Effect of film composition and various penetration enhancers concentrations on prazosin release from acrylic polymeric films.
An investigation was conducted to evaluate the effect of changing the Eudragit RL 100 ratio and the influence of different penetration enhancers in various concentrations on the release of prazosin from Carboset 525:Eudragit RL 100 polymeric films using improved Franz diffusion cells, to choose the most suitable polymeric film ratio, the most appropriate enhancer and its optimum concentration to be used to achieve the maximum release of the drug. The results show that prazosin release from polymeric films containing Carboset 525:Eudragit RL 100 in a 1:1 ratio was significantly (p < 0.05) higher than from films in a 1:0.25 ratio and non-significantly (p > 0.05) higher than from those containing 1:0.5, 1:3 polymer ratios and non-significantly lower from those containing 1:4 polymer ratios. The addition of various enhancers, n-decyl alcohol (7, 9 and 11% w/w), Azone (4, 6 and 8% w/w) and Cineole (7, 9, 11 and 14% w/w) significantly (p < 0.05) enhanced the prazosin release from these polymeric films containing the two polymers in a 1:1 ratio. The best concentrations of these enhancers were 11% n-decyl alcohol, 9% Cineole and 8% Azone. The formulations containing these concentrations of the enhancers are being further studied for drug release through rabbits skin. It was found that using either of these enhancers in these concentrations resulted in a significant (p < 0.05) increase in the amount of prazosin transported across the skin. On the other hand these enhancers did not show any significant (p > 0.05) difference between them. The mechanism of drug release from the polymeric films was further studied using water vapor permeability (W.V.P.), the permeability constant (P) and differential scanning calorimetry. The enhancers were found to increase the W.V.P. and the permeability constant (P) and the results were in very good agreement with the effect of enhancers on the in-vitro drug release. The DSC thermograms showed that the enhancers physically interacted with either or both of the polymeric film materials and prazosin which could be one of the reasons for the improvement in the release of the drug from these polymeric films.
Hosny
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EA
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Abdel Hady
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SS
Niazy
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EM
D000180:Acrylic Resins / Q000737:chemistry*; D000279:Administration, Cutaneous; D000317:Adrenergic alpha-Antagonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000818:Animals; D002152:Calorimetry, Differential Scanning; D002851:Chromatography, High Pressure Liquid; D008297:Male; D011224:Prazosin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011817:Rabbits; D012867:Skin / Q000378:metabolism
D000180:Acrylic Resins; D000317:Adrenergic alpha-Antagonists; C050528:Eudragit RS; C111565:Carboset 525; D011224:Prazosin