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.
Highlights
Nanotechnology is one of the most promising strategies developed to improve drug delivery systems
Studies demonstrated that hydrophilic nanoparticles are flattened in the membrane plane, while hydrophobic nanoparticles are elongated during penetration
This study reported that the area under the curve (AUC) parameters describing the drug concentration in the period of 0–12 h of cyclosporine A (CsA) emulsion and CsA micellar solution were, respectively, 9.2- and 28.5-fold higher than the same parameters of oil-CsA in the corneal stroma endothelium
Summary
Nanotechnology is one of the most promising strategies developed to improve drug delivery systems. Effective delivery systems allow for the protecting of drugs from fast degradation, long-term in vivo retention, immune escape, targeted controlled drug release, and give the opportunity to cross specific barriers in vivo [3,4,5,6]. Other factors, such as size, surface charge, shape, lipid composition (headgroups, the length of the tail, and even the saturability of the lipid carriers), and elastic and curvature energies may influence the barrier permeability and transport [7,8]. The unique properties of lipid-based systems, including their ability to facilitate extended circulation time, adhesion, and homologous targeting, have led to their various applications in the context of nanomedicine [6,7,8,9]
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