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

作者：Malipeddi Venkata Ramana^*; Awasthi Rajendra; Ghisleni Daniela Dal Molim; Braga Marina de Souza; Kikuchi Irene Satiko; Andreoli Pinto Terezinha de Jesus; Dua Kamal

来源：Drug Delivery and Translational Research, 2017, 7(1): 66-76.

DOI：10.1007/s13346-016-0334-7

• Metoprolol tartrate
• Polyvinyl pyrrolidone
• Polyvinyl alcohol
• Skin permeation test
• Transdermal drug delivery
• Transdermal film

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 PVAwas 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.

• 出版日期2017-1