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Preparation and characterization of metoprolol tartrate containing matrix type transdermal drug delivery system

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Abstract

The present study aimed to develop matrix-type transdermal drug delivery system (TDDS) of metoprolol tartrate using polyvinyl pyrrolidone (PVP) and polyvinyl alcohol (PVA). The transdermal films were evaluated for physical parameters, Fourier transform infrared spectroscopy analysis (FTIR), differential scanning calorimetry (DSC), in vitro drug release, in vitro skin permeability, skin irritation test and stability studies. The films were found to be tough, non-sticky, easily moldable and possess good tensile strength. As the concentration of PVA was increased, the tensile strength of the films was also increased. Results of FTIR spectroscopy and DSC revealed the absence of any drug-polymer interactions. In vitro release of metoprolol followed zero-order kinetics and the mechanism of release was found to be diffusion rate controlled. In vitro release studies of metoprolol using Keshary-Chein (vertical diffusion cell) indicated 65.5 % drug was released in 24 h. In vitro skin permeation of metoprolol transdermal films showed 58.13 % of the drug was released after 24 h. In vitro skin permeation of metoprolol followed zero-order kinetics in selected formulations. The mechanism of release was found to be diffusion rate controlled. In a 22-day skin irritation test, tested formulation of transdermal films did not exhibit any allergic reactions, inflammation, or contact dermatitis. The transdermal films showed good stability in the 180-day stability study. It can be concluded that the TDDS of MPT can help in bypassing the first-pass effect and will provide patient improved compliance, without sacrificing the therapeutic advantages of the drugs.

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Authors and Affiliations

  1. Amity Institute of Pharmacy, Amity University, Lucknow, Uttar Pradesh, 226028, India

    Venkata Ramana Malipeddi

  2. Laureate Institute of Pharmacy, Jawalamukhi, Kangra, Himachal Pradesh, 176031, India

    Rajendra Awasthi

  3. Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Rua Professor Lineu Prestes, São Paulo, 05508-000, Brazil

    Daniela Dal Molim Ghisleni, Marina de Souza Braga, Irene Satiko Kikuchi & Terezinha de Jesus Andreoli Pinto

  4. School of Pharmacy and Biomedical Sciences, The University of Newcastle, Callaghan, Newcastle, NSW, 2308, Australia

    Kamal Dua

  5. School of Pharmaceutical Sciences, Shoolini University, Solan, Himachal Pradesh, 173229, India

    Kamal Dua

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  1. Venkata Ramana Malipeddi
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  2. Rajendra Awasthi
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  3. Daniela Dal Molim Ghisleni
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  4. Marina de Souza Braga
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  5. Irene Satiko Kikuchi
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  6. Terezinha de Jesus Andreoli Pinto
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  7. Kamal Dua
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Correspondence to Venkata Ramana Malipeddi.

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The authors confirm that this article has no conflict of interest.

Declaration of animal studies

The animal experimental protocol was approved by the Institutional Animal Ethical Committee. The animals were handled as per the guidelines of the Committee for the Purpose of Control and Supervision on Experimental animals (CPCSEA), New Delhi, India.

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Malipeddi, V.R., Awasthi, R., Ghisleni, D.D.M. et al. Preparation and characterization of metoprolol tartrate containing matrix type transdermal drug delivery system. Drug Deliv. and Transl. Res. 7, 66–76 (2017). https://doi.org/10.1007/s13346-016-0334-7

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  • DOI: https://doi.org/10.1007/s13346-016-0334-7

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