Cyclosporine CsA—The Physicochemical Characterization of Liposomal and Colloidal Systems

Abstract

This paper presents an overview of the possibilities of testing various cyclosporine (CsA) formulations with an emphasis on parameters that may be key to improving the stability and biocompatibility. The feasibility of CsA colloidal systems for oral (injection) administration were investigated using different techniques and compared with similar investigations of other researchers. The chosen CsA systems were developed using dipalmitoylphosphocholine (DPPC) and/or cholesterol as a lipid matrix, stabilized with ethanol, with soybean oil or n-tetradecane as oil phase in emulsions, under natural pH, room and physiological temperature. Their integrity was found to be strictly dependent on the stabilizers. The highest CsA penetrability with the system containing phospholipid in the context of its interactions with lipid membranes was shown. Also, the bioavailability of CsA can be enhanced with the biopolymer antibacterial chitosan. This mini-review suggests the suitability of liposome/microemulsion as promising vehicles for CsA delivery. The most hopeful proved to be formulation with the smaller particle size facilitating absorption, but when safety is assessed, relying on just the particle size cannot be the only criteria. Reassumed, the CsA formulation stability known on the basis of the size and zeta potential measurements guarantees a decrease of the individual variations in the drug bioavailability, toxicity and minimizes rejection.

Analysis of Molecular Interactions between Components in Phospholipid-Immunosuppressant-Antioxidant Mixed Langmuir Films

“…Thus, the administration of this sparingly watersoluble drug is either complicated or ineffective through the oral route. 9,10 Therefore, other ways of introducing CsA into the body are being sought. The direct coating of the implant surface with the CsA film is a route that deserves exploration.…”

“…Despite the promising applications of CsA, this material is a neutral, extremely hydrophobic drug of high molecular weight (1203 Da), which exhibits low water solubility, poor permeability through biological barriers (gastrointestinal tract, skin, and cornea), and instability in the gastrointestinal medium. Thus, the administration of this sparingly water-soluble drug is either complicated or ineffective through the oral route. , Therefore, other ways of introducing CsA into the body are being sought. The direct coating of the implant surface with the CsA film is a route that deserves exploration.…”

“…The direct coating of the implant surface with the CsA film is a route that deserves exploration. Moreover, the major clinical concern is CsA-induced nephrotoxicity, hepatotoxicity, neurotoxicity, and cardiovascular diseases. ,− These side-effects are associated with reactive oxygen species (ROS). Namely, CsA action/treatment generates excessive production of oxygen free radicals that lead to lipid peroxidation, which is the main source of damage to the cell membrane integrity, e.g., in vascular and cardiac tissues, general inflamed tissues, and implanted biomaterials.…”

Unraveling Drug Delivery from Cyclodextrin Polymer-Coated Breast Implants: Integrating a Unidirectional Diffusion Mathematical Model with COMSOL Simulations

“…The difference in diffusivity can be attributed to the characteristics of the implants. For smooth implants, the thin coating on the upper substrate surface allowed for the rapid adsorption of the PBS solution, facilitating unrestricted drug movement and diffusion [ 32 , 33 , 34 ]. Conversely, the textured samples, with their thick and irregular polymer coating, adsorbed the PBS solution at a slower rate, thus favoring mass diffusion, in accordance with the molecular weight of the released drugs.…”

Preparation and Characterization of Astaxanthin-loaded Liposomes Stabilized by Sea Cucumber Sulfated Sterols Instead of Cholesterol

“…No significant difference was found in the zeta potential values of SL (−22.33±1.35 mV) and ASL (−21.13± 1.01 mV) ( p＞0.05) , which were significantly higher than those stabilized by cholesterol as of CL (−6.30±0.78 mV) and ACL (−5.61±0.38 mV) , as well as plant sterol as of PL (−4.72±0.68 mV) and APL (−5.80±0.21 mV) . The higher the absolute value of zeta potential indicated higher stability of the particle system in general 1,24) . According to the previous finding, the zeta potential of liposomes was mainly attributed to the lecithin compositions due to the lack of charge for sterols 25) .…”