Abstract:Solid lipid nanoparticles (SLNs) have a crystalline lipid core which is stabilized by interfacial surfactants. SLNs are considered favorable candidates for drug delivery vehicles since their ability to store and release organic molecules can be tailored through the identity of the lipids and surfactants used. When stored, polymorphic transitions in the core of drug‐loaded SLNs lead to the premature release of drug molecules. Significant experimental studies have been conducted with the aim of investigating the… Show more
“…The Ligand Reader and Modeler on CHARMM‐GUI [ 34,41 ] was used to create the molecular model of triolein and cholesterol ester, which were then parameterized with the CHARMM General Force Field (CGenFF), [ 42–44 ] as was done previously for tripalmitin. [ 45 ] Finally, the interactions of BODIPY‐C12 was described by the same forcefield parameters as were used previously. [ 6 ] The Verlet cut‐off scheme was employed to generate the pair lists and the electrostatic interactions were calculated using the Particle‐Mesh Ewald algorithm.…”
Understanding viscosity in complex environments remains a largely unanswered question despite its importance in determining reaction rates in vivo. Here, time‐resolved fluorescence anisotropy imaging (TR‐FAIM) is combined with fluorescent molecular rotors (FMRs) to simultaneously determine two non‐equivalent viscosity‐related parameters in complex heterogeneous environments. The parameters, FMR rotational correlation time and lifetime, are extracted from fluorescence anisotropy decays, which in heterogeneous environments show dip‐and‐rise behavior due to multiple dye populations. Decays of this kind are found both in artificially constructed adiposomes and in live cell lipid droplet organelles. Molecular dynamics simulations are used to assign each population to nano‐environments within the lipid systems. The less viscous population corresponds to the state showing an average 25° tilt to the lipid membrane normal, and the more viscous population to the state showing an average 55° tilt. This combined experimental and simulation approach enables a comprehensive description of the FMR probe behavior within viscous nano‐environments in complex, biological systems.
“…The Ligand Reader and Modeler on CHARMM‐GUI [ 34,41 ] was used to create the molecular model of triolein and cholesterol ester, which were then parameterized with the CHARMM General Force Field (CGenFF), [ 42–44 ] as was done previously for tripalmitin. [ 45 ] Finally, the interactions of BODIPY‐C12 was described by the same forcefield parameters as were used previously. [ 6 ] The Verlet cut‐off scheme was employed to generate the pair lists and the electrostatic interactions were calculated using the Particle‐Mesh Ewald algorithm.…”
Understanding viscosity in complex environments remains a largely unanswered question despite its importance in determining reaction rates in vivo. Here, time‐resolved fluorescence anisotropy imaging (TR‐FAIM) is combined with fluorescent molecular rotors (FMRs) to simultaneously determine two non‐equivalent viscosity‐related parameters in complex heterogeneous environments. The parameters, FMR rotational correlation time and lifetime, are extracted from fluorescence anisotropy decays, which in heterogeneous environments show dip‐and‐rise behavior due to multiple dye populations. Decays of this kind are found both in artificially constructed adiposomes and in live cell lipid droplet organelles. Molecular dynamics simulations are used to assign each population to nano‐environments within the lipid systems. The less viscous population corresponds to the state showing an average 25° tilt to the lipid membrane normal, and the more viscous population to the state showing an average 55° tilt. This combined experimental and simulation approach enables a comprehensive description of the FMR probe behavior within viscous nano‐environments in complex, biological systems.
“…Nowadays, however, it is known that this is not necessarily true in all cases, since disc-like shape or flat ellipsoidal geometry have also been described (Mazuryk et al, 2016;Shah et al, 2019). Moreover, the loaded drug may be attached mostly to the carrier matrix surface instead of being embedded into the solid core (Pink et al, 2019;Shah et al, 2019).…”
Section: The Tiny Big Universe Of Lipid Nanoparticlesmentioning
confidence: 99%
“…The oils in NLC act by reducing the crystalline degree of the lipid core of SLN, thus avoiding the expulsion of the drug from the matrix and increasing the drug loading capacity and physical and chemical long-term stability (Müller et al, 2002). The highlyordered crystalline structure of the lipids in a SLN has been recently studied by Pink et al (2019) whose work provides a detailed description of the internal and external structure of SLN.…”
Section: The Tiny Big Universe Of Lipid Nanoparticlesmentioning
“…A silver complex of clotrimazole was synthesized, characterized, and further encapsulated into solid lipid nanoparticles to evaluate its antibacterial activity against SA and MRSA [ 21 , 22 ]. When firstly developed, SLN were presented as tiny and spherical particles, made of solid lipids at room temperature that may be thought as perfect crystal lipid matrices, able to accommodate a drug or other molecules between fatty acid chains [ 23 ]. SLN has stable properties and simple preparation.…”
Background. With the increasing resistance of antibiotics to bacteria, new and effective methods are needed to transform existing antibiotics to solve the problem of long development cycles for new drugs. The antibiotic nanodelivery system has proven to be a promising strategy. Aim. The purpose of this study is to synthesize penicillin solid lipid nanoparticles (penicillin SLNs) to enhance the antibacterial activity of penicillin against drug-resistant Staphylococcus aureus. Materials and Methods. Penicillin SLNs were synthesized. And particle size, the polydispersity index (PI), and zeta potential (ZP) of penicillin SLNs were measured. The surface morphology of penicillin SLNs was observed using a transmission electron microscope. Results. The particle size of penicillin SLNs is
112.3
±
11.9
nm
, the polydispersity index (PI) and zeta potential (ZP) of penicillin SLNs are
0.212
±
0.03
and
−
27.6
±
5.5
mV
. The encapsulation efficiency and drug loading were
98.31
±
1.2
%
and
4.98
±
0.05
(
%
w
/
w
), respectively. Penicillin SLNs had a more significant inhibitory effect on the growth of methicillin-sensitive Staphylococcus aureus (MSSA) after the drug and the bacteria were incubated for 12 hours. The number of MRSA colonies in the penicillin group increased after 12 hours, while the number of MRSA colonies in the penicillin SLNs group did not change significantly. Conclusion. Penicillin SLNs enhance the ability of penicillin to enter cells and increase the concentration of penicillin in the cell and also extend the residence time of penicillin in the cell. Our findings indicated that penicillin SLNs enhance the inhibitory effect of penicillin on drug-resistant Staphylococcus aureus.
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