Document Type : Original Article
Authors
1
Faculty of Pharmacy, Heliopolis University, Department of Pharmaceutics & Pharmaceutical Technology, Cairo, Egypt
2
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.
3
Pharmaceutical Technology Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Cairo
4
Pharmaceutical Technology Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Cairo,
5
Pharmaceutical Technology Department, Pharmaceutical and Drug Industries Research Division, National Research Centre, Cairo, Egypt
Abstract
Carvedilol is a third-generation non-selective beta blocker commonly used in the long term management of hypertension in elderly people. Carvedilol is superior to older generation beta blockers in avoidance of fatigue due to low cerebral and cardiac blood flow because unlike other beta blockers, it works by decreasing peripheral resistance without any change in cardiac output. As the case with many beta blockers, carvedilol undergoes significant metabolism by liver enzymes, which leads to deficient oral bioavailability and the necessity of multiple dosing per day.
Carvedilol has been formulated as ethosomal vesicles using the cold method based on a four-factor three-level box-Behnken experimental design. The ethosomes were evaluated for vesicle size (Y1) and entrapment efficiency % (Y2). The effect of X1: phospholipid concentration, X2: Carvedilol concentration, X3: ethanol concentration, and X4: sonication time on Y1 and Y2 was evaluated and analysed using contour plots and second order polynomial equations.
The vesicle size ranged between 46.75 ± 8.0 nm and 259.3 ± 8.02nm and the entrapment efficiency % ranged between 86 % and 97 % for F7 and F23 respectively. Vesicle size (Y1) increased as the phospholipid concentration increased and sonication time decreased, yet the ethanol and Carvedilol concentrations gave concave curves with inflection points. There was an inverse relation between phospholipid concentration and EE%, but a positive effect (between Carvedilol concentration and EE% was observed.
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