Transdermal atenolol releasing system: an approach towards its development.
A polymer matrix system for transdermal delivery of atenolol was developed for its prolonged and controlled release using different ratios of ethylcellulose and hydroxypropyl methylcellulose. These polymeric matrix films were characterized for thickness, tensile strength, moisture content and drug content. They were also studied for in vitro drug release and in vitro drug skin permeation. The drug release from the films was found to be Fickian diffusion type and exhibiting linear relationship between drug release (Q) vs. square root of time (t0.5). The in vitro skin permeation of drug from transdermal drug delivery system (TDDS) was evaluated using dermatomed pig skin. The product which shows in vitro drug skin permeation near to 64 mcg/h/ml was selected for in vivo studies. The in vivo studies revealed that Ma EC HPMC 46 is most effective among the other polymeric matrix TDDS. The AUC0-28 with Ma EC HPMC 46 was better than orally administered conventional doses at twelve hours interval (AUC0-28 1587 ng h/ml) as well as no trough and peaks in drug plasma level was recorded with TDDS. Hence, it could be concluded that the designed polymeric matrix TDDS of atenolol could be used successfully for effective and prolonged delivery of atenolol. However, it further demands exploration in clinic, an insight vision towards the development of TDDS for commercial use.
Gupta
S P
SP
Government College of Pharmacy, Opp. Govt. Polytechnic, Vedant Road, Aurangabad, MS, 431005, India. sadhanashahi@yahoo.com
Jain
S K
SK
D000279:Administration, Cutaneous; D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D001262:Atenolol / Q000008:administration & dosage* / Q000493:pharmacokinetics; D002482:Cellulose / Q000031:analogs & derivatives; D002626:Chemistry, Pharmaceutical; D004058:Diffusion; D004339:Drug Compounding; D004355:Drug Stability; D005079:Excipients; D065347:Hypromellose Derivatives; D066298:In Vitro Techniques; D008747:Methylcellulose / Q000031:analogs & derivatives; D011817:Rabbits; D012867:Skin / Q000378:metabolism / Q000528:radiation effects; D012869:Skin Absorption / Q000187:drug effects; D012995:Solubility; D013552:Swine; D013718:Tensile Strength
D000319:Adrenergic beta-Antagonists; D005079:Excipients; D065347:Hypromellose Derivatives; D001262:Atenolol; C013517:ethyl cellulose; D002482:Cellulose; D008747:Methylcellulose