Transdermal atenolol releasing system: An approach towards its development

Abstract

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.

Poloxamer 407 microspheres for orotransmucosal drug delivery. Part II: In vitro/in vivo evaluation

“…Pharmacokinetic data of the market tablet showed a peak of AT concentration (2.77 ± 0.67 g/ml) 3 h after administration and a residual AT concentration at 24 h of 0.20 ± 0.10 g/ml with AUC value of 21.91 ± 6.89 g/ml h. The scientific literature reports opposing data about AT pharmacokinetic on rabbits. Gupta and Jain (2006) obtained C max and AUC values much lower than those of the present research in spite of the same T max value (3.00 h). In a comparative study among different formulations containing AT (oral, intravenous and transdermal matrices), Shin and Choi (2003) found AUC and C max values similar to our data after oral administration although the peak time was 1.6 h and absolute bioavailability very higher (77.4% vs 17.42%).…”

Effect of Polyunsaturated Fatty Acids and Some Conventional Penetration Enhancers on Transdermal Delivery of Atenolol

“…In case of oral administration, it can induce such side effects as diarrhea, nausea, ischemic colitis, and mesenteric arterial thrombosis. In recent years, owing to the advantages offered 108 C. PUGLIA AND F. BONINA by transdermal administration and the extensive use of atenolol in the treatment of various cardiovascular disorders, several authors have proposed different strategies to enhance penetration through the skin of atenolol (Cho and Shin 2004;Gupta and Jain 2006). Unfortunately the best part of these works were developed evaluating the percutaneous absorption of atenolol by means of synthetic membranes or animal skins that could not provide a real prediction of in vivo drug transdermal administration in humans (Scott, Walker, and Dugard 1986).…”