Preparation and characterization of metoprolol tartrate containing matrix type transdermal drug delivery system.
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.
Amity Institute of Pharmacy, Amity University, Lucknow, Uttar Pradesh, 226028, India. mvramana@lko.amity.edu.
Venkata Ramana
VR
Malipeddi
Laureate Institute of Pharmacy, Jawalamukhi, Kangra, Himachal Pradesh, 176031, India.
Rajendra
0000-0002-1286-1874
R
Awasthi
Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Rua Professor Lineu Prestes, São Paulo, 05508-000, Brazil.
Daniela Dal Molim
DD
Ghisleni
Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Rua Professor Lineu Prestes, São Paulo, 05508-000, Brazil.
Marina
M
de Souza Braga
Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Rua Professor Lineu Prestes, São Paulo, 05508-000, Brazil.
Irene Satiko
IS
Kikuchi
Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of São Paulo, Rua Professor Lineu Prestes, São Paulo, 05508-000, Brazil.
Terezinha
T
de Jesus Andreoli Pinto
School of Pharmacy and Biomedical Sciences, The University of Newcastle, Callaghan, Newcastle, NSW, 2308, Australia.|School of Pharmaceutical Sciences, Shoolini University, Solan, Himachal Pradesh, 173229, India.
Kamal
K
Dua
D000279:Administration, Cutaneous; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000737:chemistry; D002152:Calorimetry, Differential Scanning; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004355:Drug Stability; D066298:In Vitro Techniques; D008790:Metoprolol / Q000008:administration & dosage* / Q000737:chemistry; D011142:Polyvinyl Alcohol / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D051381:Rats; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D023422:Skin Irritancy Tests; D017550:Spectroscopy, Fourier Transform Infrared
D000959:Antihypertensive Agents; D011142:Polyvinyl Alcohol; D011205:Povidone; D008790:Metoprolol
Metoprolol tartrate; Polyvinyl alcohol; Polyvinyl pyrrolidone; Skin permeation test; Transdermal drug delivery; Transdermal film
Acta Pharm. 2003 Jun;53(2):119-25
14764246
Clin Drug Investig. 2007;27(12):833-9
18020541
Curr Drug Deliv. 2012 May;9(3):285-96
22452403
Pharm Dev Technol. 2008;13(4):283-9
18649219
Drug Deliv. 2016;23 (2):378-94
25026414
Yakugaku Zasshi. 2008 Sep;128(9):1325-31
18758147
Curr Drug Deliv. 2005 Apr;2(2):125-31
16305413
Acta Pharm. 2010 Dec;60(4):467-78
21169138
Drug Deliv. 2004 Jan-Feb;11(1):27-31
15168788
Interv Med Appl Sci. 2016 Jun 1;8(2):68-76
28386462
Ther Deliv. 2010 Jul;1(1):109-31
21132122
Eur J Pharm Biopharm. 2004 Jul;58(1):107-19
15207544
Saudi Pharm J. 2015 Nov;23(6):587-602
26702253
Int J Pharm Investig. 2013 Oct;3(4):183-7
24350037
Indian J Pharm Sci. 2013 Mar;75(2):162-70
24019564