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Formulation and Evaluation of Eudragit® RL Polymeric Double Layer Films for Prolonged-Release Transdermal Delivery of Tamsulosin Hydrochloride

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Abstract

Transdermal drug delivery systems (TDDSs) were developed for prolonged tamsulosin (TMS) delivery. Double layer (DL) TDDSs were prepared using Eudragit® RL by conventional film-forming. Ethylene-vinyl acetate was used as the backing layer, triethylcitrate as plasticizer, and Capmul® PG-8-70 NF and Captex 170 EP as penetration enhancers (PEs). An increase in either drug or PE concentration caused a significant increase in drug permeation flux. Modulation of drug permeation across Strat-M® membrane was examined using a single layer (SL) having the same thickness and drug content as the DLs, while the DLs were formulated to have variable drug spatial distribution across each layer (DL 4:6 and DL 6:4). SL/TDDS showed significantly higher daily drug permeation than DL/TDDSs for the first 4 days which could be related to the presence of high TMS concentration located on the upper surface of SL/TDDS as a result of solute migration of TMS during the drying process. However, this increase was followed by a progressive linear decrease after 5 days. Deflection points that were characterized by lower drug flux had been shown by SL/TDDS at more than one-point times. In contrast, DL 4:6 and DL 6:4 TDDSs demonstrated an ability to sustain TMS delivery for up to 2 weeks.

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Acknowledgements

The authors would like to acknowledge the Target Chemicals, Jordan, for donating Eudragit® RL and Al Taqaddom Pharmaceuticals Industries, Jordan, for providing tamsulosin hydrochloride.

Funding

This research was funded by the Jordan University of Science and Technology grant number 20200116.

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Authors and Affiliations

  1. Department of Pharmaceutical Technology, Faculty of Pharmacy, Jordan University of Science and Technology, P. O. Box 3030, Irbid, 22110, Jordan

    Shereen M. Assaf, Aya M. Ghanem & Shayma’a A. Alhaj

  2. Department of Pharmaceutics and Pharmaceutical Technology, School of Pharmacy, The University of Jordan, Amman, 11942, Jordan

    Enam A. Khalil

  3. Al Taqaddom Pharmaceuticals Industries, P.O. Box 960761, Amman, 11196, Jordan

    AlSayed Alarabi Sallam

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  1. Shereen M. Assaf
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Contributions

Conceptualization, Assaf S.M., and Sallam A.A.; Methodology, Assaf S.M., Khalil E.A., and Sallam A.A.; validation, Assaf S.M., Ghanem A.M., and Sallam A.A.; formal analysis, Ghanem A.M.; investigation, Ghanem A.M. and Alhaj, S.A.; resources, Ghanem A.M. and Alhaj S.A.; data curation, Assaf S.M., Ghanem A.M., and Sallam A.A.; writing – original draft preparation, Assaf S.M.; Writing – Review & Editing, Assaf S.M., Ghanem A.M., Sallam A.A.; visualization, Ghanem A.M.; supervision, Assaf A.A., Sallam A.A., and Khalil E.A.; project administration, Assaf S.M. and Sallam A.A.; funding acquisition, Assaf S.M.

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Correspondence to Shereen M. Assaf.

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Supplementary Information

ESM 1

SEM images of the Strat-M membrane: (A) before permeation study and after (B) one week and (C) two weeks of the permeation study at 2500x magnification power. (GIF 86 kb)

ESM 2

Two-week in vitro permeation profiles of TMS from P9 after storing at 5 °C (refrigerated), 30 °C/ 60% RH (30 degrees), and 40 °C/ 75% RH (40 degrees), through Strat-M® membrane into phosphate buffer (pH 6.8) at 32 ± 1 oC, compared with its permeation from a freshly prepared patch (mean ± RSD, n=3). (GIF 12 kb)

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Assaf, S.M., Ghanem, A.M., Alhaj, S.A. et al. Formulation and Evaluation of Eudragit® RL Polymeric Double Layer Films for Prolonged-Release Transdermal Delivery of Tamsulosin Hydrochloride. AAPS PharmSciTech 23, 210 (2022). https://doi.org/10.1208/s12249-022-02358-x

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