Development And Evaluation Of Niosomal Formulation Of Carvedilol Using Food-Grade Surfactant

Abstract

Background:Efficient and safe drug delivery remains one of the major challenges in modern medicine. The emergence of nanotechnology has revolutionized drug delivery strategies, with nanocarriers being explored as potential “magic bullets” due to their ability to selectively target diseased tissues while sparing healthy cells. Among nanocarriers, niosomes have gained attention as promising alternatives to liposomes owing to their advantages, including lower production cost, improved chemical and physical stability, extended shelf life, broader pH tolerance, better oral bioavailability, reduced toxicity, and ease of handling and storage.

Aim:The present study aimed to formulate and characterize carvedilol-loaded niosomes prepared by the ultrasonication method, and to evaluate their entrapment efficiency, particle size distribution, morphology, and drug release profile in order to identify the most effective formulation.

Methodology:Niosomes were prepared using cremophor and cholesterol at molar ratios of 1:3, 1:6, and 1:12, with ethanol as a co-solvent. Carvedilol was entrapped via the ultrasonication technique. Morphological characteristics were evaluated using optical microscopy and transmission electron microscopy (TEM). Entrapment efficiency (%EE) was determined after gel filtration with Sephadex G-50. Particle size distribution and polydispersity index (PDI) were measured using a particle size analyzer. In vitro drug release was assessed using a USP type II dissolution apparatus (paddle type) in 900 mL of distilled water over 12.5 hours.

Results:All prepared niosomes were spherical in morphology with an average particle size of approximately 200 nm. The entrapment efficiency ranged from 72–90%, with the maximum observed in the F2 formulation (cremophor:cholesterol 1:6). The PDI values were below 0.4, indicating good uniformity and stability. In vitro release studies revealed sustained release patterns, with F2 showing the slowest release rate and maximum control over drug release compared to other formulations.

Conclusion:The findings suggest that carvedilol-loaded niosomes prepared by ultrasonication provide a stable and efficient drug delivery system. The F2 formulation was identified as the most promising, offering maximum entrapment efficiency and controlled release. These results highlight the potential of food-grade surfactants in developing safe and effective oral niosomal formulations for carvedilol and other drugs with poor bioavailability.