahiya
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  4. Amita Sarwal
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Contributions

All authors contributed to study conception and design. Material preparation, data collection, and analysis were performed by Rajiv Kumar and Amita Sarwal. First draft of manuscript was written by Rajiv Kumar and all authors commented on previous versions of manuscript. All authors read and approved the final manuscript.

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Correspondence to Rajiv Kumar or Amita Sarwal.

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All protocols involving laboratory animals are approved from institutional animal ethical committee, Panjab University, Chandigarh.

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Kumar, R., Sinha, V.R., Dahiya, L. et al. Preclinical Investigation of Transdermal Route for Enhanced Bio-performance of Duloxetine HCl. AAPS PharmSciTech 24, 154 (2023). https://doi.org/10.1208/s12249-023-02607-7

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