Showing papers on "Solid lipid nanoparticle published in 2004"
TL;DR: The biological activity of parenterally applied SLN and biopharmaceutical aspects such as pharmacokinetic profiles as well as toxicity aspects are reviewed.
1,302 citations
TL;DR: The use of nanoparticulate carriers, developed in the research group, are described as one solution to overcome drug-associated delivery problems, i.e. drug nanocrystals, solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and lipid-drug conjugate (LDC) nanoparticles.
741 citations
TL;DR: The obtained results demonstrate the use of these lipid nanoparticles as modified release formulations for lipophilic drugs over a period of 10 h, and the entrapment efficiency was higher than 50%.
582 citations
TL;DR: DSC and PXRD analysis showed that clozapine is dispersed in SLN in an amorphous state and the release pattern of drug is analyzed and found to follow Weibull and Higuchi equations.
518 citations
TL;DR: The investigated SLN appear as thin platelets with oil spots sticking on the surface and very short diffusion pathways in platelets, increased water-lipid interfaces and low drug incorporation in crystalline lipids are the drawback of SLN and NLC compared to conventional nanoemulsions.
422 citations
TL;DR: By employing an oscillation frequency sweep test, significant differences in elastic response of SLN and NLC aqueous dispersions could be observed and it could be demonstrated that physical properties of the dispersed lipid phase have a great impact on the rheological Properties of the prepared semisolid formulations.
198 citations
TL;DR: The development and characterize of a solid lipid nanoparticle (SLN) system containing an anionic polymer for the delivery of cationic antineoplastic agents and chemosensitizers laid the foundation for a "one-bullet" dosage form that may provide convenient and effective delivery of multiple drug treatment of tumors.
167 citations
TL;DR: The results demonstrate the principle suitability of SLN as a prolonged release formulation for hydrophilic peptide drugs and a novel preparation method in the present research for peptide-loaded SLN was established.
159 citations
TL;DR: Preliminary in vitro results suggest that SLN could be proposed as alternative drug delivery system for conventional drug formulations and exerted a greater-than-additive antiproliferative effect at 24 h exposure.
158 citations
TL;DR: Electric dipole movements in the broad field of a frequency span from 0.1 to 100 MHz demonstrate that glucocorticoids are attached to the particle surface but are not incorporated into the lipid matrix, demonstrating that an adequate association of drug and carrier is essential for epidermal targeting.
139 citations
TL;DR: Results indicate that well tolerated and highly efficient in vitro transfection could be achieved with SLN whenever selecting good combinations of two-tailed cationic lipids and matrix lipids.
TL;DR: Strengths and weaknesses of the lipid assemblies, in particular solid lipid nanoparticles, in promoting drug delivery by the oral route for systemic or Peyer's patch uptake will be highlighted, and possible future research pathways will be suggested.
Abstract: Of all the methods employed by formulators when presented with the task of improving oral bioavailability, the use of lipid assemblies is perhaps the least understood. Nonetheless, lipid-based formulations, and in particular solid lipid nanoparticles (SLN), show great promise for enhancing the oral bioavailability of some of the most poorly absorbed compounds. The physical/chemical characteristics of lipid-based systems are highly complex because of the existence of a variety of lipid assembly morphologies, the morphology-dependent solubility of drug, the interconversion of assembly morphology as a function of time and chemical structure, and the simultaneous lipid digestion. The present work will center on recent studies of the relevant physicochemical characteristics of SLN, most notably solubility of the drug in the lipid matrix, location of the drug in the aggregate, drug release properties of the aggregate, and particle size stability. Strengths and weaknesses of the lipid assemblies, in particular solid lipid nanoparticles, in promoting drug delivery by the oral route for systemic or Peyer's patch uptake will be highlighted, and possible future research pathways will be suggested.
TL;DR: In this article, the differences and similarities in structure and performance between solid lipid nanoparticles and liposomes were investigated, and the results showed that cationic lipid composition was more dominant for in vitro transfection performance than the kind of colloidal structure it is arranged in.
TL;DR: The structure of loaded solid lipid nanoparticles (SLN) has been studied to elucidate the incorporation of coenzyme Q10 and indicates two different fractions of the active ingredient: whereas the majority of the coen enzyme Q10 is found to be homogeneously mixed with the solid lipid, the residual amount clearly forms a separate, solid phase associated to the particles.
Abstract: Purpose. The structure of loaded solid lipid nanoparticles (SLN) has been studied to elucidate the incorporation of coenzyme Q10.
Journal Article•
TL;DR: New and upcoming developments such as nanosuspensions and solid lipid nanoparticles are highlighted, which may enable new possibilities for therapy that presently have not been investigated.
Abstract: Over the years, controlled drug delivery as well as site-specific delivery have made considerable advances. One area that contributed significantly to this progress is the rapidly developing field of colloidal drug delivery systems. Nanoparticles, one of the colloidal drug delivery systems, may enable new possibilities for therapy that presently have not been investigated. Recent advances in nanoparticle research are discussed here. The present review highlights new and upcoming developments such as nanosuspensions and solid lipid nanoparticles.
Journal Article•
TL;DR: It was found that 1.5% TegoCare 450 was the most effective stabilizer for the Witepsol E85 SLN dispersion compared to Tween 80, Tyloxapol and Pluronic F68 according to the data obtained from differential scanning calorimetry (DSC), zeta potential (ZP) measurements and particle size analysis.
Abstract: The choice of surfactant or surfactant mixtures at suitable concentrations contributes to the stability of solid lipid nanoparticles (SLN). In this study, it was found that 1.5% TegoCare 450 was the most effective stabilizer for the Witepsol E85 SLN dispersion compared to Tween 80, Tyloxapol and Pluronic F68 according to the data obtained from differential scanning calorimetry (DSC), zeta potential (ZP) measurements and particle size analysis.
Journal Article•
TL;DR: FR-targeted solid-lipid nanoparticles incorporating the lipophilic drug HpSa were capable of specific receptor binding in cultured KB cells, which warrants further investigation.
Abstract: Purpose: This study was aimed at the synthesis, formulation and in vitro evaluation of folate receptor (FR)- targeted solid-lipid nanoparticles (SLNs) as a carrier for a lipophilic derivative of the photosensitizer hematoporphyrin (Hp), in FR-overexpressing tumor cells. Materials and Methods: FR-targeted hematoporphyrin-stearylamine (HpSa) SLN composed of Triolein:Egg-phosphatidylcholine (EPC):Tween-80 (T-80) (64:25:10), with 0.5 mole % of folatepolyethyleneglycol- cholesterol (FPC) or polyethyleneglycoldistearoylphosphatidylethanolamine (PEG-DSPE), were prepared by ethanol injection method. Stability of the SLN was monitored by changes in particle size at 4°C and drug retention at various time points. Cellular uptake and IC50 values of the FR-targeted formulations were determined in vitro in the FR (+) KB cells. Results: Stable targeted SLNs were prepared by ethanol injection encapsulating greater than 95 percent of 5 mole % of HpSa, having a mean diameter < 200 nm. In vitro cytotoxicity assay on the FR-targeted SLN gave IC50 of 1.57 μM in KB cells and non-targeted SLNs gave an IC50 of 5.17 μM. FR selectivity was confirmed by fluorescence microscopy. Conclusion: FR-targeted SLNs incorporating the lipophilic drug HpSa were capable of specific receptor binding in cultured KB cells, which warrants further investigation.
TL;DR: A significant increase in dispersion viscosity was found in the triglyceride sequence trimyristin < tripalmitin < tristearin, which can be clearly attributed to an increase in particle shape anisometry with increasing length of the lipid's fatty acid chains.
01 Jan 2004
TL;DR: Parallel alignment of tripalmitin nanoplatelets is a completely reversible and concentration-dependent effect that can be attributed to the overlap of the exclusion volumes of the anisometric particles.
Abstract: Purpose. The effect of spontaneous particle self-assembly into stack-like structures occurring in dispersions of melt-homogenized tripalmitin nanocrystals (solid lipid nanoparticles; SLNs) was studied in dependence of lipid concentration, stabilizer type, stabilizer concentration, and particle size.
Journal Article•
TL;DR: The suitability of SLN produced with the proposed method as a prolonged release formulation for lipophilic drugs is demonstrated, with nearly 4% of the drug being released each day.
Abstract: Solid lipid nanoparticles were prepared by a novel solvent diffusion method in an aqueous system. The lipophilic model drug cyclosporin A was incorporated into SLN to study encapsulation efficiency, zeta potential (charge) and drug delivery. Stearylamine and cyclosporin A were dissolved in ethanol and acetone and the resultant organic solution was dropped into water at 60 degrees C. The drug-loaded SLN suspension quickly formed with an azury color. After burst drug release with 18% of the drug over the first 12 hours, a distinctly prolonged release over a monitored period of 16 days was observed, with nearly 4% of the drug being released each day. These results demonstrate the suitability of SLN produced with the proposed method as a prolonged release formulation for lipophilic drugs.
30 Jun 2004
TL;DR: In this article, the particle size of solid lipid nanoparticles (SLN) were measured using photon correlation spectroscopy and laser diffraction and the results showed that the diameter of SLN were influenced by lipid matrix and surfactant nature as well as their concentrations.
Abstract: Solid lipid nanoparticles (SLN) have gained increasing attention as a colloidal drug carrier system, particularly for lipophilic drugs, because SLN combine the advantages of polymeric nanoparticles, fat emulsions, and liposomes but avoiding their disadvantages. Solid lipid nanoparticles are composed of high melting point lipid as a solid core coated by surfactants. The solid core allows the prolonged and controlled release of drugs and may protect incorporated drugs against chemical degradation. Lipid and surfactant nature are important in drug loading capacity, also affect size distribution and physical stability. In this study SLN were prepared by using different ratios of lipid/surfactant. The lipid nanopellets were produced by using the high speed homogenizer and by high pressure homogenizer. The particle size measurements were carried out using the photoncorrelation spectroscopy and laser diffraction. The results showed that the diameter of SLN were influenced by lipid matrix and surfactant nature as well as their concentrations. Particle size diameter was decreased as a function of surfactant concentration till it reach a certain limit after which it has no effect. Methods of preparation showed a potential effect on the presence of large particles and on the polydispersity index. In conclusion, physical characteristics of SLN are not only influenced by variation in process parameters but also by chemical nature of the used surfactant and lipid matrix that have a potential influence on the particle size distribution of SLN.
29 Nov 2004
Patent•
06 Oct 2004
TL;DR: In this paper, a solid lipid nanoparticle is characterized by containing lipophilic lipid and amphiphilic lipid, and having a particle size of 500nm, preferably 100nm or less.
Abstract: PURPOSE: Provided are a solid lipid nanoparticle containing lipophilic lipid and amphiphilic lipid and having a particle size of 500nm, preferably 100nm or less, a pharmaceutical composition containing the solid lipid nanoparticle for delivering the active substance and a preparing method thereof. CONSTITUTION: The solid lipid nanoparticle is characterized by containing lipophilic lipid and amphiphilic lipid and having a particle size of 500nm, preferably 100nm or less, wherein the lipophilic lipid is hard fat or wax having a melting point of 40 deg.C, and the amphiphilic lipid is polyethyleneglycol(PEG) bound hard fat or wax having a melting point of 40 deg.C. The pharmaceutical composition contains 20 wt.% of lipophilic lipid, amphiphilic lipid, water insoluble substance and dispersant, based on the total weight of the composition.
Journal Article•
TL;DR: In this paper, the main factor affecting solid lipid nanopaticals containing volatile oil of Lignum Dalbergia odoriferae quality in the preparation technics was researched by the single factor exploration and orthogonal design.
Abstract: Objective To prepare solid lipid nanoparticals containing volatile oil of Lignum Dalbergia odoriferae by the high pressure homoenizer mothod and hot-dispersion technique respectively.Method The main factor affecting solid lipid nanopaticals containing volatile oil of Lignum Dalbergia odoriferae quality in the preparation technics was researched by the single factor exploration and orthogonal design.The satisfactory formulation was selected.Results The results revealing the nanoparticles were spherelike with the mean size of 40.0 nm and 34.5 nm,the content of dispersion was 72.1% and 71.54%.Entrapment efficiency of nanoparticles was 91.27% and 92.36%.Conclusion The hot-dispersion technique on the preparation of solid lipid nanoparticles containning volatile oil of Lignum Dalbergia odoriferae has great practical use.
Journal Article•
TL;DR: The present work describes the performance of nanoparticulate delivery systems in skin care, and solid lipid nanoparticles (SLN), ethosomes and cubosomes are presented as innovative carrier systems alternative to liposomes.
Abstract: The present work describes the performance of nanoparticulate delivery systems in skin care. In particular solid lipid nanoparticles (SLN), ethosomes and cubosomes are presented as innovative carrier systems alternative to liposomes. Skin care studies performed by the use of SLN indicate an increase in skin hydration and a reduction in wrinkle depth, moreover it has been demonstrated that SLN can improve uptake of cosmetic agents. Concerning ethosomes, their soft structure enables facilitated delivery of the incorporated active agent into the skin lipid bilayers. Specifically, the major potential of ethosomes in promoting penetration through skin with respect to liposomes is ascribed to an interaction between ethosomes and skin lipids. Cubic liquid crystalline materials are an active research topic because their unique structure lends itself well to controlled release and skin care applications. Cubosomes usually have been produced by means of time-consuming methods involving high energy input. Conversely we have recently tested more conventional dispersion techniques demonstrating that the emulsification of monoglyceride/surfactant mixtures in water results in the formation of aqueous dispersions composed of large lipid particles (28 % w/w) and cubosomes characterized by spheroidal shape, few aggregates, mean diameter of 193.5 nm, and high percentage of recovery (88% w/w). Organoleptic and morphological features of cubosomes do not change by time, appearing free from phase-separation phenomena for almost 1 year from production. Photon Correlation Spectroscopy studies showed that cubosomes undergo an initial increase in mean diameter within the first month following production; afterwards they generally maintain their dimensions for the next 6 months.
Journal Article•
TL;DR: The technique of preparing baicalin solid lipid nanoparticles by film-ultrasonic wave dissolving technique is feasible and the products had good size distributions.
Abstract: Objective: To optimize technique of preparing baicalin solid lipid nanoparticles (BC-SLN) by film-ultrasonic wave dissolving techniques. Methods: The influence of various factors, including the dosage of baicalin, stearic acid, lecithin and tween 80 on the entrapment efficiency were investigated. And the optimum formula was selected through orthogonal design test. Results: 20 mg baicalin, 90 mg stearic acid, 90 mg lecithin and 10 ml tween-80 (2.5%) for the technique. The products had good size distributions. The mean particle size diameter was 289.3 nm, and the average entrapment efficiency was 67.17%. Conclusion: The technique of preparing BC-SLN by film-ultrasonic wave dissolving technique is feasible.
01 Jan 2004
Journal Article•
TL;DR: In this article, an emulsion evaporation-solidification at low temperature was used to prepare the stearic acid solid lipid nanoparticles (SLN) containing oridonin and its morphology and particle size were examined by transmission electron microscope.
Abstract: OBJECTIVE To prepare the oridonin solid lipid nanoparticles with stearic acid, and investigate their quality and characteristics. METHODS The method of emulsion evaporation-solidification at low temperature was used to prepare the stearic acid solid lipid nanoparticles (SLN) containing oridonin. Its morphology and particle size were examined by transmission electron microscope. Entrapment efficiency, zeta potential, structural properties quality and the release of oridonin in vitro were studied. RESULTS The oridonin-SLN assumed spherical shape.Its distribution of diameter was even with average particle size (22.22±15.5)nm. The zeta potential was - 45.07 mV. Entrapment efficiency was (44.83±1.504) % . The release of oridonin in vitro conformed to Higuchi Equation. The formation of a new material phase was testified by analysis of differential scanning calorimetry (DSC) and X-ray scattering. CONCLUSION Oridonin loaded stearic acid solid lipid nanoparticles were produced with stable physical properties.