Abstract
The main objective of the investigation was to develop a transdermal therapeutic system for alfuzosin hydrochloride and to study the effects of polymeric system and loading dose on the in vitro skin permeation pattern. Principles of experimental design have been exploited to develop the dosage form. Ratio of ethyl cellulose (EC) and polyvinyl pyrrolidone (PVP) and loading dose were selected as independent variables and their influence on the cumulative amount of alfuzosin hydrochloride permeated per cm2 of human cadaver skin at 24 h (Q24), permeation flux (J) and steady state permeability coefficient (PSS) were studied using experimental design. Various physicochemical parameters of the transdermal films were also evaluated. Activation energy for in vitro transdermal permeation has been estimated. Ratio of EC and PVP was found to be the main influential factor for all the dependent variables studied. Drug loading dose was also found to influence the dependent variables but to a lesser extent. Physicochemical parameters of the prepared films were evaluated and found satisfactory. Activation energy for alfuzosin permeation has also been estimated and reported. The therapeutic system was found to be dermatologically non-irritant and hence, a therapeutically effective amount of alfuzosin hydrochloride can be delivered via a transdermal route.
Highlights
Benign prostatic hypertrophy (BPH) is a condition characterized by a nodular enlargement of prostatic tissue leading to obstruction of the urethra
It is thought that alpha-1 adrenergic receptor antagonists may be implicated in the pathophysiology of BPH and may cause relaxation of smooth muscles, improvement in urine flow and reduction in lower urinary tract symptoms (LUTS) [3]
The result of the moisture uptake (%) and moisture content (%) studies revealed that the moisture uptake/content was found to increase with increasing concentration of hydrophilic polymer polyvinyl pyrrolidone (PVP)
Summary
Benign prostatic hypertrophy (BPH) is a condition characterized by a nodular enlargement of prostatic tissue leading to obstruction of the urethra. LUTS including increased urinary frequency, nocturia, incomplete emptying, and urinary hesitancy are often associated with BPH. These symptoms can be caused by altered function of the smooth muscle tone that is regulated by the alpha-1 adrenergic receptors in the prostate and its capsule, the bladder base and neck, and the prostatic urethra [2]. A quinazoline derivative, is a selective and competitive alpha-1 adrenoceptor antagonist. It distributes preferentially in the prostate, compared with plasma, and decreases the sympathetically controlled tone of prostatic smooth muscle. Lower urinary tract symptoms suggestive of benign prostatic hyperplasia (BPH) are improved [4]
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