Abstract
Lipid nanocarriers have a great potential for improving the physicochemical characteristics and behavior of poorly water-soluble drugs, such as aqueous dispersibility and oral bioavailability. This investigation presents a novel nanostructured lipid carrier (NLC) based on a mixture of solid lipid glycerides, fatty acid esters of PEG 1500 (Gelucire® 44/14), and an oil mix composed of capric and caprylic triglycerides (Miglyol® 812). These NLCs were developed by a simple low-energy method based on melt emulsification to yield highly encapsulating and narrowly distributed nanoparticles (~100 nm, PdI = 0.1, and zeta potential = ~−10 mV). Rhodamine 123 was selected as a poorly water-soluble drug model and owing to its spectroscopic properties. The novel NLCs were characterized by dynamic light scattering (DLS), zeta potential, nanoparticle tracking analysis (NTA), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and colloidal stability. The drug release was determined through a dialysis bag and vertical Franzs’ cells to provide insights about the methods’ suitability, revealing similar performance regardless of their different fluid dynamics. Rhodamine 123 followed a characteristic biphasic release profile owing to the swelling of the hydrophilic polymer coating and diffusion process from the lipid core as revealed by the Korsmeyers–Peppas kinetic modeling. Moreover, to elucidate the formation and incorporation of Rhodamine 123 into the NLC core, several molecular dynamics simulations were conducted. The temperature was shown to be an important condition to improve the formation of the nanoparticles. In addition, the liquid lipid incorporation to the formulation forms nanoparticles with imperfect centers, in contrast to nanoparticles without it. Moreover, Miglyol® 812 improves hydrophobic molecule solubility. These results suggest the potential of novel NLC as a drug delivery system for poorly water-soluble drugs.
Highlights
The membrane superficial area in dialysis bag and Franz’s cells was 1.38 cm2 and 0.63 cm2, respectively. Both experiments were performed at pH 7.4 for 72 h and the results show that the Rhodamine 123 (Rho) release at 25 ◦ C through dialysis bag and Franz’s cells were 33.7% and 42.5%, respectively (Figure 6a)
A nanostructured lipid carrier was successfully manufactured by a low-energy method and characterized by different methodologies
The hydrodynamic diameter of the formulation was stable at different pH, the Nanostructured Lipid Carriers (NLC) obtained can be an attractive candidate for oral pharmaceutical formulations
Summary
Pharmaceutics 2021, 13, 531 nanoparticles [5] The characteristics they give in pharmaceutical formulations to active molecules include enhanced solubility, increased storage stability, improved bioavailability and permeability, controlled release, and prolonged half-life, among others [6]. These advantages are related to the NLC components’ ratio because it comprises solid lipids, liquid lipids, and surfactants suspended in aqueous media. Franz diffusion cells have some limitations, such as low solution hydrodynamics, poor mixing, and temperature difference between donor and receptor compartments [10] Another critical parameter is the membrane type and MWCO because it could impact the results, since permeation kinetics may be related to the dialysis membrane porosity or the interactions between the drug molecules and membrane materials [11]. The molecular dynamics simulations were used to capture a wide variety of important biomolecular processes, including the NLC self-assembly processes
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
