Characterization and stability studies of a novel liposomal cyclosporin A prepared using the supercritical fluid method: comparison with the modified conventional Bangham method

Abstract

Abstract:A novel method to prepare cyclosporin A encapsulated liposomes was introduced using supercritical fluid of carbon dioxide (SCF-CO 2 ) as an antisolvent. To investigate the strength of the newly developed SCF-CO 2 method compared with the modified conventional Bangham method, particle size, zeta potential, and polydispersity index (PDI) of both liposomal formulations were characterized and compared. In addition, entrapment efficiency (EE) and drug loading (DL) characteristics were analyzed by reversed-phase high-performance liquid chromatography. Significantly larger particle size and PDI were revealed from the conventional method, while EE (%) and DL (%) did not exhibit any significant differences. The SCF-CO 2 liposomes were found to be relatively smaller, multilamellar, and spherical with a smoother surface as determined by transmission electron microscopy. SCF-CO 2 liposomes showed no significant differences in their particle size and PDI after more than 3 months, whereas conventional liposomes exhibited significant changes in their particle size. The initial yield (%), EE (%), and DL (%) of SCF-CO 2 liposomes and conventional liposomes were 90.98 ± 2.94, 92.20 ± 1.36, 20.99 ± 0.84 and 90.72 ± 2.83, 90.24 ± 1.37, 20.47 ± 0.94, respectively, which changed after 14 weeks to 86.65 ± 0.30, 87.63 ± 0.72, 18.98 ± 0.22 and 75.04 ± 8.80, 84.59 ± 5.13, 15.94 ± 2.80, respectively. Therefore, the newly developed SCF-CO 2 method could be a better alternative compared with the conventional method and may provide a promising approach for large-scale production of liposomes.

Potential Use of Guarana-Loaded Liposomes in Topical Applica-Tions: Toxicity Profile Assessment Using Different Skin Cell Lines

“…The low zeta potential values agree with the characteristics of the phospholipid (soy phosphatidylcholine) used for the production of these liposomes [65]. The findings in this paper corroborated the results obtained by Karn, Parkl and Hwangl, (2013) [66], where they produced liposomes using Lipoid S100  and cholesterol obtained vesicles with potentials of -6.8 to -7.7 mV.…”

Assembling Surfactants-Mucoadhesive Polymer Nanomicelles (ASMP-Nano) for Ocular Delivery of Cyclosporine-A

“…Restasis®from Allergan (Irvine, CA, USA) is a 0.05% CyA anionic emulsion, containing castor oil and polysorbate 80 as emulsifying agent, and was launched on the United States market before 2012, while Ikervis®(Santen Oy, Tampere, Finland), a 0.1% CyA stable cationic nanoemulsion based on Nanosorb®technology, was granted marketing authorisation by the European Commission (EC) for treatment of severe keratitis in adult patients with DED only after 2015. These commercial products result from many attempts done by using different strategies, still in continuous development, such as prodrugs [12], liposomes [13], nanoparticles [14], nanosphere [15], solid lipid nanoparticles [16][17][18], contact lenses [19], ocular inserts [20,21], implants [22] and emulgel [23]. Each of these techniques has contributed to solve various critical issues such as cytotoxicity, low precorneal residence time after ocular instillation with reduced bioavailability and low solubility.…”

Lipid nanoparticle-based formulations for high-performance dentistry applications

“…64 This method is termed as the supercritical antisolvent method, which results in improved entrapment efficiency and stability when compared to the conventional Bangham method. 65 Spray drying involves the utilization of the heating of mixture of core carriers such as mannitol or lactose, ethanolsolubilized lipid, and L-leucine (aerosol modifier for reducing the surface tension of the spray-dried powder) in the aqueous phase to form a homogenous solution. 66 Drug-ethanol solution is then added to the previously homogenized solution to form a clear solution, which is then spray-dried to form powdered proliposomes.…”