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[Display omitted] The oral administration of therapeutic peptides and proteins is favoured from a patient and commercial point of view. In order to reach the systemic circulation after oral administration, these drugs have to overcome numerous barriers including the enzymatic, sulfhydryl, mucus and epithelial barrier. The development of oral formulations for therapeutic peptides and proteins is therefore necessary. Among the most promising formulation approaches are lipid-based nanocarriers such as oil-in-water nanoemulsions, self-emulsifying drug delivery systems (SEDDS), solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), liposomes and micelles. As the lipophilic character of therapeutic peptides and proteins can be tremendously increased such as by the formation of hydrophobic ion pairs (HIP) with hydrophobic counter ions, they can be incorporated in the lipophilic phase of these carriers. Since gastrointestinal (GI) peptidases as well as sulfhydryl compounds such as glutathione and dietary proteins are too hydrophilic to enter the lipophilic phase of these carriers, the incorporated therapeutic peptide or protein is protected towards enzymatic degradation as well as unintended thiol/disulfide exchange reactions. Stability of lipid-based nanocarriers towards lipases can be provided by the use to excipients that are not or just poorly degraded by these enzymes. Nanocarriers with a size <200 nm and a mucoinert surface such as PEG or zwitterionic surfaces exhibit high mucus permeating properties. Having reached the underlying absorption membrane, lipid-based nanocarriers enable paracellular and lymphatic drug uptake, induce endocytosis and transcytosis or simply fuse with the cell membrane releasing their payload into the systemic circulation. Numerous in vivo studies provide evidence for the potential of these delivery systems. Within this review we provide an overview about the different barriers for oral peptide and protein delivery, highlight the progress made on lipid-based nanocarriers in order to overcome them and discuss strengths and weaknesses of these delivery systems in comparison to other technologies. [ABSTRACT FROM AUTHOR]

Abstract: Although less specific proteases have been established in proteomics, resulting peptides are often disadvantaged in mass spectrometric analysis compared to tryptic peptides. This is due to the high number of theoretically possible peptides as well as their relatively inefficient ionization and fragmentation. One possibility to improve the performance of less specific digests is to employ amine reactive, basic labels such as tandem mass tags (TMT) for the N-terminal derivatization of peptides. This study uses elastase and thermolysin digestion of cytosolic extracts with and without the use of TMT labeling for analysis via nanoflow high-performance liquid chromatography (nLC) coupled to an electrospray ionization quadrupole orthogonal acceleration time-of-flight (ESI-QoTOF) mass spectrometer. Differences between tryptic and less specific digests and their behavior during chromatographic separation and tandem mass spectrometric (MS/MS) analysis are highlighted. Furthermore, this work shows how the tandem mass spectrometric analysis of less specific digests can be optimized with reference to peptide ionization and fragmentation. The effect of TMT labeling on the number and characteristics of identified peptides as well as peptide fragmentation behavior is examined. Taking all these factors into consideration, this work constitutes an optimized strategy for the analysis of less specific digests via nLC–ESI-QoTOF-MS/MS. [Copyright &y& Elsevier]

Abstract: Chemically modified tetracyclines (CMTs) have been reported to strongly inhibit proliferation and metastasis of various cancers, but their efficacy is restricted by poor water solubility. In the present study, a hydrophilic 4-dedimethylamino sancycline (CMT-3) loaded nanostructured lipid carrier (CMT-3/NLC) was produced by high pressure homogenization (HPH). The physical properties of CMT-3/NLC formulations were characterized by dynamic light scattering (DLS), high efficiency liquid chromatography (HPLC), atomic force microscopy (AFM), scanning electron microscopy (SEM), small-angle neutron scattering (SANS), small-angle X-ray scattering (SAXS) and wide-angle X-ray powder diffraction (XRD). The lipid and surfactant ingredients, as well as drug/lipid concentrations (m/m) were optimized to produce stable and sustained NLC formulations. In vitro cytotoxicity of CMT-3/NLC against HeLa cells was evaluated by MTT assay. The diameter of CMT-3/NLC was found to increase from 153.1±3.0nm to a maximum of 168.5±2.0nm after 30 days of storage, while the entrapment efficiency remained constant at >90%. CMT-3/NLC demonstrated a burst-sustained release profile in release media with different pH, a property attributed to the 3-dimensional structure of CMT-3/NLC. Cell uptake and localization studies indicated that NLC reached the cytoplasm and could thereby facilitate CMT-3 entry into HeLa cells. [Copyright &y& Elsevier]

Abstract: Coenzyme Q10 (CoQ10) acts as an antioxidant in the skin and is frequently contained in anti-aging products. In previous studies, it could be shown that nano-structured lipid carriers (NLC) with a size of about 230nm are beneficial for the dermal delivery of CoQ10. They increased Q10 skin penetration when compared to equally sized nanoemulsion. In this study, ultra-small NLC were prepared with even smaller mean particles sizes of around 80nm. The influence of this decrease of particle size was investigated in terms of skin permeation and penetration as well as physicochemical stability of the NLC. Improved dermal delivery of CoQ10 by ultra-small NLC could be achieved. [Copyright &y& Elsevier]

Nowadays solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) have been investigated as carrier systems for many applications. SLNs consist of pure solid lipids, while NLCs are made of a solid matrix that entraps liquid lipid nano-compartments. These systems revealed several advantages compared to other colloidal carrier systems. They provide a controlled drug release and an increase in chemical stability of the incorporated drugs. Moreover, they are safe carriers which can be produced easily in a large scale. This paper reviews the commonly used materials, production techniques, characterization, and physical stability of these systems. [ABSTRACT FROM AUTHOR]

This study was performed to develop solid lipid nanoparticles of water soluble drug ciprofloxacin HCl using quick solvent diffusion evaporation technique (ouzo effect). A statistical central composite rotatable design was used to study the effect of independent variables. In the subsequent step, optimized SLN were further compared with nanostructured lipid carriers and nanoemulsion for particle size, zeta potential, drug entrapment, drug release, and stability. Comparative study revealed that the drug encapsulation efficiencies were enhanced by adding the Capmul MCM C8 into the solid lipid nanoparticles. The in vitro drug release study of all three formulations showed rapid release for nanoemulsion while controlled release for SLN. Stability study of all the formulation proved that nanostructured lipid carrier and SLN could prevent the drug expulsion during the storage period. Results of the study suggested that the SLN and nanostructured lipid carriers produced by the principle of ouzo effect could potentially be exploited for better drug entrapment efficiency and controlled drug release of water soluble actives. [ABSTRACT FROM PUBLISHER]

Auditory detection is essential for survival and reproduction of vertebrates, yet the genetic changes underlying the evolution and diversity of hearing are poorly documented. Recent discoveries concerning prestin, which is responsible for cochlear amplification by electromotility, provide an opportunity to redress this situation. We identify prestin genes from the genomes of 14 vertebrates, including three fishes, one amphibian, one lizard, one bird, and eight mammals. An evolutionary analysis of these sequences and 34 previously known prestin genes reveals for the first time that this hearing gene was under positive selection in the most recent common ancestor (MRCA) of tetrapods. This discovery might document the genetic basis of enhanced high sound sensibility in tetrapods. An investigation of the adaptive gain and evolution of electromotility, an important evolutionary innovation for the highest hearing ability of mammals, detects evidence for positive selections on the MRCA of mammals, therians, and placentals, respectively. It is suggested that electromotility determined by prestin might initially appear in the MRCA of mammals, and its functional improvements might occur in the MRCA of therian and placental mammals. Our patch clamp experiments further support this hypothesis, revealing the functional divergence of voltage-dependent nonlinear capacitance of prestin from platypus, opossum, and gerbil. Moreover, structure-based cdocking analyses detect positively selected amino acids in the MRCA of placental mammals that are key residues in sulfate anion transport. This study provides new insights into the adaptation and functional diversity of hearing sensitivity in vertebrates by evolutionary and functional analysis of the hearing gene prestin. [ABSTRACT FROM PUBLISHER]

Nanostructured lipid carriers (NLC) have gained high interest as enhancing drug delivery systems via topical application during the last few years. NLC can enhance stability of many active substances against environmental stress. The extremely small size of NLC plays an important role in skin penetration. The unchanged size of NLC upon storage indicates its physical stability. The aim of this work was to investigate the effect of surfactant type on physical properties and stability of lycopene-loaded NLC. The preparation of the NLC was achieved by means of high pressure homogenization. The results indicate that different types of surfactant yield NLC with different properties. We also explored the effect of contact angle on the size of the NLC. It was found that the small contact angle gave NLC with small size. Among two small contact angle surfactants, Plantacare 1200 gave lycopene-loaded NLC with smaller size, higher zeta potential and narrower size distribution. The particle size, size distribution, and zeta potential of lycopene-loaded NLC prepared with Plantacare 1200 was unchanged during 30 days of storage. It was concluded that Plantacare 1200 is the most suitable surfactant for lycopene-loaded NLC. The chemical stability of lycopene entrapped in the NLC was significantly enhanced. [ABSTRACT FROM AUTHOR]

A major obstacle to the application of nanostructured lipid carriers (NLCs) as carriers for hydrophilic drugs is the limited loading capacity (LC) and encapsulation efficiency (EE) of NLCs for these molecules. The purpose of this research was to design and implement a strategy to enhance the LC and EE of NLCs for the hydrophilic drug, didanosine (DDI). DDI was dispersed in Transcutol® HP and the particle size of DDI in the liquid lipid was reduced gradually using hot high pressure homogenization (HPH). The product obtained thereafter was added to Precirol® ATO 5 and the hot mixture was immediately dried using liquid nitrogen. The dried materials were then ground and passed through a 200 μm sieve and the solid lipid particles were dispersed in a surfactant solution and subsequently used to manufacture DDI-loaded NLCs using cold HPH. The LC and EE of NLCs for DDI manufactured using the new strategy were 3.39 ± 0.63% and 51.58 ± 1.31%, respectively, compared to 0.079 ± 0.001% and 32.45 ± 0.08%, respectively, obtained when DDI-loaded NLCs were produced using conventional hot HPH. The enhanced LC and EE for DDI make NLCs a potential technology for the oral administration of DDI to paediatric patients. [ABSTRACT FROM AUTHOR]

Abstract: Different types of extraction protocols are described for identifying proteins in seed and pulp of olive (Olea europea), by employing both conventional extraction methods and capture with ProteoMiner as well as with in house-made combinatorial peptide ligand libraries (HM-CPLLs) at pH 7.4 and at pH 2.2. Thanks to the use of CPLLs, able to dramatically amplify the signal of low-abundance species, a quite large number of compounds has been indeed identified: 61 in the seed (vs. only four reported in current literature) and 231 in the pulp (vs. 56 described so far), the deepest investigation up to the present of the olive proteome. In the seed, it highlights the presence of seed storage proteins, oleosins and histones. In the pulp, the allergenic thaumatin-like protein (Ole e 13) was confirmed, among the other 231, as the most abundant protein in the olive pulp. The present research has also been undertaken with the aim of identifying proteins in olive oil and ascertaining the relative contribution of seed and pulp proteins in their presence, if any, in oils. [Copyright &y& Elsevier]

Abstract: Various nanometer scaled transport systems are used in pharmaceutics and cosmetics to increase penetration or storage of actives. Nanostructured lipid carriers (NLCs) are efficient drug delivery systems for dermatological applications. Electron paramagnetic resonance (EPR) spectroscopy was used for the determination of TEMPO (2,2,6,6-tetramethyl-1-piperidinyloxy) distribution within the carrier and to investigate the dynamics of skin penetration. Results of ex vivo penetration of porcine skin and in vivo data – forearm of human volunteers – are compared and discussed to previously obtained results with invasomes under comparable conditions. W-band measurements show 35% of TEMPO associated with the lipid compartments of the NLC. Application of TEMPO loaded NLC to skin ex vivo increases the observation time by 12min showing a stabilisation of the nitroxide radical. Moreover, stabilisation is also seen with data generated in vivo. Thus, same as invasomes NLCs are a suitable slow release depot system. [Copyright &y& Elsevier]

Abstract: The main travelling wave linacs of the compact linear collider (CLIC) operate at a frequency of 11.9942GHz with a phase advance per cell of 2π/3. In order to minimise the overall footprint of the accelerator, large accelerating gradients are sought. The present baseline design for the main linacs of CLIC demands an average electric field of 100MV/m. To achieve this in practical cavities entails the dual challenges of minimising the potential for electrical breakdown and ensuring the beam excited wakefield is sufficiently suppressed. We present a design to meet both of these conditions, together with a description of the structure, CLIC_DDS_A, expressively designed to experimentally test the ability of the structure to cope with high powers. [Copyright &y& Elsevier]

The preferential in vitro adsorption of apolipoprotein E (Apo E) onto the surface of colloidal drug carriers may be used as a strategy to evaluate the in vivo potential for such systems to transport drugs to the brain. The aim of this research was to investigate the in vitro protein adsorption patterns of didanosine-loaded nanostructured lipid carriers (DDI-NLCs), using two-dimensional polyacrylamide gel electrophoresis (2-D PAGE), in order to establish the potential for NLCs to deliver DDI to the brain. NLC formulations were manufactured using high-pressure homogenization using a lipid matrix consisting of a mixture of Precirol®® ATO 5 and Transcutol®® HP. The 2-D PAGE analysis revealed that NLCs in formulations stabilized using Solutol®® HS 15 alone or with a ternary surfactant system consisting of Solutol®® HS 15, Tween®® 80, and Lutrol®® F68, preferentially adsorbed proteins, such as Apo E. Particles stabilized with Tween®® 80 and Lutrol®® F68 did not adsorb Apo E in these studies, which could be related to the relatively large particle size and hence small surface area observed for these NLCs. These findings have revealed that DDI-loaded NLCs may have the potential to deliver DDI to the brain in vivo and, in addition, to Tween®® 80, which has already been shown to have the ability to facilitate the targeting of colloidal drug delivery systems to the brain. Solutol®® HS 15--stabilized nanoparticles may also achieve a similar purpose. [ABSTRACT FROM AUTHOR]

Abstract: Noctilucent clouds and polar mesospheric summer echoes are both manifestations of ice particles near the summer polar mesopause. These ice particles are believed to form mainly on pre-existing ice condensation nuclei. The characteristics and especially the concentrations of such nuclei have been considered important factors in determining ice properties. More ice condensation nuclei would, given the limited amount of water vapor, yield more but smaller ice particles, and thus a dimmer noctilucent cloud. However, here it is shown that the sensitivity of observable ice properties to condensation nuclei concentration is much less than one would expect from the simple situation described above. In particular, both ice mass and cloud brightness is close to independent of condensation nuclei concentration. The reason for this lack of sensitivity is further examined. [Copyright &y& Elsevier]

Abstract: The two polyhydroxy surfactants polyglycerol 6-distearate (Plurol®Stearique WL1009 – (PS)) and caprylyl/capryl glucoside (Plantacare® 810 – (PL)) are a class of PEG-free stabilizers, made from renewable resources. They were investigated for stabilization of aqueous solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC) dispersions. Production was performed by high pressure homogenization, analysis by photon correlation spectroscopy (PCS), laser diffraction (LD), zeta potential measurements and differential scanning calorimetry (DSC). Particles were made from Cutina CP as solid lipid only (SLN) and its blends with Miglyol 812 (NLC, the blends containing increasing amounts of oil from 20% to 60%). The obtained particle sizes were identical for both surfactants, about 200nm with polydispersity indices below 0.20 (PCS), and unimodal size distribution (LD). All dispersions with both surfactants were physically stable for 3 months at room temperature, but Plantacare (PL) showing a superior stability. The melting behaviour and crystallinity of bulk lipids/lipid blends were compared to the nanoparticles. Both were lower for the nanoparticles. The crystallinity of dispersions stabilized with PS was higher, the zeta potential decreased with storage time associated with this higher crystallinity, and leading to a few, but negligible larger particles. The lower crystallinity particles stabilized with PL remained unchanged in zeta potential (about −50mV) and in size. These data show that surfactants have a distinct influence on the particle matrix struture (and related stability and drug loading), to which too little attention was given by now. Despite being from the same surfactant class, the differences on the structure are pronounced. They are attributed to the hydrophobic–lipophilic tail structure with one-point anchoring in the interface (PL), and the loop conformation of PS with two hydrophobic anchor points, i.e. their molecular structure and its interaction with the matrix surface and matrix bulk. Analysis of the effects of the surfactants on the particle matrix structure could potentially be used to further optimization of stability, drug loading and may be drug release. [Copyright &y& Elsevier]

Purpose: Nanostructured lipid carriers were loaded with testosterone undecanoate (TU), which has a low oral bioavailability. Methods: Different NLC dispersions were produced using the hot high pressure homogenization method. Particles were characterized using dynamic and static light scattering techniques, differential scanning calorimetry and X-ray diffraction. And the bioavailability was compared to a marketed product. Results: Nanostructured lipid carriers with up to 30% TU load and sizes of about 600 and 200 nm could be achieved, allowing a direct comparison of the size effect in in vivo bioavailability studies. The zeta potentials varied between − 20 and − 40 mV. The bioavailability of Andriol Testocaps® in the fed state was matched. Conclusions: This opens the perspective of administering a single dose of dose of TU in one oral dosage unit and simultaneously having a bioavailability less dependent on the fed state. [ABSTRACT FROM AUTHOR]

liquid crystal optical device made of an optically anisotropic heterostructure is considered. The device consists of a cholesteric liquid crystal (CLC) layer sandwiched by two phase-shifting anisotropic layers of a nematic liquid crystal (NLC). In this structure each of the NLC layers is a quarterwave plate. The problem is solved both by Ambartsumian’s method of layer addition and Muller’s matrix method. The peculiarities of reflection spectra, eigen polarizations, rotation of polarization plane and polarization ellipticity are studied. It is shown that this device can work as a light modulator or a system for obtaining linearly polarized light with electrically tunable rotation of the polarization plane (which is especially important for optical communication), as well as a device for obtaining the linearly polarized light from a non-polarized one. [ABSTRACT FROM AUTHOR]

Abstract: Due to their positive features (e.g., increased penetration of actives, re-enforcement of the lipid barrier and increase in skin hydration), nanostructured lipid carriers (NLC) are used in many dermal formulations. These formulations require preservation, and preservatives can impair the physical stability of disperse systems. Therefore, in this study, the influence of preservatives on the physical stability of Q10-loaded NLC was investigated using 11 different preservative mixtures. Whereas for nanosuspensions, only a limited number of preservatives are known from the literature not affecting their physical stability, a surprisingly high number of seven preservatives could be identified to be suitable for the preservation of NLC dispersions. For Q10-loaded NLC, Hydrolite 5 proved to be the best preservative, as it was found surprisingly to stabilize the NLC dispersion. Based on the data, a preservative classification system is suggested and a mechanistic model describing six key parameters affecting the physical stability of NLC could be developed. As most suitable characterization method to screen for suitable preservatives, light microscopy was identified. By being a simple, fast and cost efficient method, even extensive preservative screening studies can be performed very efficiently. [ABSTRACT FROM AUTHOR]

Abstract: The purpose of this study was to develop a novel nanostructured lipid carrier (NLC) for the intravitreal-targeting delivery of triamcinolone acetonide (TA) by direct ocular instillation. A five-level central composite rotable design was used to study the influence of four different variables on the physicochemical characteristics of NLCs. The analysis of variance (ANOVA) statistical test was used to assess the optimization of NLC production parameters. The systems were produced by high pressure homogenization using Precirol®ATO5 and Squalene® as solid and liquid lipids respectively, and Lutrol®F68 as surfactant. Homogenization at 600bar for 3 cycles of the optimized formulation resulted in the production of small NLC (mean diameter<200nm) with a homogeneous particle size distribution (polydispersity index (PI)∼0.1), of negatively charged surface (∼|45|mV) and high entrapment efficiency (∼95%). Surface morphology was assessed by SEM which revealed fairly spherical shape. DSC, WAXS and FT-IR analyses confirmed that TA was mostly entrapped into the NLC, characterized by an amorphous matrix. In vivo Draize test showed no signs of ocular toxicity. [Copyright &y& Elsevier]

Abstract: The aim of this study was to develop nanostructured lipid carriers (NLC) for topical delivery of fluticasone propionate (FP) with the aim to further improve the safety profile and decrease the adverse-side effects commonly reported in topical corticotherapy. NLC are colloidal drug-carriers consisting of a blend of a solid lipid and a small amount of liquid lipid since these carriers have proved to be effective in epidermal targeting in particular of glucocorticoids. NLC consisting of glyceryl palmito-stearate, and PEG-containing medium chain triglycerides mixture, stabilised by polysorbate 80 and soybean phosphatidylcholine were prepared. A mean particle size between 380 and 408nm and entrapment efficacy of 95% were obtained for FP-loaded NLC. The crystallinity and polymorphic phase behaviour of FP-free and FP-loaded NLC were examined by differential scanning calorimetry and wide angle X-ray diffraction. Results revealed a low-crystalline structure and confirmed the incorporation of FP into the particles. The suitability of PEG-containing liquid lipids to form the lipid matrix of NLC was also confirmed. [Copyright &y& Elsevier]

Abstract: Condensed water particles are known to exist in the high latitude upper mesosphere during the summer months. However, the mechanism or mechanisms through which they nucleate remains uncertain. It is postulated here that particles of amorphous solid water (ASW, condensed water with a non-crystalline structure) may nucleate homogeneously in the summer mesosphere. Using classical nucleation theory and a one-dimensional model, it is shown that more than 105 cm−3 amorphous solid water particles can nucleate homogeneously under mesopause conditions. Furthermore, it is shown that homogeneous nucleation competes with heterogeneous nucleation on meteoric smoke particles when the cooling rate is >0.5K/h. The homogeneous nucleation of amorphous solid water could provide an explanation for the high density of ice particles (many thousands per cm3) thought to be required for electron depletions in the upper mesosphere. A parameterisation for homogeneous nucleation is presented which can be used in other mesospheric cloud models. [Copyright &y& Elsevier]

Abstract: In this study, nanoemulsions (NE) of medium chain triacylglycerols (MCT) and nanostructured lipid carriers (NLC) of cetyl palmiate/MCT were produced to load coenzyme Q10 (Q10) and characterized for their stability before and after incorporation into xanthan gum hydrogels. After storage at 4, 25 and 40°C, the particles remained in the nanosize range for 12 months, with zeta potential higher than |40mV|. Similar results were found in xanthan gum-based hydrogels containing NE or NLC. The crystallinity index of Q10-loaded NLC increased after being incorporated into hydrogels. The Q10 entrapped in NLC and NE remained higher than 90% at all temperatures for 12 months but dramatically decreased when exposed to light. From the rheological studies, both NLC and NE dispersions possessed pseudoplastic flow having more liquid characteristics, whereas NLC and NE hydrogels exhibited plastic flow with thixothopy, showing more elastic rather than viscous properties. The occurrence of a spatial arrangement of lipid molecules was observed in the matrix of NLC when entrapped into hydrogels. From in vitro permeation studies, it could be stated that the amount of Q10 released and occlusiveness were major keys to promote the deep penetration of Q10 into the skin. [Copyright &y& Elsevier]

This review highlights the application of lipid nanoparticles (Solid Lipid Nanoparticles, Nanostructured Lipid Carriers, or Lipid Drug Conjugates) as effective drug carriers for pathologies affecting the posterior ocular segment. Eye anatomy and the most relevant diseases affecting the posterior segment will be summarized. Moreover, preparation methods and different types and subtypes of lipid nanoparticles will also be reviewed. Lipid nanoparticles used as carriers to deliver drugs to the posterior eye segment as well as their administration routes, pharmaceutical forms and ocular distribution will be discussed emphasizing the different targeting strategies most recently employed for ocular drug delivery. [ABSTRACT FROM AUTHOR]

Solid lipid nanoparticles (SLN®), nanostructured lipid carriers (NLC®), and lipid-drug conjugates (LDC®), commonly produced by high-pressure homogenization, are interesting vectors for oral delivery of lipophilic and, to a certain extent, hydrophilic substances. Their production can be done without the use of organic solvents. Techniques to make them a physically stable delivery system have been developed. Scaling up of the production process from lab-size to large-scale dimensions using high-pressure homogenization can be easily achieved by using a different type of homogenizer. The machines used for large-scale production often yield an even better product quality than the lab-scale types. This review article covers the methods of production, characterization, mechanisms of oral bioavailability enhancement, scale-up, final oral dosage forms, and regulatory aspects of lipid nanoparticles for oral drug delivery. It focuses mainly on high-pressure homogenization production methods. [ABSTRACT FROM AUTHOR]

The aim of the investigation is to develop solid lipid nanoparticles (SLN) and nano-structured lipid carrier (NLC) as carriers for topical delivery of nitrendipine (NDP). NDP-loaded SLN and NLC were prepared by hot homogenization technique followed by sonication, and they were characterized for particle size, zeta potential, entrapment efficiency, stability, and in vitro release profiles. Also the percutaneous permeation of NDPSLN A, NDPSLN B, and NDPNLC were investigated in abdominal rat skin using modified Franz diffusion cells. The steady state flux, permeation coefficient, and lag time of NDP were estimated over 24 h and compared with that of control (NDP solution). The particle size was analyzed by photon correlation spectroscopy (PCS) using Malvern zeta sizer, which shows that the NDPSLN A, NDPSLN B, and NDPNLC were in the range of 124-300 nm during 90 days of storage at room temperature. For all the tested formulations (NDPSLN A, NDPSLN B, and NDPNLC), the entrapment efficiency was higher than 75% after 90 days of storage. The cumulative percentage of drug release at 24 h was found to be 26.21, 30.81, and 37.52 for NDPSLN A, NDPSLN B, and NDPNLC, respectively. The results obtained from in vitro release profiles also indicated the use of these lipid nanoparticles as modified release formulations for lipophilic drug over a period of 24 h. The data obtained from in vitro release from NDPSLN A, NDPSLN B, and NDPNLC were fitted to various kinetic models. High correlation was obtained in Higuchi and Weibull model. The release pattern of drug is analyzed and found to follow Weibull and Higuchi equations. The permeation profiles were obtained for all formulations: NDPSLN A, NDPSLN B, and NDPNLC. Of all the three formulations, NDPNLC provided the greatest enhancement for NDP flux (21.485 ± 2.82 μg/h/cm2), which was fourfold over control (4.881 ± 0.96 μg/h/cm2). The flux obtained with NDPSLN B (16.983 ± 2.91 μg/h/cm2) and NDPNLC (21.485 ± 2.82 μg/h/cm2) meets the required flux (16.85 μg/h/cm2). [ABSTRACT FROM AUTHOR]

Abstract: Dermal therapy is still a challenge due to the difficulties in controlling the active pharmaceutical ingredient (API) fate within the skin. Recently, lipid nanoparticles have shown a great potential as vehicle for topical administration of active substances, principally owing to the possible targeting effect and controlled release in different skin strata. Ketoprofen and naproxen loaded lipid nanoparticles were prepared, using hot high pressure homogenization and ultrasonication techniques, and characterized by means of photo correlation spectroscopy and differential scanning calorimetry. Nanoparticle behavior on human skin was assessed, in vitro, to determine drug percutaneous absorption (Franz cell method) and, in vivo, to establish the active localization (tape-stripping technique) and the controlled release abilities (UVB-induced erythema model). Results demonstrated that the particles were able to reduce drug penetration increasing, simultaneously, the permeation and the accumulation in the horny layer. A prolonged anti-inflammatory effect was observed in the case of drug loaded nanoparticles with respect to the drug solution. Direct as well as indirect evidences corroborate the early reports on the usefulness of lipid nanoparticles as carriers for topical administration, stimulating new and deeper investigations in the field. [Copyright &y& Elsevier]

Abstract: The aims of this study were to investigate the effect of the oil content on the physicochemical properties of NLC and to elucidate the potential of NLC for skin targeting. The obtained results showed that an increase in the oil content did not affect the mean particle size of NLC but impacted on the zeta potential. The inner structure of NLC was influenced by the increasing proportion of oil towards the less ordered structure as confirmed by differential scanning calorimetry (DSC) and X-ray diffraction (XRD), particularly for the higher medium chain triglycerides (MCT) loading. The data from proton nuclear magnetic resonance (1H NMR) revealed that cetyl palmitate nanoparticles did not completely recrystallize after cooling down to room temperature. 1H NMR and DSC results indicate that MCT molecules were restricted in the NLC as compared to the nanoemulsions (NE). Nile red distribution and penetration into skin from NLC were pronounced as compared to NE and dependent on the MCT loading. The deep penetration and high amount of Nile red were related to the occlusion factor. Moreover, the epidermal targeting was achieved by NLC applications, particularly those containing 5% MCT (NLC-5) depending on the amount of MCT loading. [Copyright &y& Elsevier]

Synopsis A detailed review of the literature is presented in attempts to emphasize several advantages of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) for cosmetic applications. Examples of several actives are given and the main features of the solid core of SLN and NLC for topical delivery of cosmetics are discussed. Lipid nanoparticles have been more and more explored in pharmaceutical technology, showing superior advantages for topical purposes over conventional colloidal carriers. [ABSTRACT FROM AUTHOR]

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Abstract: Noctilucent clouds (NLC) and polar mesospheric summer echoes (PMSE) are phenomena that occur in the summertime polar regions due to the presence of ice particles around the mesopause. That ice particles are able to form in a region with such low water vapour concentration as the mesopause is noteworthy. Even though the summer mesopause is the coldest region on Earth, temperatures are generally not low enough for homogeneous nucleation to occur, which necessitates the presence of pre-existing condensation nuclei. The nature of these nuclei has long puzzled the scientific community and many candidates have been suggested, such as particles of meteoric origin, ion clusters, sodium bi-carbonate, sulfate aerosols and soot particles. Out of these the so-called “smoke particles”, i.e. particles re-condensed from ablated meteoritic material, have long been considered the most likely. Generally, it has been believed that these particles exist in numbers of the order of thousands per cubic centimetre at the mesopause. This belief is based on 1-dimensional studies of meteoric material. A recent 2-dimensional model study, which includes the atmospheric circulation from summer to winter pole however, suggests much lower number densities at the summer mesopause. We here investigate the implications of low number densities for the formation of ice particles. We find that even though resulting ice particle distribution may produce typical NLC brightness, the number density of ice particles is not consistent with what is expected for NLC and PMSE. In particular, it is much lower than the ice particle concentration (>1000cm−3) typically expected to explain the “electron bite-outs” that are frequently observed in the vicinity of PMSE’s. We therefore re-examine the assumptions and parameters that determine the smoke distribution. We show that even though the number of condensation nuclei at the polar summer mesopause can be increased within the uncertainties, the results in most scenarios remain insufficient. We show that charged particles, perhaps in combination with significant deviations from the mean mesospheric state, may be necessary for condensation of ice particles in the polar summer mesosphere. Hence, we raise the question whether the conventional ideas of nucleation on meteoric smoke, which are used in current mesospheric ice models, are correct. [Copyright &y& Elsevier]

Transparent electrodes are indispensable for most of the flat panel display as liquid crystal display (LCD). We investigated liquid crystal (LC) aligning capabilities and electro-optical (EO) characteristics of transparent electrodes as Al-doped ZnO (ZnO:Al) substituting indium tin oxide (ITO). The experiment results show that a uniform vertical LC alignment on ZnO:Al electrodes based on a rubbed polyimide (PI) surface were achieved. A high pretilt angle of about 88° was obtained. EO performances of the VA-LCD on rubbed PI surfaces with ZnO:Al is almost the same as that of the VA-LCD with ITO electrodes. These results appeared that ZnO:Al electrodes as transparent electrodes of LCDs could substitute ITO electrodes. [ABSTRACT FROM AUTHOR]

Abstract: Noctilucent clouds (NLC) have been observed by a Rayleigh/Mie/Raman (RMR) lidar in Northern Norway (69N,16E) capable to measure the aerosol backscatter coefficients at three wavelengths (355nm, 532nm, 1064nm) and since 1998 also under sunlight conditions. For strong noctilucent cloud events the three backscatter coefficients are used to calculate the parameters of a monomodal particle distribution describing the observed optical properties. We deduce the radius of the particle size distribution, the width, and the average number density of the particle ensemble. To minimize the smearing by a changing structure of the noctilucent clouds we use the lowest possible time and altitude resolutions, which are 14 and 150min, respectively. Using this, the vertical structure of the particle properties below and above the peak is investigated. From a statistical comparison of the observed ratios of backscatter coefficients we find that under the assumption of spherical particles the lognormal distribution describes the optical properties of NLC above ALOMAR better than the Gaussian distribution. If the optical analysis is extended to aspherical particles then both Gaussian and lognormal distribution can sufficiently describe the optical properties when the axis ratio of the particles is allowed to vary from 1/10 to 10. Using the traditional optical model but the new data inversion method on the summer 1998 NLC data leads to the same results found by von Cossart et al. [von Cossart, G., Fiedler, J., von Zahn, U. Size distributions of NLC particles as determined from 3-colour observations of NLC by ground-based lidar, Geophys. Res. Lett., 26 (11), 1513–1516. doi: 10.1029/1999GL900226, 1999]. Using the new optical model we find that independent of the assumed particle shape the average size of strong NLCs above ALOMAR in 2005 is 47±3nm for spheroids or cylinders with Gaussian distribution while it is 54±3nm for the same particles but assuming a lognormal size distribution. The distribution widths are s =16±1nm or σ =1.25±0.03 for Gaussian or lognormal distribution while the particle number-density is N =120cm−3 for both cases. This comparison shows that the combination of three widely separated wavelengths used in backscatter geometry allows a robust measurement of the particle size. We recommend performing the sensitivity test of the deduced particle properties on the particle shape also for other optical instruments sounding the NLC particle sizes. [Copyright &y& Elsevier]

Abstract: In the present study, nanostructured lipid carriers (NLC) composed of cetyl palmitate with various amounts of caprylic/capric triacylglycerols (as liquid lipid) were prepared and Coenzyme Q10 (Q10) has been incorporated in such carriers due to its high lipophilic character. A nanoemulsion composed solely of liquid lipid was prepared for comparison studies. By photon correlation spectroscopy a mean particle size in the range of 180–240nm with a narrow polydispersity index (PI) lower than 0.2 was obtained for all developed formulations. The entrapment efficiency was 100% in all cases. The increase of oil loading did not affect the mean particle size of NLC formulations. NLC and nanoemulsion, stabilized by the same emulsifier, showed zeta potential values in the range −40/−50mV providing a good physical stability of the formulations. Scanning electron microscopy studies revealed NLC of disc-like shape. With respect to lipid polymorphism, a decrease in the ordered structure of NLC was observed with the increase of both oil and Q10 loadings, allowing therefore high accommodation for Q10 within the NLC. Using static Franz diffusion cells, the in vitro release studies demonstrated that Q10-loaded NLC possessed a biphasic release pattern, in comparison to Q10-loaded nanoemulsions comprising similar composition of which a nearly constant release was observed. The NLC release patterns were defined by an initial fast release in comparison to the release of NE followed by a prolonged release, which was dependent on the oil content. [Copyright &y& Elsevier]

Abstract: Enhancement of the chemical stability of ascorbyl palmitate (AP) after incorporation into nanostructured lipid carriers (NLC) has been reported. However, the formulation parameters of AP-loaded NLC have not been completely investigated. Moreover, the long-term chemical stability of AP in any colloidal systems has not been yet achieved. Therefore, in this study the formulation parameters affecting the stability of AP after incorporation into NLC were evaluated including types of lipids, types of surfactants, storage conditions, i.e. temperature and nitrogen gas flushing, the effects of drug loading as well as types of antioxidants. After storage for 90 days, the mean particle size analyzed by photon correlation spectroscopy (PCS) was lower than 350nm. The zeta potential measured by the Zetasizer IV was higher than −30mV in all developed AP-loaded NLC formulations which varied according to the types of lipid and surfactant. Concerning the chemical stability of AP, it was found that AP-loaded NLC prepared and stored in non-degassing conditions, a higher percentage of AP loading in NLC, lower storage temperature (4°C), addition of antioxidants as well as selection of suitable surfactants and solid lipids improved the chemical stability of AP. Moreover, an improvement of long-term chemical stability of AP was achieved by addition of antioxidants with nitrogen gas flushing as compared to those without antioxidant. The percentage of drug remaining at both 4°C and room temperature (25°C) was higher than 85% during 90 days of storage. [Copyright &y& Elsevier]

Abstract: The first generation of lipid nanoparticles was introduced as solid lipid nanoparticles (SLN), the second, improved generation as nanostructured lipid carriers (NLC). Identical to the liposomes, the lipid nanoparticles (NLC) appeared as products first on the cosmetic market. The article gives an overview of the cosmetic benefits of lipid nanoparticles, that means enhancement of chemical stability of actives, film formation, controlled occlusion, skin hydration, enhanced skin bioavailability and physical stability of the lipid nanoparticles as topical formulations. NLC are on the market as concentrates to be used as cosmetic excipients, special formulation challenges for these products are discussed. NLC appeared also in a number of finished cosmetic products world-wide. An overview of these products is provided including their special effects due to the lipid nanoparticles, lipids used for their production and incorporated cosmetic actives. [Copyright &y& Elsevier]

Abstract: The present review discusses the potential use of solid lipid nanoparticles for brain drug targeting purposes. The state of the art on surfactant-coated poly(alkylcyanoacrylate) nanoparticles specifically designed for brain targeting is given by emphasizing the transfer of this technology to solid lipid matrices. The available literature on solid lipid nanoparticles and related carriers for brain drug targeting is revised as well. The potential advantages of the use of solid lipid nanoparticles over polymeric nanoparticles are accounted on the bases of a lower cytotoxicity, higher drug loading capacity, and best production scalability. Solid lipid nanoparticles physicochemical characteristics are also particularly regarded in order to address the critical issues related to the development of suitable brain targeting formulations. A critical consideration on the potential application of such technology as related to the current status of brain drug development is also given. [Copyright &y& Elsevier]

We studied liquid crystal (LC) alignment with ion beam (IB) on polyimide and electro-optical characteristics of twisted nematic (TN)-liquid crystal display (LCD) on the polyimide surface using obliquely ion beam (IB) exposure with new IB type equipment (DuoPIGatron type ion gun). A good uniform alignment of the nematic liquid crystal (NLC) alignment with the ion beam exposure on the polyimide surface was observed. In addition, it can be achieved the good EO properties of the ion-beam-aligned TN-LCD on polyimide surface. Also the EO characteristics of the ion-beam-aligned TN-LCD on a polyimide (PI) surface with ion beam exposure using new type IB equipment is almost the same as that of ion-beam-aligned TN-LCD on a polyimide (PI) surface with ion beam exposure using Kaufman-type Ar ion gun. [ABSTRACT FROM AUTHOR]

Abstract: From June 29 to July 6 2003, the German-Norwegian ROMA-SvalRak campaign (ROMA=Rocket borne Observations in the Middle Atmosphere) took place at the SvalRak rocket range, Ny-Ålesund (78.9°N, 11.9°E; Spitzbergen). The main scientific aim of this campaign was to study polar mesosphere summer echoes (PMSE) and mesospheric turbulence. During this campaign a total of three instrumented sounding rockets was launched. In addition, ground based observations with a VHF radar and a potassium lidar at Longyearbyen complemented the in situ measurements. All three sounding rockets were equipped with the CONE (COmbined sensor for Neutrals and Electrons) instrument to measure small scale structure of neutral air and electron density, and neutral temperature. The PIP (positive ion probe) instrument was used to measure small scale structure of the positive ion density. Furthermore, two cold plasma probes were flown to measure electron temperature, and a particle detector was employed to detect signatures of charged aerosols. During the first launch, an electric field experiment was also incorporated, while during the other two launches, Faraday rotation experiments yielded absolute electron number densities. During all three rocket flights a PMSE was observed by the VHF radar, whereas the potassium lidar detected a noctilucent cloud (NLC) only during the second launch. Signatures of charged particles forming the PMSE and NLC layers were recorded by the onboard particle detectors. [Copyright &y& Elsevier]

Compritol®888 ATO (glycerol behenate) is widely used as a pharmaceutical excipient in the field of solid dosage forms due to its lubricating properties. It is an amphiphilic material with a high melting point (&nvsim;70°C) and, therefore, it can also be used to prepare aqueous colloidal dispersions. The aim of this paper is to study the suitability of Compritol®888 ATO for the production of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) for the entrapment of a lipophilic model drug. This study assesses the crystalline structure of the bulk lipid, as well as the changes that occur in its crystal lattice with the addition of ‘impurities’, such as oil ( α -tocopherol) and drug (ketoconazole), using DSC and X-ray diffraction analysis before and after thermal stress. Aqueous SLN and NLC dispersions were produced using an appropriate surfactant/co-surfactant system and their physicochemical stability was assessed by PCS, LD, DSC and by WAXS. It was found that the crystalline lattice of Compritol®888 ATO is composed of very small amounts of the unstable α polymorphic form characteristic of triacylglycerols, which disappears after thermal stress of bulk lipid. Mixing oils and drug molecules which are soluble in this lipid decreased its lattice organization and, thus, was revealed to be suitable for production of lipid nanoparticles containing ketoconazole. However, particle growth could not be avoided during shelf life. [ABSTRACT FROM AUTHOR]