فهرست نشریات علمی دسترسی آزاد ایران

Carvedilol is a non-selective β-adrenergic blocker used in the management of cardiovascular disorders such as hypertension, heart failure, and post-myocardial infarction complications, with additional antioxidant and cytoprotective properties; however, its poor aqueous solubility and low oral bioavailability limit its therapeutic efficacy. This study aimed to enhance the solubility of carvedilol by developing an optimised liposomal formulation using the thin-film hydration method. The optimised composition, containing DPPC, HSPC, and cholesterol, was prepared and characterised for particle size, polydispersity index (PDI), zeta potential, entrapment efficiency (EE), drug loading (DL), and morphological and structural attributes. The resulting liposomes exhibited a mean particle size of 90.8 nm, a PDI of 0.031, and a zeta potential of −15.2 mV, indicating a stable nanosized dispersion. The EE and DL were 86.5% and 10.61%, respectively, confirming efficient drug encapsulation. X-ray diffraction (XRD) revealed the conversion of carvedilol from a crystalline to an amorphous state, while FESEM images demonstrated spherical vesicles with smooth surfaces. In vitro release studies in phosphate buffer (pH 6.8) showed a biphasic pattern, with sustained release up to 83.1% after 14 hours. The solubility of carvedilol increased by approximately 22 % in the liposomal formulation compared with the pure drug, and stability studies confirmed minimal aggregation and acceptable retention of EE % after three months at 4 °C. Overall, the optimised liposomal system successfully improved the solubility and release behaviour of carvedilol, highlighting its potential as a promising delivery platform for poorly water-soluble drugs.