The effect of a lipid composition and a surfactant on the characteristics of the solid lipid microspheres and nanospheres (SLM and SLN)

Sznitowska, Małgorzata; Wolska, Eliza; Baranska, Helena; Cal, Krzysztof; Pietkiewicz, Justyna

doi:10.1016/j.ejpb.2016.10.023

Cited by 32 publications

(33 citation statements)

References 30 publications

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“…They revealed that using nonionic hydrophilic surfactants such as Tween 80 leads to smaller particle sizes than nanoparticles prepared by other counterparts. Similar results were obtained by Sznitowska et al [39] and Soddu et al [40]. In the present study, by using Tween 80 and lecithin as surfactants, nanoparticles with less than 300 nm were obtained.…”

Section: Particle Size As Shown In Tablesupporting

confidence: 92%

Development of Perphenazine-Loaded Solid Lipid Nanoparticles: Statistical Optimization and Cytotoxicity Studies

Farsani

Mahjub

Mohammadi

et al. 2021

BioMed Research International

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Objective. Perphenazine (PPZ), as a typical antipsychotic medical substance, has the same effectiveness compared to atypical antipsychotic medications for the treatment of schizophrenia. Despite the lipophilic essence, PPZ encounters limited bioavailability caused by the first-pass metabolism following oral administration. In the present study, PPZ-containing solid lipid nanoparticles (PPZ-SLNs) were prepared and optimized based on different factors, including lipid and surfactant amount, to develop appropriate and safe novel oral dosage forms of PPZ. Methods. The solvent emulsification-evaporation method was utilized to form SLNs by using soybean lecithin, glycerol monostearate (GMS), and Tween 80. Statistical optimization was done by the Box-Behnken design method to achieve formulation with optimized particle size, entrapment efficiency, and zeta potential. Also, transmission electron microscopy, in vitro release behavior, differential scanning calorimetry (DSC), and powder X-ray diffractometry (P-XRD) studies and cytotoxicity studies were assessed. Results. Optimization exhibited the significant effect of various excipients on SLN characteristics. Our finding indicated that the mean particle size, zeta potential, and entrapment efficiency of optimized PPZ-SLN were, respectively, 104 ± 3.92 nm , − 28 ± 2.28 mV , and 83 % ± 1.29 . Drug release of PPZ-SLN was observed to be greater than 90% for 48 h that emphasized a sustained-release pattern. The DSC and P-XRD studies revealed the amorphous state of PPZ-SLN. FTIR spectra showed no incompatibility between the drug and the lipid. Performing cytotoxicity studies indicated no significant cytotoxicity on HT-29 cell culture. Conclusion. Our study suggests that PPZ-SLNs can make a promising vehicle for a suitable therapy of schizophrenia for the oral drug delivery system.

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Section: Particle Size As Shown In Tablesupporting

confidence: 92%

Development of Perphenazine-Loaded Solid Lipid Nanoparticles: Statistical Optimization and Cytotoxicity Studies

Farsani

Mahjub

Mohammadi

et al. 2021

BioMed Research International

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“…In this study, the radial distribution function for different pairs of molecule types were calculated in the simulated systems. Since it is not possible to present the calculated RDFs for all the simulated systems, only the calculated RDFs for ST70-OL30 system was presented as this ratio is one of the preferred solid to liquid ratios for NLCs according to the available studies on NLCs [9]. Fig.…”

Section: Radial Distribution Functionmentioning

confidence: 99%

“…Although it can be very efficient in protecting the chemically unstable compounds against degradation [5,6], there are also reported disadvantages associated with SLNs, including highly ordered recrystallization of the structure after cooling, which results in lower encapsulation, poor controlled release as well as physical instability [7,8]. Accordingly, nanostructured lipid carriers (NLC) with the coexistence of solid and liquid lipid matrix were developed to deal with these issues (with preferably solid to liquid ratio in the range of 70:30 up to 99.9:0.1) [9]. It was supposed that the existence of liquid lipid inside the nanoparticle would inhibit highly ordered recrystallization after the preparation process leading to an increased drug loading capacity and improved release profile [10].…”

Section: Introductionmentioning

confidence: 99%

Vesicle-like structure of lipid-based nanoparticles as drug delivery system revealed by molecular dynamics simulations

Khalkhali

Mohammadinejad

Khoeini

et al. 2019

International Journal of Pharmaceutics

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Lipid-based drug delivery systems are considered as promising vehicles for hydrophobic drug compounds. Lipid distribution within the droplet can affect drug loading capacity in these carriers. However, it is extremely challenging to determine the nanostructure within these carriers through the implementation of the direct experimental methods due to the ultrafine size. Therefore, coarse grained molecular dynamics (MD) simulation was utilized to model different kinds of lipid-based nanoparticles of the diameter about 12 nm including solid lipid nanoparticles (SLN), nanoemulsion (NE), and nanostructured lipid carriers (NLC), and the organization of the lipids within the carriers was explored. The aforementioned nanoparticles consisted of stearic acid, oleic acid as lipids, and sodium dodecyl sulfate (SDS) as a surfactant in water medium. Furthermore, the impact of solid to liquid mass ratio on the lipid distribution within the lipid matrix was investigated regarding the NLC simulations. In the equilibrium state, we observed the vesicle-like structure for all the investigated systems in which the hydrophilic moieties of the lipids and surfactant organized a semi-bilayer fold into the droplet and the hydrophobic tails accumulated among them. It is worth mentioning although SDS as a harsh surfactant, which is a special case, was expected to be present in the surface of the droplet, it penetrated into the lipids. Additionally, our results showed remarkable entrapped water beads inside the droplet in the form of one or more cavities along the internal layer of the head groups which was surrounded by lipid head groups. It was also reported that in the building structure of the nanoemulsion and SLN, in the central parts of the droplets, lipids were denser than the case of NLCs. Moreover, no crystallization occurred within the lipid-based carriers. Finally, the results indicated that, in the case of NLC simulations, the lipid distribution within the lipid matrix was insensitive to the mass fraction of solid to liquid lipids.

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“…Special attention should be paid to the characterization of the SLM by using various analytical tools. While the research on various types of lipid dispersions is based on commonly conducted studies of particle size distributions (laser diffraction method or dynamic light scattering), microscopic observations, pH or zeta potential [ 14 , 15 , 16 , 17 , 18 ], the choice of more advanced research techniques is less obvious. The utilization of modern high-resolution analytical techniques might provide an opportunity for an in-depth study of the changes and processes that occur in the SLM formulations during preparation and long-term storage.…”

Section: Introductionmentioning

confidence: 99%

Analytical Techniques for the Assessment of Drug-Lipid Interactions and the Active Substance Distribution in Liquid Dispersions of Solid Lipid Microparticles (SLM) Produced de novo and Reconstituted from Spray-Dried Powders

et al. 2020

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Solid lipid microparticles (SLM) can be presented as liquid suspension or spray-dried powder. The main challenge in SLM technology is to precisely determine the location of the active substance (API) in the different compartments of the formulation and its changes during SLM processing. Therefore, the purpose of the research was to assess the distribution of the API and to investigate the nature of the API-lipid interaction when the formulation was subjected to spray drying, with an indication of the most suitable techniques for this purpose. SLM were prepared with two various lipids (Compritol or stearic acid) and two model APIs: cyclosporine (0.1% and 1% w/w) and spironolactone (0.1% and 0.5% w/w). Physicochemical characterizations of the formulations, before and after spray drying, were performed by differential scanning calorimetry (DSC), atomic force microscopy (AFM), Raman spectroscopy and nuclear magnetic resonance (NMR). The API distribution between the SLM matrix, SLM surface and the aqueous phase was determined, and the release study was performed. It was demonstrated that, in general, the spray drying did not affect the drug release and drug distribution; however, some changes were observed in the SLM with Compritol and when the API concentration was lower. Only in the SLM with stearic acid was a change in the DSC curves noted. Measurements with the AFM technique proved to be a useful method for detecting differences in the surface properties between the placebo and API-loaded SLM, while the Raman spectroscopy did not show such evident differences.

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The effect of a lipid composition and a surfactant on the characteristics of the solid lipid microspheres and nanospheres (SLM and SLN)

Cited by 32 publications

References 30 publications

Development of Perphenazine-Loaded Solid Lipid Nanoparticles: Statistical Optimization and Cytotoxicity Studies

Development of Perphenazine-Loaded Solid Lipid Nanoparticles: Statistical Optimization and Cytotoxicity Studies

Vesicle-like structure of lipid-based nanoparticles as drug delivery system revealed by molecular dynamics simulations

Analytical Techniques for the Assessment of Drug-Lipid Interactions and the Active Substance Distribution in Liquid Dispersions of Solid Lipid Microparticles (SLM) Produced de novo and Reconstituted from Spray-Dried Powders

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