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

Malipeddi, VR; Awasthi, R; Ghisleni, DDM; de Souza Braga, M; Kikuchi, IS; de Jesus Andreoli Pinto, T; Dua, K

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

Malipeddi, VR Awasthi, R Ghisleni, DDM de Souza Braga, M Kikuchi, IS de Jesus Andreoli Pinto, T Dua, K

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Publication Type:: Journal Article
Citation:: Drug Delivery and Translational Research, 2017, 7 (1), pp. 66 - 76
Issue Date:: 2017-02-01

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Field	Value	Language
dc.contributor.author	Malipeddi, VR	en_US
dc.contributor.author	Awasthi, R	en_US
dc.contributor.author	Ghisleni, DDM	en_US
dc.contributor.author	de Souza Braga, M	en_US
dc.contributor.author	Kikuchi, IS	en_US
dc.contributor.author	de Jesus Andreoli Pinto, T	en_US
dc.contributor.author	Dua, K https://orcid.org/0000-0002-7507-1159	en_US
dc.date.issued	2017-02-01	en_US
dc.identifier.citation	Drug Delivery and Translational Research, 2017, 7 (1), pp. 66 - 76	en_US
dc.identifier.issn	2190-393X	en_US
dc.identifier.uri	http://hdl.handle.net/10453/125257
dc.description.abstract	© 2016, Controlled Release Society. 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.	en_US
dc.relation.ispartof	Drug Delivery and Translational Research	en_US
dc.relation.isbasedon	10.1007/s13346-016-0334-7	en_US
dc.subject.mesh	Skin	en_US
dc.subject.mesh	Animals	en_US
dc.subject.mesh	Rats	en_US
dc.subject.mesh	Metoprolol	en_US
dc.subject.mesh	Polyvinyl Alcohol	en_US
dc.subject.mesh	Povidone	en_US
dc.subject.mesh	Antihypertensive Agents	en_US
dc.subject.mesh	Drug Delivery Systems	en_US
dc.subject.mesh	Calorimetry, Differential Scanning	en_US
dc.subject.mesh	Spectroscopy, Fourier Transform Infrared	en_US
dc.subject.mesh	Administration, Cutaneous	en_US
dc.subject.mesh	Drug Stability	en_US
dc.subject.mesh	Skin Irritancy Tests	en_US
dc.subject.mesh	Skin Absorption	en_US
dc.subject.mesh	In Vitro Techniques	en_US
dc.subject.mesh	Drug Liberation	en_US
dc.title	Preparation and characterization of metoprolol tartrate containing matrix type transdermal drug delivery system	en_US
dc.type	Journal Article
utslib.citation.volume	1	en_US
utslib.citation.volume	7	en_US
utslib.for	1115 Pharmacology and Pharmaceutical Sciences	en_US
pubs.embargo.period	Not known	en_US
pubs.organisational-group	/University of Technology Sydney
pubs.organisational-group	/University of Technology Sydney/Graduate School of Health
utslib.copyright.status	closed_access
pubs.issue	1	en_US
pubs.publication-status	Published	en_US
pubs.volume	7	en_US

Abstract:

© 2016, Controlled Release Society. 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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http://hdl.handle.net/10453/125257