Influence of drug/lipid interaction on the entrapment efficiency of isoniazid in liposomes for antitubercular therapy: a multi-faced investigation

High-Resolution Ultrasound Spectroscopy for the Determination of Phospholipid Transitions in Liposomal Dispersions

“…Other studies have investigated the influence of the different hydrophilicity of model drugs in relation to their ability to be located in liposomes such as entrapped inside the aqueous compartment, adsorbed or partially inserted at the level of the water-bilayer interface or partitioned in the phospholipid membrane [ 38 , 39 ]. Specifically, the relationship between the drug localization and the thermal behaviour of loaded liposomes has been mainly investigated by using calorimetry in association with other techniques such as small-angle scattering [ 40 , 41 ]. Here, the comparison between mDSC and HR-US is proposed, instead.…”

Two Types of Liposomal Formulations Improve the Therapeutic Ratio of Prednisolone Phosphate in a Zebrafish Model for Inflammation

“…Theoretical encapsulation efficiency ( EE% theoretical ) and measured encapsulation efficiency ( EE% measured ) were determined as follows: where C encapsulated is the PLP concentration after removal of the free drug (by SEC), as determined by the absorbance of PLP via UV–Vis and its calibration curve ( Supplementary Materials Figure S4 ), multiplied by 20 (due to the dilution in MeOH for liposome disruption) and by 2.5 (due to the dilution during SEC); C initial is the initial PLP concentration used to hydrate the lipid film before extrusion; C expected is the theoretical PLP concentration that can be entrapped, based on the total inner volume of the liposomal core ( Φ inner ) [ 59 , 60 ] ( Supplementary Materials Table S1 ).…”

Mixing-demixing transition and void formation in quasi-2D binary mixtures on a sphere

“…To check the influence of the system size on demixing, we simulated three systems characterized by different particle numbers (N p = 250, 500, 1000) and the same area fraction occupied by the particles φ = N p σ 2 AA 16R 2 s = 0.5, corresponding to a reduced density ρ * = 4φ π = 0.63. The choice of the system size has been made to ensure that the particle-to-sphere size ratio σ AA /2R s , ranging here from 0.044 to 0.089, was comparable to the bilayerto-vesicle size ratios encountered in small lipid vesicles 42 , the latter being ≈ 0.05. The attractive interaction between the confined particles (≤ 2k B T , see section III) and the energy scale (…”

“…Simulations including N AP = 1000 free bulk particles have been carried out only for mixtures with N p = 500. The choice of such an excess of bulk particles has been inspired by the experimental system recently investigated by the author and coworkers 42 in which lipid phase separation in mixed liposomes has been observed in excess of Isoniazide, one of the primary drugs used in the tuberculosis treatment. An investigation on the effect of bulk particle concentration, temperature and mixture composition are currently in progress and will be the subject of a future publication.…”

“…Passive transport through biomembranes and bilayer lipid membranes is in many cases controlled by existing small holes (or voids) within them 37,38 . There are several experimental evidences that proton, water and potentially drug permeability of mixed lipid membranes is enhanced by raft formation [39][40][41][42] , since inter-domain interfaces enhances ions and small molecules intrusion, and that membranes can be even destabilized by lipid substitution 39 or multivalent ions 43 . In addition to biological membranes, hole formation have been used to describe the rupture of bilayer (Newtonian) black foam films 44,45 , the evaporation of liquids through adsorbed monolayers 46 , as well as the thermodynamic equilibrium of monolayers on liquid surfaces 47 .…”