Development of Carvedilol-Encapsulated Liposomal Nanoparticles Using the Thin Film Hydration Method: A Design Expert®-Based Approach

نویسندگان

1 Najaf Health Directorate, Alzahraa Teaching Hospital, Najaf, Iraq

2 Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, University of Kufa, Najaf-52001, Iraq

doi
10.22052/JNS.2025.04.054
چکیده

Liposomes are tiny spherical structures made from phospholipid bilayers that can encapsulate drugs with varying solubility profiles. Their unique ability to improve drug solubility, protect active compounds, and enable targeted delivery makes them valuable in pharmaceutical applications. This nanocarrier system is handy for enhancing the bioavailability of drugs like carvedilol, which have poor water solubility. Carvedilol is a non-selective beta-blocker commonly used to treat hypertension and heart failure. However, its poor water solubility limits its bioavailability and therapeutic effectiveness. Incorporating carvedilol into liposomal nanoparticles can improve its solubility and controlled release, potentially enhancing its clinical performance. This study aimed to prepare carvedilol-loaded liposomal nanoparticles using the hydration method and to apply Design Expert® software to choose the best formulation while minimising time and cost. The quantities of phospholipids and cholesterol were varied and considered as independent variables. In contrast, particle size, polydispersity index (PDI), entrapment efficiency, drug loading and zeta potential were considered as characterisation outcomes. The liposomes were prepared using the thin film hydration method. The particle size and polydispersity index (PDI) were analysed using the ABT-9000 Nano Laser particle Size analyser. The particle size ranged from 147-61 nm, with a homogeneous distribution indicated by a PDI of ≤ 0.1, and the zeta potential values of the liposomal formulations ranged from −0.3 mV to −12.4 mV. The entrapment efficiency (EE) and drug loading (DL) of the formulations ranged from 55.41% to 92.38% and from 6.52% to 13.58%, respectively, as determined using a Shimadzu UV–Visible spectrophotometer. Liposomes were successfully prepared using the film hydration method, followed by particle size reduction through extrusion. The selected formulation consisted of 45 mg DPPC, 18.5 mg HSPC, and 8 mg cholesterol.

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