Showing papers on "Solid lipid nanoparticle published in 2003"
TL;DR: It seemed this modified method could prepare high quality SLNs loading lipophilic drugs, and it was suggested that the majority of the SLNs were less ordered arrangement of crystals, and this was favorable for increasing the drug loading capacity.
378 citations
TL;DR: Particle size of the solid lipid nanoparticles (SLN) was affected by using different emulsifiers and different lipid loads and an increase of the mean diameter from 205 to 695 nm and from 320 to 368nm was observed for the SLN prepared using benzyl alcohol and butyl lactate.
370 citations
TL;DR: The dependence of the occlusive effect on the particle size of SLN due to film formation is presented by in vitro data and an in vivo study showed that addition of 4% SLN to a conventional o/w cream lead to an increase of skin hydration of 31% after 4 weeks.
309 citations
TL;DR: The results indicated that these SLN dispersions and microemulsions could serve as efficient promoters for the TP penetrating into skin and the anti-inflammatory activity of SLN dispersion was stronger than that of microemulsion in carrageenan induced rat paw edema.
292 citations
TL;DR: Electron microscopic investigations reveal that, in both cases, the particles in the alpha-modification are less anisometric than those of the stable beta-form, indicating that major rearrangements still may take place in solid lipid nanoparticles after recrystallization.
183 citations
TL;DR: Experimental data let us conclude that NLCs are not spherical solid lipid particles with embedded liquid droplets, but they are rather solid platelets with oil present between the solid platelet and the surfactant layer.
Abstract: Purpose. Recently, colloidal dispersions made of mixtures from solid and liquid lipids have been described to combine controlled-release characteristics with higher drug-loading capacities than solid lipid nanoparticles (SLNs). It has been proposed that these nanostructured lipid carriers (NLCs) are composed of oily droplets that are embedded in a solid lipid matrix. The present work investigates the structure and performance of NLCs.
179 citations
TL;DR: AFM imaging revealed that the SLNs are protected by this layer against flattening on surfaces, and shown the ability to interact with bovine serum albumin (BSA), which forms a capping layer up to 17nm in depth.
82 citations
TL;DR: It is concluded that the biodegradable SLN stabilized with Tween 80 can potentially be used as drug carriers to the blood-brain barrier having a relatively long residence time in the blood stream.
Abstract: The plasma proteins adsorbing onto intravenously injected carriers are considered to be crucial factors determining the organ distribution. Plasma protein adsorption patterns were analyzed on solid lipid nanoparticles (SLN) stabilized with Tween 80 or stabilized with poloxamer 188. The binding patterns were determined by applying two different sample preparation methods, i.e. removal of the SLN from the plasma by (a) centrifugation and (b) gel filtration to assess, if the separation method has an effect on the patterns obtained. The Tween 80-modified SLN adsorbed the major plasma proteins known from particles with blood-brain barrier specificity. Poloxamer 188-surface modified SLN adsorbed the proteins known from model particles that exhibit prolonged circulation time in the blood. It is concluded that the biodegradable SLN stabilized with Tween 80 can potentially be used as drug carriers to the blood-brain barrier having a relatively long residence time in the blood stream. For the poloxamer 188-stabilized SLN a relatively long resistance time in the blood is predicted leading to potential accumulation in the bone marrow when looking at the distinct CII/CIII adsorption.
77 citations
TL;DR: Notably the particle size of the solid lipid microparticle formulations only affected the biological activity slightly and the emulsifiable concentrate formulation had about the same insecticidal activity on both Dysdercus cingulatus nymphs and Spodoptera littoralis larvae.
74 citations
TL;DR: All carbohydrates tested showed excellent cryoprotection and redispersion properties with the calixarene based SLNs.
65 citations
Patent•
28 Jan 2003TL;DR: In this paper, a pharmaceutical composition consisting of a low-solubility drug and a concentrationenhancing polymer and a lipophilic micro-phase-forming material is presented. But the formulation is different from ours.
Abstract: A pharmaceutical composition comprises a solid amorphous dispersion comprising a low-solubility drug and a concentration-enhancing polymer and a lipophilic microphase-forming material. Alternatively, a solid amorphous dispersion comprising a low-solubility drug and a concentration-enhancing polymer is co-administered with a lipophilic microphase-forming material to an in vivo use environment.
TL;DR: Contact mode atomic force microscopy has been carried out on gels of four current polymers containing dispersions of solid lipid nanoparticles of amphiphilic calixarenes, showing the presence of nanoparticles in the sub-surface region and that the SLNs affect the local mechanical properties of the gels.
TL;DR: In SLN dispersions, it was estimated that the ratio of SP between solid lipid core, phospholipid layers, and water is for Tempol 0:0:100, and the experimentally obtained partition coefficients increase in the order Tempol < MeFASL < C(14)-Tempo, showing the same trend as the partition coefficients calculated according to Rekker.
TL;DR: 5-FuS-SLN has significant liver targeting properties and seems to be an alternative strategy to the traditional colloidal delivery system, according to the preparation method presented.
Abstract: To enhance the liver targeting and reduce the side effects of 5-fluorouracil (5-Fu), it was acylated by stearyl chloride to obtain N1-stearyl-5-Fu (5-FuS). The chemical structure of the prodrug was confirmed by Nuclear Magnetic Resonance and Infrared Spectrometry. 5-FuS was incorporated into solid lipid nanoparticles (SLN), which were prepared by the physical agglomeration method. The mean diameter of 5-FuS-SLN was 240.19 nm and the drug loading was 20.53%. The release characteristics in vitro of 5-FuS-SLN were fitted to the first-order pharmacokinetic model. Compared with 5-Fu injection, a study on the distribution of 5-FuS-SLN in mice showed that 5-FuS-SLN could double 5-Fu concentration in mice livers. The main pharmacokinetic parameters of 5-FuS-SLN in rabbits is shown as follows: Vd=0.04336 L/kg, T(1/2) beta=1.2834 h, CL=0.1632 L/h. In conclusion, 5-FuS-SLN has significant liver targeting properties. The employment of a prodrug to enhance drug liposoluble properties and the preparation method presented in this paper, seem to be an alternative strategy to the traditional colloidal delivery system.
TL;DR: Both the hydrophobic chain length and the nature of the polar head-groups on the amphiphilic calix-arene derived Solid LipidNanoparticles have been investigated and no haemolyticeffects are observed.
Abstract: The haemolytic effects of a series of amphiphilic calix-arene derived Solid LipidNanoparticles (SLNs) have been measured on human erythrocytes. The effectsof both the hydrophobic chain length and the nature of the polar head-groups on theamphiphilic calix[4]arene have been investigated. For all systems, no haemolyticeffects are observed.
Patent•
31 Oct 2003
TL;DR: In this paper, solid lipid nanoparticles (SLNs) with a mean diameter between 50 and 400 nm were used for topical ocular administration and for systemic administration. But the authors did not consider the use of a pharmacologically active substance for ophthalmic treatment.
Abstract: Pharmaceutical compositions for the treatment of ophthalmic diseases, suitable for topical ocular administration and for systemic administration, comprising solid lipid nanoparticles (SLNs) with a mean diameter comprised between 50 and 400 nm wherein, within said nanoparticles, a pharmacologically active substance for the specific ophthalmic treatment is incorporated.
Patent•
13 Jun 2003TL;DR: In this article, solid lipid nanoparticle compositions containing 1 to 40% by weight of an oil-soluble UV absorber, 20 to 98.9% of a solid lipid, 0.1 to 20% of an emulsifier, and 0.
Abstract: Solid lipid nanoparticle compositions containing
(a) 1 to 40% by weight of an oil-soluble UV absorber, (b) 20 to 98.9% by weight of a solid lipid, (c) 0.1 to 20% by weight of an emulsifier and (d) 0 to 40% by weight of a liquid lipid or a liquid oil-miscible UV absorber The compositions according to the invention enhance the solubility behaviour of oil-soluble UV filters in cosmetic formulations and thereby also improve their effectiveness.
TL;DR: The development of solid lipid nanoparticles (SLN) as colloidal carriers for cloricromene suggests that this colloidal system could be useful for targeted drug delivery to the central nervous system after intravenous administration.
Abstract: This article describes the development of solid lipid nanoparticles (SLN) as colloidal carriers for cloricromene. Nanoparticles were prepared by the microemulsion or precipitation technique. In vitro drug release profile from SLN was studied under various experimental conditions mimicking some body fluids. The drug release rate of drug at pH 7.4 and human plasma is high. In plasma, after 15 min, about 70% of drug was released. The cloricromene that was not released within 4 hr was found in the SLN. This result suggests that this colloidal system could be useful for targeted drug delivery to the central nervous system after intravenous administration.
Journal Article•
TL;DR: Particle size distribution data indicate that by optimizing the homogenization process and formulation parameters it is possible to produce SLN within a desired size range as required for carrier mediated drug targeting.
Abstract: This work deals with the formulation and development of Solid Lipid Nanoparticles (SLN) using pressure homogenization technique, nimesulide being used as the model drug. Main emphasis of the work was to study the effect of individual process parameters (homogenization pressure and homogenization cycles) and formulation parameters (lipid concentration and surfactant concentration) on particle size distribution and drug loading. Particle size distribution data indicate that by optimizing the homogenization process and formulation parameters it is possible to produce SLN within a desired size range as required for carrier mediated drug targeting. Approaches to improve drug loading efficiency indicate that drug loading was higher in case of SLN prepared from glyceryl beheanate, palmitostearate and glyceryl tristearate + span 60 as compared to monoacid triglyceride (MAT) tristearate. Thermal analysis by differential scanning calorimetry of the drug loaded SLN indicates the solid nature of the lipid carrier as required for sustained drug release.
Journal Article•
TL;DR: Microemulsion technique can be used to prepare solid lipid nanoparticles and the device temperature, water temperature, and delivery rate were the key factors that influence the preparation process of SLN, and Tw was extremely important.
Abstract: AIM To prepare solid lipid nanoparticles by microemulsion technique. METHODS Stearic acid was used as the oil phase, lecithin as surfactant, alcohol as cosurfactant and distilled water as the aqueous phase. Microemulsion was prepared by mixing the above component in proper ratio. The corresponding pseudoternary phase diagram monitored Microemulsion formation field of different lecithin/alcohol. Solid lipid nanoparticles (SLN) were prepared by dispersing warm microemulsion in cold water under magnetic stirring. Then appropriate microemulsions that can contain more water phase and suitable oil phase were selected to prepare SLN. The influence of formulation, process variables on the preparation and quality of SLN were studied. Based on the investigation of single factors, orthogonal design was used to optimize SLN formulation and preparation process, and more, the reproducibility of the optimized results were studied. RESULTS The results showed that the device temperature (Ti), water temperature (Tw), and delivery rate (Rd) were the key factors that influence the preparation process of SLN, and Tw was extremely important. The ratio of microemulsion formulation, the ratio of microemulsion and distilled water had also influence on its quality. CONCLUSION Microemulsion technique can be used to prepare solid lipid nanoparticles.
01 Jan 2003
TL;DR: In this article, the entrapment ratio, structural properties, quality and the release of AZM-SLN in vitro were investigated using transmission electron microscopy (TEM).
Abstract: Objcetive:To prepare solid l ip id nanoparticles containing AZM with stearic acid,and investigate the character istic of AZM solid lipid nanoparticles(AZM-SLN)in vitro release.Methods:AZM-SLN was prepared by the method of emulsion evaporation-solidification at low temperature,and its morphology and particle size were examined by transmission electron microscope.Entrapment ratio,structural properties,quality and the r elease of AZM in vitro were studied.Results:The AZM-SLN as-sumed spherical s hape.Its distribution of particle diameter was even,with an average particle s ize of(17.75±5.00)nm.The entrapment ratio was(81.57±1.3 3)%.The in vitro release of AZM-SLN conformed to Higuchi Equation.The for mation of a new material phase was testified by analysis of differential scannin g calorimetry(DSC).Conclusion:Stearic acid solid lipid nanoparticles might be a novel drug delivery carrier.
TL;DR: The Px-SLN might be a promising candidate for an alternative formulation for the parenteral delivery of paclitaxel in order to formulate a new delivery system suitable for intravenous administration without toxic excipients.
Abstract: Many studies have been attempted to overcome the problems of paclitaxel related to the extremely low aqueous solubility of paclitaxel and the unexpected side-effects caused by EL in a commercial paclitaxel formulation, . In order to formulate a new delivery system suitable for intravenous administration without toxic excipients, in this study, paclitaxel was incorporated into solid lipid nanoparticles (Px-SLN) by hot homogenization technique using a microfluidizer. Particle size and zeta potential were measured by a Zetasizer. In vitro drug release experiment was performed by a dialysis diffusion method. Each Px-SLN or was intravenously administered to the male Sprague-Dawley rats at a dose of 5 mg/kg as paclitaxel. Blood samples were deproteinated with acetonitrile and assayed for paclitaxel by the validated HPLC/MS/MS method. Mean particle size and zeta potential were measured as 72.1 nm (. The of Px-SLN was 3.4-fold greater than that of . The Px-SLN might be a promising candidate for an alternative formulation for the parenteral delivery of paclitaxel.
Journal Article•
TL;DR: Solid lipid nanoparticle as topical transdermal delivery system may play a role to control drug release, increase drug effects and decrease side effects.
Abstract: OBJECTIVE To study the preparation of triptolide loaded solid lipid nanoparticle for transdermal delivery and its anti inflammatory activity.METHODS Triptolide loaded solid lipid nanoparticle was prepared by hot melting dispersion technique.The transdermal delivery effects of different TP SLN formulations were assessed by an in vitro permeation technique using modified Franz diffusion cells.The anti inflammatory activity for complete Freund's adjuvant (CFA) induced arthritis was investigated in rats.RESULTS Stable SLN systems were obtained by different lipids,emulsifiers and co emulsifiers.The smallest particle size was ( 123.4 ±1.9) nm.The cumulative transdermal absorption fraction during 12h of the formulation B was 78.5%,whereas that of the conventional solution was 32.4%.In addition,the smaller the particle size was,the stronger the anti inflammotory activity was.CONCLUSION Solid lipid nanoparticle as topical transdermal delivery system may play a role to control drug release,increase drug effects and decrease side effects.
Patent•
31 Oct 2003
TL;DR: In this article, solid lipid nanoparticles (SLNs) with a mean diameter between 50 and 400 nm were used for topical ocular administration and for systemic administration. But the authors did not consider the use of a pharmacologically active substance for ophthalmic treatment.
Abstract: Pharmaceutical compositions for the treatment of ophthalmic diseases, suitable for topical ocular administration and for systemic administration, comprising solid lipid nanoparticles (SLNs) with a mean diameter comprised between 50 and 400 nm wherein, within said nanoparticles, a pharmacologically active substance for the specific ophthalmic treatment is incorporated.