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Shreyasi Chakraborty, Nabanita Kar, Leena Kumari, Asit De, Tanmoy Bera Laboratory of Nanomedicine, Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, India Background: Type I hypersensitivity is an allergic reaction characterized by the overactivity of the immune system provoked by normally harmless substances. Glucocorticoids, anti-histamines, or mast cell stabilizers are the choices of treatment for type I hypersensitivity. Even though these drugs have the anti-allergic effect, they can have several side effects in prolong use. Cedrol is the main bioactive compound of Cedrus atlantica with anti-tumor, anti-oxidative, and platelet-activating factor inhibiting properties.Methods: In this study, the preparation and anti-anaphylactic effect of cedrol-loaded nanostructured lipid carriers (NLCs) were evaluated. NLCs were prepared using Compritol® 888 ATO and triolein as lipid phase and vitamin E D-α-tocopherylpolyethyleneglycol 1000 succinate, soya lecithin, and sodium deoxycholate as nanoparticle stabilizers.Results: The average diameter of cedrol-NLCs (CR-NLCs) was 71.2 nm (NLC-C1) and 91.93 nm (NLC-C2). The particle had negative zeta potential values of –31.9 mV (NLC-C1) and –44.5 mV (NLC-C2). Type I anaphylactoid reaction in the animal model is significantly reduced by cedrol and cedrol-NLC. This in vivo activity of cedrol resulted that cedrol suppressed compound 48/80-induced peritoneal mast cell degranulation and histamine release from mast cells. Furthermore, compound 48/80-evoked Ca2+ uptake into mast cells was reduced in a dose-dependent manner by cedrol and cedrol-NLC. Studies confirmed that the inhibition of type I anaphylactoid response in vivo in mice and compound 48/80-induced mast cell activation in vitro are greatly enhanced by the loading of cedrol into the NLCs. The safety of cedrol and CR-NLC was evaluated as selectivity index (SI) with prednisolone and cromolyn sodium as positive control. SI of CR-NLC-C2 was found to be 11.5-fold greater than both prednisolone and cromolyn sodium.Conclusion: Administration of CR-NLC 24 hours before the onset of anaphylaxis can prevent an anaphylactoid reaction. NLCs could be a promising vehicle for the oral delivery of cedrol to protect anaphylactic reactions. Keywords: mast cell, degranulation, allergy, NLC, cedrol, anaphylaxis

Purpose: Due to the antimicrobial property, menthol have significant potential for food preservation and foodstuff shelf life improvement. Nevertheless, menthol instability, insolubility, and rapid crystallization in aqueous media make it unsuitable for used in food products. This work was aimed to prepare menthol-loaded nanostructured lipid carriers (NLCs) to enhance its antimicrobial activity. Methods: Morphology, particle size and size distribution, encapsulation efficiency percent (EE%), and physical stability of the optimized formulation, prepared by hot melt homogenization method, were characterized by scanning electron microscopy, particle size analyzing, gas chromatography, and X-ray diffraction (XRD) methods. Minimum inhibitory concentration and minimum bactericidal concentration of menthol-loaded NLCs were evaluated and compared with conventional menthol emulsion against various Gram-positive (Staphylococcus aureus, Bacillus cereus) and Gram-negative bacteria (Escherichia coli), as well as one fungus (Candida albicans). Results: Menthol-loaded NLCs were spherically shaped nanosized (115.6 nm) particles with narrow size distribution (PDI = 0.2), suitable menthol EE% (98.73%), and appropriate physical stability after 90 days of storage period. XRD results indicated that menthol was in the amorphous form in the nanoparticles matrix. Antibacterial assay results revealed that the menthol-loaded NLCs exhibited significantly higher in vitro antimicrobial property than conventional menthol emulsion. The results also indicated that menthol-loaded NLCs had better effect on fungi than bacteria, and furthermore, antibacterial efficiency on Gram-positive bacteria was higher than Gram-negative bacteria. Conclusion: In conclusion, NLCs could be a promising carrier for improvement of antimicrobial activity and preservation efficacy of essential oils in foodstuffs.

Purpose: Nanostructured lipid carriers (NLCs) composed of solid lipid and oil are a new generation of lipid nanoparticles which have exhibited some merits over traditional used lipid nanoparticles in fortifying food and beverages and nutraceuticals delivery systems such as liposomes and solid lipid nanoparticles. Methods: In this study, Precirol and Compritol as solid lipids, Miglyol and Octyloctanoat as liquid lipids, Tween80, Tween20 and Poloxamer407 as surfactants were used to prepare vitamin D3-loaded NLC dispersion using hot homogenization method. The particle size and size distribution for all formulations were evaluated by immediately after production and during a storage period of 60 days. Results: The Precirol-based NLC showed superiority over Compritol-based NLC in the point of physical stability. Results clearly suggested that an optimum concentration of 3% of Poloxamer407 or 2% of Tween20 was sufficient to cover the surface of nanoparticles effectively and prevent agglomeration during the homogenization process. Octyloctanoat was introduced for the first time as a good substituent for Miglyol in the preparation of NLC formulations. The vitamin D3 Intestinal absorption enhanced by the incorporating in NLCs. Conclusion: It was concluded that NLC showed a promising approach for fortifying beverages by lipophilic nutraceuticals such as vitamin D.

The aim of the present study was to develop a poly-arginine modified nanostructured lipid carrier (R-NLC) by fusion-emulsification method and to test its pharmaceutical characteristics. The influence of R-NLC on A549 cells like cellular uptake and cytotoxicity was also appraised using unmodified NLC as the controlled group. As the results revealed, R-NLC had an average diameter of about 40 nm and a positive zeta potential of about +17 mv, the entrapment efficiency decreased apparently, and no significant difference on the in vitro drug release was found after R8-modification. The cellular uptake and cytotoxicity increased obviously compared with unmodified NLC. The cellular uptake mechanisms of R-NLC involved energy, macropinocytosis, clathrin-mediated endocytosis, and caveolin-mediated endocytosis. The outcomes of the present study strongly support the theory that cell penetrating peptides have the ability of enhancing the cellular uptake of nanocarriers.

Background: Nanostructured lipid carriers (NLCs) are explored as vehicles for ophthalmic drug delivery owing to their better drug loading, good permeation, and satisfactory safety profile., Objective: The purpose of the study was to fabricate and characterize an in situ ocular gel of loratadine as a model drug based on NLCs to enhance the drug residence time., Methods: NLCs were fabricated using the microemulsion method in which solid lipid as Compritol 888 ATO, lipid as oleic acid, surfactant as Tween 80, and isopropyl co-surfactant as alcohol, were used. Based on the evaluation of formulation batches of NLCs, the optimized batch was selected and further utilized for the formulation of in situ gel containing Carbopol 934 and HPMC K15M as gelling agents, and characterized., Results: The optimized NLCs of loratadine exhibited entrapment efficiency of 83.13 ± 0.13 % and an average particle size of 18.98 ± 1.22 nm. Drug content and drug release were found to be 98.67 and 92.48 %, respectively. Excellent rheology and mucoadhesion were demonstrated by the loratadine NLC-loaded in situ gel to enhance its attachment to the mucosa. NLC-based in situ ocular gel showed the desired results for topical administration. The prepared gel was observed to be non-irritating to the eye., Conclusion: The optimized NLC-based in situ gel formulation presented better corneal retention and it was found to be stable, offering sustained release of the drug. Thus, the joined system of sol-gel was found promising for ophthalmic drug delivery., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Background: The disease of the posterior segment of the eye is a major concern worldwide, and it affects more than 300 million people and leads to serious visual deterioration. The current treatment available is invasive and leads to serious eye complications. These shortcomings and patient discomfort lead to poor patient compliance. In the last decade, Nanostructured lipid carriers (NLC) have established a remarkable milestone in the delivery of drug substances to the posterior segment of the eye. Additionally, NLC can reduce the clearance due to adhesive properties which are imparted due to nano-metric size. This attribute might reduce the adverse effects associated with intravitreal therapy and thus enhance therapeutic efficacy, eventually raising patient adherence to therapy. The current review provides an inclusive account of NLC as a carrier to target diseases of the posterior segment of the eye., Objective: The review focuses on the various barrier encountered in the delivery of drugs to the posterior segment of the eye and the detail about the physicochemical property of drug substances that are considered to be suitable candidates for encapsulation to lipid carriers. Therefore, a plethora of literature has been included in this review. The review is an attempt to describe methods adopted for assessing the in-vivo behavior that strengthens the potential of NLC to treat the disease of the posterior segment of the eye., Conclusion: These NLC-based systems have proven to be a promising alternative in place of invasive intravitreal injections with improved patient compliance., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Purpose: This study aimed to prepare, characterize, and in vitro and in vivo evaluate a novel nanostructured lipid carriers (NLCs) formulation containing two fractions of Glycyrrhiza glabra L. (licorice) extract for the treatment of hyperpigmentation., Methods: Two fractions, one enriched with glabridin (FEG) and the other enriched with liquiritin (FEL), were obtained by partitioning the methanol (MeOH) extract of licorice roots with ethyl acetate (EtOAc) and partitioning the EtOAc fraction with butanol (n-BuOH) and water. The quantities of glabridin (Glab) and liquiritin (LQ) in the fractions were determined by high-performance liquid chromatography (HPLC). FEG and FEL were loaded in different NLC formulations, and surface characterization and long-term stability were studied using Dynamic Light Scattering (DLS). The best formulation was chosen for further surface characterization, including Transmission Electron Microscopy (TEM), Differential Scanning Calorimetry (DSC), and Fouriertransform infrared (FTIR) spectroscopy. Moreover, entrapment efficiency percentage (EE%), in vitro drug release, in vivo skin penetration, cytotoxicity on B16F10 melanoma cells, effect on melanin production, and anti- tyrosinase activity were tested for the selected formulation., Results: Based on HPLC results, FEG contained 34.501 mg/g of Glab, and FEL contained 31.714 mg/g of LQ. Among 20 different formulations, NLC 20 (LG-NLCs) showed desirable DLS results with a Z-average size of 185.3 ± 1.08 nm, polydispersity index (PDI) of 0.229 ± 0.35, and zeta potential of -16.2 ± 1.13 mV. It indicated good spherical shape, high EE% (79.01% for Glab and 69.27% for LQ), two-stage release pattern (an initial burst release followed by sustained release), efficient in vivo skin penetration, and strong anti-tyrosinase activity. LG-NLCs had acceptable physiochemical stability for up to 9 months and were non-cytotoxic., Conclusion: The LG-NLC formulation has revealed desirable surface characterization, good physiochemical stability, efficient drug release pattern and in vivo penetration, and high EE%. Therefore, it can be a suitable nanosystem for the delivery of licorice extract in the treatment of hyperpigmentation., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Lipid nanocarriers have a great potential for improving the physicochemical characteristics and behavior of poorly water-soluble drugs, such as aqueous dispersibility and oral bioavailability. This investigation presents a novel nanostructured lipid carrier (NLC) based on a mixture of solid lipid glycerides, fatty acid esters of PEG 1500 (Gelucire® 44/14), and an oil mix composed of capric and caprylic triglycerides (Miglyol® 812). These NLCs were developed by a simple low-energy method based on melt emulsification to yield highly encapsulating and narrowly distributed nanoparticles (~100 nm, PdI = 0.1, and zeta potential = ~−10 mV). Rhodamine 123 was selected as a poorly water-soluble drug model and owing to its spectroscopic properties. The novel NLCs were characterized by dynamic light scattering (DLS), zeta potential, nanoparticle tracking analysis (NTA), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), and colloidal stability. The drug release was determined through a dialysis bag and vertical Franzs’ cells to provide insights about the methods’ suitability, revealing similar performance regardless of their different fluid dynamics. Rhodamine 123 followed a characteristic biphasic release profile owing to the swelling of the hydrophilic polymer coating and diffusion process from the lipid core as revealed by the Korsmeyers–Peppas kinetic modeling. Moreover, to elucidate the formation and incorporation of Rhodamine 123 into the NLC core, several molecular dynamics simulations were conducted. The temperature was shown to be an important condition to improve the formation of the nanoparticles. In addition, the liquid lipid incorporation to the formulation forms nanoparticles with imperfect centers, in contrast to nanoparticles without it. Moreover, Miglyol® 812 improves hydrophobic molecule solubility. These results suggest the potential of novel NLC as a drug delivery system for poorly water-soluble drugs.

The present study focuses on the optimization of process parameters for preparation of nano lipid carriers (NLC's) by emulsion solvent evaporation technique. A definitive screening design using JMP I 3 was used to analyze the effect of process parameters on nano lipid carriers. The critical process parameters evaluated were solid lipid- liquid lipid ratio, phase volume ratio, surfactant concentration and homogenization speed. Each variable was tested at two different levels. Thirteen formulations were prepared as per the design. The design was employed to estimate the effect of each variable on particle size, PDI and surface charge. Model validation was carried out at a significance level of p<0.05 and the process was optimized at a desirability of 0.90. Three optimized formulations were prepared in the design space using optimized process parameters. The percentage bias of particle size, PDI and zeta potential of the predicted and the observed values were found to be less than 5%. The optimized formulations were subjected for SEM study, which revealed the formation of nano particles. Gas chromatography of the optimized formulation showed the residual solvent content was within the limit as per ICH Q3 R6 guidelines. The suitability of the process to Improve solubility was proved by formulation of nano lipid carriers of highly lipophilic drugs. Therefore, the design was found to be effective for production of nano lipid carriers by emulsion solvent evaporation technique. [ABSTRACT FROM AUTHOR]

Nanoparticulate drug delivery systems have an advanced and modern approach over the traditional delivery system. This systematic review on nanoparticulate drug delivery containing lipid and focus on preparation, challenges and advancement of delivery of the drug via topical and transdermal route. The first era of lipid nanoparticles were SLN and have more sustaining action as well as suitable for the higher permeation of drug. The NLC is the second generation lipid nanoparticles developed to overcome the limitation associated with SLN i.e low drug loading capacity, polymorphism of solid lipid. Production of solid lipid nanoparticles and nanostructured lipid carriers are produced by a variety of technologies which explored in the current review. Lipid nanoparticle has various properties for topical use of cosmetics and other pharmaceutical formulation, i.e. controlled and sustained release of medicaments, Physical and chemical stability of active pharmaceutical ingredients, targeted release, film formation and enhancing penetration with the enhancement of skin hydration. Skin hydration plays a major role in the topical delivery of API as it hydrates the skin which leads to opening of pores of skin. Due to occlusion nature of lipid nanoparticles trans epidermal water loss decline which softening the skin. The use of biodegradable grade lipid makes it more suitable because it does not cause any toxicity as created by polymeric nanoformulations. Furthermore, a discussion about the benefit/risk ratio of a nanoparticulate system containing lipids also explored in this paper. The SLN and NLC are a "nanosafe" carrier for the delivery of active pharmaceutical via topical route. [ABSTRACT FROM AUTHOR]

The usefulness of nanotechnology to increase the bioavailability of drugs and decrease their toxicity may be a tool to deal with multiresistant P. aeruginosa (Mr-Pa) respiratory infections. We describe the preparation and the in vivo efficacy and safety of sodium colistimethate-loaded nanostructured lipid carriers (SCM-NLC) by the pulmonary and intramuscular routes. Nanoparticles showed 1-2 mg/L minimum inhibitory concentration against eight extensively drug-resistant P. aeruginosa strains. In vivo , SCM-NLC displayed significantly lower CFU/g lung than the saline and similar to that of the free SCM, even the dose in SCM-NLC group was lower than free SCM. There was no tissue damage related to the treatments. Biodistribution assessments showed a mild systemic absorption after nebulization and a notorious absorption after IM route. Altogether, it could be concluded that SCM-NLC were effective against P. aeruginosa in vivo , not toxic and distribute efficiently to the lung and liver after pulmonary or intramuscular administrations. A novel formulation against different Pseudomonas aeruginosa multiresistant clinical isolates based on sodium colistimethate-loaded nanostructured lipid carriers (SCM-NLC) was developed, characterized and administered by pulmonary and intramuscular routes. In addition, the effectiveness, safety and biodistribution of SCM-NLC were tested against non-encapsulated SCM, using both in vitro and in vivo models. Encapsulation process enhances the pharmacological efficacy of SCM and decreases toxicity, and both administration routes result in an efficient therapy against P. aeruginosa : pulmonary route for maintenance therapy due to its main effect in lungs, while intramuscular route for an emergency as it showed a faster absorption. Unlabelled Image [ABSTRACT FROM AUTHOR]

The present work reports the development, optimization and characterization of novel lipid based nanoformulations viz., Liquid crystalline nanoparticles (LCNP), solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) and liposomes loaded with Tacrolimus (Tac) for topical delivery. Different nanoformulations were developed after screening lipids and suitable surfactants depending upon emulsification ability. The various nanoformulations were then optimized (to achieve higher entrapment efficacy, lower particle size, PDI and zeta potential), characterized and loaded into gel. The gels loaded with nanoformulations were also characterized depending upon rheology and viscosity. The gels were analyzed for in vitro drug release, HaCaT cell lines studies and skin permeation studies. The in vivo efficacy studies were carried out using mouse tail model and skin irritation studies using Draize patch test and measurement of TEWL. The developed nanoformulations showed optimum particle size (<200 nm), polydispersity index (PDI < 0.3), zeta potential (≥−10 mV) and higher entrapment efficiency (>85%). The nanoformulations showed higher penetration of Tac into skin. Tac-LCNP, Tac-SLN, Tac-NLC and Tac-liposomes loaded gels showed 14, 11.5, 12.5 and 3.7 folds increment in dermal bioavailability respectively, in comparison to free Tac loaded gel and 2.5, 2 and ∼2 folds augmentation in dermal bioavailability respectively as compared to Tacroz™ Forte. In case of Tac-liposomes, the dermal bioavailability was lower as compared with the marketed formulation, Tacroz™ Forte. Despite, the increased bioavailability into the skin, the developed nanoformulations showed no significant skin irritation. The above mentioned nanoformulations were able to achieve greater penetration of Tac into the skin as compared to marketed ointment of Tac, Tacroz™ Forte. [ABSTRACT FROM AUTHOR]

Abstract The objective of this study was to assess the effect of resveratrol and resveratrol-loaded nanostructured lipid carriers (NLC) supplementation of semen extender on values for fertility variables of cryopreserved rooster semen. Rooster semen was cryopreserved in modified Beltsville extender containing 0 (control group), resveratrol at 20, 40 and 60 μM and resveratrol-loaded NLC at 20, 40 and 60 μM. After thawing, motility properties, abnormal morphology, viability, membrane functionality, mitochondrial activity, apoptotic status, malondialdehyde (MDA) and antioxidant activities (glutathione peroxidase (GPx), superoxide dismutase (SOD), and total antioxidant capacity (TAC)) and fertility potential (fertility and hatchability rates) were assessed. Using 40 μM resveratrol and resveratrol-loaded NLC improved total motility. The results indicated that sperm fertility and hatching rate, viability and membrane functionality were greater in the 40 μM resveratrol and resveratrol-loaded NLC compared to control group. The percentage of apoptotic spermatozoa in 40 μM resveratrol and resveratrol-loaded NLC group was less compared with the 60 μM resveratrol, 60 resveratrol-loaded NLC and control groups. Mitochondria activity was greater in the 40 μM resveratrol and resveratrol-loaded NLC extender group compared to 20 and 60 μM resveratrol, 60 resveratrol-loaded, and control groups. Also, the 40 μM resveratrol and resveratrol-loaded NLC extender group had a greater TAC and reduced MDA. Morphology and SOD were not affected by dose of resveratrol. The results indicate supplementation of the modified Beltsville extender with 40 μM resveratrol and resveratrol-loaded NLC resulted in a greater quality of frozen-thawed rooster sperm. [ABSTRACT FROM AUTHOR]

The global burden of cancer have encouraged oncologists to develop novel strategies for treatment. Present study was proposed to develop Arginyl-glycyl-aspartic acid (RGD)-containing nanostructured lipid carriers (NLC) as a delivery system for improving the anticancer capability of epigallocatechin gallate (EGCG) on breast cancer cell line by attaching to integrin superfamily on cancer cells. For this purpose, RGD-containing EGCG-loaded NLC were prepared by hot homogenization technique and characterized by different techniques. Then, cytotoxic and apoptotic effects of prepared nanoparticles and their uptake into cells was evaluated. As results, the nanoparticles with particle size of 85 nm, zeta potential of −21 mV, encapsulation of 83% were prepared. Cytotoxicity and apoptosis experiments demonstrated that EGCG-loaded NLC-RGD possessed greatest apoptotic activity. Furthermore, it has been shown that, EGCG-loaded NLC-RGD causes cell cycle arresting more effective than EGCG. Therefore, loading EGCG into NLC-RGD make it more effective in both targeting and accumulation into tumour cells, which results from specialized uptake mechanism by adhesion to αvβ3 integrin. The results strengthen our hope that loading EGCG into RGD-containing NLC could possibly overcome the therapeutic limitations of EGCG and make it more effective in cancer therapy. [ABSTRACT FROM AUTHOR]

This project was designed to extract anti-hyperlipidaemic activity of simvastatin for the longer duration of time and the solubility enhancement of this BCS class II drug was also sought by preparing nanostructured lipid carrier (NLC). The method for NLC preparation involved melt-emulsification followed by ultrasonication. The developed formulation was optimized by 3-level, 3-factor Box-Behnken design. The independent variables were % lipid mixture, % surfactant and sonication time (minutes). The responses selected were particle size, PDI and entrapment efficiency. The optimized formulation had particle size 114.62 ± 5.65, PDI 0.210 ± 0.034 and entrapment efficiency 85.20 ± 7.98%. The optimized formulation was further characterized by TEM and SEM. Spherical shape and nano size distribution of the optimized formulation were confirmed by SEM and TEM, respectively. The DSC of optimized formulation hints for the loss of crystalline nature of drug whereas the FT-IR spectra reveal that there is no interaction between drug and excipients when incorporated in NLC. The drug release from the NLC was biphasic (burst release was followed by sustained release). The kinetic of drug release followed Fickian diffusion with Korsmeyer-Peppas model. When the antihyperlipidaemic activity of SMV-NLC was compared with SMV-suspension, it was found that SMV-NLC significantly decreased the total cholesterol and triglyceride level by 2.77 and threefolds, respectively. [ABSTRACT FROM AUTHOR]

Butamben is a topical local anesthetic which formulation in lipid-based drug delivery systems (DDS) is challenging due to its affinity for hydrophilic excipients. This means that a medium polarity excipient is preferred for the development of a stable nanostructured lipid carrier (NLC) formulation. In turn, in NLC, the type and number of excipients will determine the active pharmaceutical ingredient (API) solubility and the maximum drug upload. To solve this dilemma and get the best formulation, a throughout screening study to evaluate API solubilization in different excipients was carried out. Subsequently, excipients with different solubilization capacities were selected for microscopic evaluation by Raman mapping, and in turn analysis of the distributional homogeneity index (DHI) and standard deviation of the histograms allowed solving the posed question. Design of experiments (DoE) was employed to understand better the interactions between the excipients; linear and higher-order models were obtained with R2 above of 0.8824. Even though DHI is a good parameter to be used as response, an API concentration higher than 30% (w/w) provided a homogeneous surface in case of good miscibility and, in this case, this parameter needs to be employed with an inspection and/or evaluation of other parameters. A curve of concentration vs. mean scores of images proved to be an alternative to identify the saturation/limit of linear range. [Display omitted] • Screening of promising excipients for a 'brick dust' type compound. • Different miscibility of drug and excipients presented different surface images. • DHI was used as the response of a mixture design of experiments (DoE). • The methodology is helpful to stablish the drug load to be used. [ABSTRACT FROM AUTHOR]

The aim of the present study was to encapsulate rutin by nanostructured lipid carriers (R-NLCs), as a solution to eliminate the fortification difficulties and provide healthier functional foods. Rutin was loaded into food grade NLCs in different rutin to lipid ratios using high shear rate homogenization method. Colloidal properties of R-NLCs such as particle size, poly dispersity index, encapsulation efficiency, loading capacity, and encapsulation stability were studied. R-NLCs with a rutin to lipid ratio of 10% were selected as an optimum formulation. Morphological studies have shown that R-NLCs are round shaped particles with smooth surfaces. The R-NLC fortified food samples and models were subjected to pH, physical and thermal stability, and turbidity analysis. The results indicated that the developed R-NLCs could provide a method for designing new functional foods based on nanocarriers.

During the past decade, pharmaceutical science has seen rapid growth in interest for nanoscale materials. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are popular research topics recently introduced as nano-scale drug carriers; they have shown numerous merits in drug delivery. Size is the most important index in a nanocarrier affecting its drug delivery efficiency. The influence of preparation conditions and type of lipidic components on the size of SLN and NLC in comparable states seems to be interesting for researchers who investigate these types of carriers. This review highlights the results of SLN and NLC particle size and size distribution comparisons.

Capsaicin is an active compound in chili peppers (Capsicum chinense) that has been approved for chronic pain treatment. The topical application of high-strength capsaicin has been proven to reduce pain; however, skin irritation is a major drawback. The aim of this study was to investigate an appropriate and scalable technique for preparing nanostructured lipid carriers (NLCs) containing 0.25% capsaicin from capsicum oleoresin (NLC_C) and to evaluate the irritation of human skin by chili-extract-loaded NLCs incorporated in a gel formulation (Gel NLC_C). High-shear homogenization with high intensity (10,000 rpm) was selected to create uniform nanoparticles with a size range from 106 to 156 nm. Both the NLC_C and Gel NLC_C formulations expressed greater physical and chemical stabilities than the free chili formulation. Release and porcine biopsy studies revealed the sustained drug release and significant permeation of the NLCs through the outer skin layer, distributing in the dermis better than the free compounds. Finally, the alleviation of irritation and the decrease in uncomfortable feelings following the application of the Gel NLC_C formulation were compared to the effects from a chili gel and a commercial product in thirty healthy volunteers. The chili-extract-loaded NLCs were shown to be applicable for the transdermal delivery of capsaicin whilst minimizing skin irritation, the major noncompliance cause of patients.

The aim of this study was to develop lipid-based nanoparticles that entrapped a high concentration of capsaicin (0.25%) from a capsicum oleoresin extract. The solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) were strategically fabricated to entrap capsaicin without a hazardous solvent. Optimized nanosize lipid particles with high capsaicin entrapment and loading capacity were achieved from pair-wise comparison of the solid lipid mixtures consisting of fatty esters and fatty alcohols, representing small and large crystal-structure molecules combined with a compatible liquid lipid and surfactants (crystallinity index = 3%). This report was focused on selectively captured capsaicin from oleoresin in amorphous chili extract-loaded NLCs with 85.27% ± 0.12% entrapment efficiency (EE) and 8.53% ± 0.01% loading capacity (LC). The particle size, polydispersity index, and zeta potential of chili extract-loaded NLCs were 148.50 ± 2.94 nm, 0.12 ± 0.03, and −29.58 ± 1.37 mV, respectively. The favorable zero-order kinetics that prolonged capsaicin release and the significantly faster transdermal penetration of the NLC attributed to the reduction in skin irritation of the concentrated capsaicin NLCs, as illustrated by the in vitro EpiDermTM three-dimensional human skin irritation test and hen’s egg test chorioallantoic membrane assay (HET-CAM).

Purpose: Nanostructured lipid carrier (NLC) is a useful delivery system with high capacity for bioactive loading, and suitable stability for fortification of foods and beverages. The objective of the present work is to prepare vitamin A palmitate (vitA)-loaded NLC and to investigate surfactant concentration effect on physicochemical properties of prepared formulation. Methods: VitA-loaded NLC was prepared by hot homogenization method. Preciol as solid lipid, Octyloctanoate as liquid oil, and Poloxamer as surfactant were used to prepare the formulation. The effect of different concentrations of Poloxamer on particle size, particle size distribution, encapsulation efficiency and stability of vitA during storage were investigated. Fourier transform infrared spectra (FTIR) was exploited to study the possible bioactive-lipid complex formation. Results: NLCs stabilized with 6% Poloxamer showed significantly lower particle size and particle size distribution. The encapsulation efficiency of this formulation was 98.5% and it was stable during the storage at 25°C for two months. Conclusion: This study suggests that surfactant significantly influences the final product properties. Our findings may pave the way of researchers to focus on fortifying the beverages with various lipophilic nutraceuticals.

Graphical abstract Abstract Carbamazepine is a valuable pharmacological agent prescribed in treatment of epilepsy and trigeminal neuralgia. Poor bioavailability, successive dose adjustments and reported long term toxic effects are the main hurdles associated with carbamazepine oral administration. Bees wax containing NLC formulations were developed using high shear homogenization/sonication technique to overcome drug limitations. Formulations were successfully produced and evaluated for both in vitro and in vivo assessments. Results showed particles in nanometric range with negative surface charge and satisfying encapsulation efficiencies (from 93.1 ± 7.6 to 95.7 ± 5.6%). In vitro release studies revealed biphasic pattern and faster release was accompanied with higher bees wax concentration. Interaction between drug and NLC components was assessed using infrared and thermal analysis. Using validated chromatographic analytical method, selected formulation showed good pharmacokinetic profile depriving from plasma fluctuation with 2.27-fold and 1.83-fold improved bioavailability compared to conventional drug suspension and Tegretol™ suspension respectively. It also showed stronger anticonvulsant activity, with respect to conventional drug suspension, in terms of seizure latency, frequency and duration. Toxicity studies revealed undetectable liver or testicular toxicity in biochemical, histological and immunohistochemical investigations verifying its superiority above other investigated formulations. Collectively, results indicate potential suitability of NLC system to effectively and safely deliver carbamazepine orally. [ABSTRACT FROM AUTHOR]

In the present work attempts have been made to prepare the nanostructured lipid carriers (NLC) gel, by using the poorly water-soluble drug isotretinoin (IT), which is preferably used in the case of acne. The four different formulations of IT-NLC (NLC 1-NLC 4) were prepared using solid and liquid lipid with Tween 80 in different ratios by the hot homogenization method. Properties of entrapment efficiency and drug release behavior were investigated for all formulations from this NLC 4 formulation and optimized. Evaluation of NLC 4 such as particle size, zeta potential, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), transmission electron microscopy (TEM), x-ray diffraction (XRD), and photostabilty study was performed. The nanoparticles were suitably gelled and evaluated for drug content, pH, spreadability, extrudability, rheology, and drug release. Safety to gel was assessed using primary skin irritation studies. The formulated NLC 4 was spherical in shape, with average particle size 154.1 nm, zeta potential -26.9 mV, and entrapment efficiency 91.85% ± 0.10%. The results showed that entrapment of IT into NLCs reduced its photo degradation. IT-NLC gel showed a faster onset of action and elicited prolonged activity. The IT-NLC gel was less irritating, which shows improving ability for skin tolerability and being a carrier for topical delivery. [ABSTRACT FROM AUTHOR]

We present the first results on the retrieval of noctilucent cloud (NLC) albedos and occurrence rates from SCIAMACHY (SCanning Imaging Absorption spectroMeter for Atmospheric CHartography) nadir data. The applicability of already available algorithms is discussed and necessary changes are reasoned. The occurrence rates for different latitude ranges are presented. During the summer period, when NLCs occur, the NLC occurrence rates show a maximum which is strongest at the highest latitudes. This is consistent with other observation methods. For the spring and autumn period, however, false NLC detections are observed at latitudes between 45°N and 65°N, where no NLCs are expected. The reason for this, and why it does not affect the retrieval during the NLC season is discussed. We also compared the SCIAMACHY nadir NLC occurrence rates with the ones retrieved from the SCIAMACHY limb measurements and the ones of SBUV and found qualitative agreement of these data sets. [ABSTRACT FROM AUTHOR]

Essential oils are recognized as valuable active pharmaceutical ingredients attributed to a set of biological properties, which include antibacterial, antifungal, antiviral, antioxidant, anticancer, immune-modulatory, analgesic and anti-inflammatory activities. Their use in pharmaceutics is however compromised by their limited water solubility and low physicochemical stability (i.e. volatility, oxidation). In order to overcome these limitations, we aimed to develop nanostructured lipid carriers (NLC) as delivery systems for Mediterranean essential oils, in particular Rosmarinus officinalis L., Lavandula x intermedia “Sumian”, Origanum vulgare subsp. hirtum and Thymus capitatus essential oils, selected on the basis of their antioxidant and anti-inflammatory activities. NLC composed of Softisan (as solid lipid) have been produced by phase inversion temperature (PIT) and high-pressure homogenization (HPH), using two different emulsifiers systems. Particles have been further characterized for their mean particle size, polydispersity, zeta potential, morphology and chemical interactions. Best NLC formulations were obtained with Kolliphor/Labrafil as surfactants, and using Rosmarinus , Lavandula and Origanum as essential oils (PDI between 0.126 and 0.141, Zave < 200 nm). Accelerated stability studies have also been carried out to estimate the effect of the production method and surfactant composition on the long-term stability of EOs-loaded NLC. In vitro biological cell viability and anti-inflammatory activities were evaluated in Raw 264.7 cells (macrophage cell line), while in vitro antioxidant activity was checked by DPPH assay. Lavandula and Rosmarinus NLC were shown to be the most biocompatible formulations up to a concentration of 0.1% (v/v), whereas they were able to induce a dose-dependent anti-inflammatory activity in the order Lavandula  >  Rosmarinus  ≥  Origanum . [ABSTRACT FROM AUTHOR]

Nanostructured lipid carriers (NLC), comprises of a blend of solid and liquid lipids which results in a partially crystallized lipid system and imparts many advantages over solid lipid nanoparticles such as enhanced drug loading capacity, drug release modulation flexibility and improved stability. NLC have found numerous applications in both pharmaceutical and cosmetic industry due to ease of preparation, the feasibility of scale-up, biocompatibility, non-toxicity, enhanced targeting efficiency and the possibility of site-specific delivery via various routes of administration. This review highlights the NLC with focus on the structure, the various fabrication techniques used and the characterization techniques which are critical in the development of a suitable and stable formulation. The review also provides an insight into the potential of NLC as site-specific delivery systems and the therapeutic applications explored via various routes of administration. [ABSTRACT FROM AUTHOR]

Helicobacter pylori infection is one of the major risk factors for gastric cancer development. Available antibiotic-based treatments not only fail in around 20% of patients but also have a severe negative impact on the gut microbiota. Recently, we demonstrated that nanostructured lipid carriers (NLC), even without any drug loaded, are bactericidal against H. pylori at low concentrations. This work aims to clarify NLC mode of action and to evaluate if their bactericidal effect is specific to H. pylori without affecting bacteria from microbiota. NLC were produced by hot homogenization followed by ultrasonication method, using Precirol®ATO5 and Miglyol®812 as lipids and Tween®60 as a surfactant. NLC were able to eradicate H. pylori without affecting the other tested bacteria ( Lactobacillus, E. coli, S. epidermidis and S. aureus). Bioimaging assays demonstrated that NLC rapidly bind to and cross the H. pylori bacterial membrane, destabilizing and disrupting it, which leads to leakage of the cytoplasmic contents and consequent bacterial death. In an era where efficient alternatives to antibiotics are urgent, NLC are an interesting route to be explored in the quest for new antibiotic-free therapies to fight H. pylori infection. [ABSTRACT FROM AUTHOR]

This is the first report in literature using hydrophilic interaction liquid chromatography (HILIC) in combination with diode array detector (DAD) for stability indicating determination of 5-Fluorouracil (5-FU) from its bulk form, pharmaceutical preparations, developed solid lipid nanoparticle (SLN) and nano structured lipid carrier (NLC) drug delivery systems as well as the rat skin extracts. The separation was performed at 45 °C, on Sequant Zic HILIC (250 mm × 4.60 mm ID, 5 μm, 200 A o ), peek HPLC column. Mobile phase is consisting of a mixture of acetonitrile: buffer containing 5 mM ammonium acetate (95:5; v/v). The pH of the mobile phase was adjusted to 7.0 using 1 M NaOH. The analysis was carried out at 0.75 mL min −1 flow rate with a detection wavelength of 265 nm and the injection volume was arranged as 10 μL. The developed method was fully validated in accordance with the International Council on Harmonization (ICH) Guidelines. Specificity of this method was demonstrated by forced degradation studies. As a result of calibration studies, the calibration curve was found linear in the concentration range of 1–250 μg mL −1 (R 2  = 0.999). The precision of this technique calculated within the frame of intra-day and inter-day based on a percentage of relative standard deviation (RSD%) values (<2%). The limits of detection and quantification were 11 and 37 ng mL −1 respectively. On the other hand, 5-FU loaded SLN and NLC formulations with average particle size of 370 nm were also developed and compared in order to increase the permeation of drug into the rat skin. Ex-vivo Penetration/Permeation Studies indicated that higher dermal accumulation of 5-FU was obtained with NLC formulation. As a conclusion, the present work expressed the optimization and the validation of a selective, simple, precise and accurate fully validated HILIC method with sufficient sensitivity for the estimation of 5-FU in raw materials, marketed formulation and rat skin extract after applying both of the commercial product and newly developed nanoparticulate drug delivery systems on to the rat skins with high percentage recoveries. [ABSTRACT FROM AUTHOR]

Nanostructured lipid carriers (NLC) comprising soy lecithin (SLC), tristearin (TS) and palmitic acid (PA) having molar ratio 2:2:1 was modified by partially replacing SLC with ion pair amphiphile (NLC IPA ), prepared by mixing equimolar aqueous solution of sodium dodecyl sulphate and hexadecyltrimethylammonium bromide. Hot homogenization followed by ultrasonication method was employed for the preparation of NLC and NLC IPA . Desirable SLC / IPA ratio for NLC IPA formulations were obtained by analyzing the interfacial behavior of the lipidic components in the presence of IPA at air-water interface. Considering the interfacial behavior and mutual miscibility, lipid compositions having SLC/IPA ratio equal to 2:3, 3:7 and 1:4 were selected for the preparation of NLC IPA . Analytical techniques like dynamic light scattering, differential scanning calorimetry, transmission electron microscopy, fridge fractured electron microscopy and atomic force electron microscopy assured higher stability of NLC IPA formulations compared to the conventional NLC and the NLC IPA with 30 mol% SLC was found to be optimum. Experimental evaluation of interfacial, solution phase and thermal characteristics of oleanolic acid (OA) loaded NLC and NLC IPA formulations indicated the accumulation of OA on the palisade layer and the drug acquisition was higher in NLC IPA than the conventional NLC. NLC IPA formulations were found even more promising to sustain the release of OA to a desirable extent. Higher cytotoxic activity for the OA loaded NLC IPA than the NLC was noted during the cytotoxicity studies on hepatocellular carcinoma, hepatocyte-derived carcinoma and colorectal carcinoma cancer cell lines. The NLC IPA formulations, therefore, can be considered as promising alternate to conventional NLC in improving the therapeutic efficacy of OA as the anticancer drug. [ABSTRACT FROM AUTHOR]

Abstract: Homologues long‐chain chrysin derivatives (LCD, Cn: 8–18) were synthesized and incorporated into nanostructured lipid carriers (NLC) with the aim to treat human neuroblastoma. Mutual miscibility and attractive interactions among the NLC components, namely tripalmitin (TP), cetyl palmitate (CP), oleic acid (OA), and the chrysin (CHR) derivatives (LCD) at the air–water interface were assessed by the Langmuir monolayer approach. Optimum combination for the NLC formulations was found to be 2:2:1 (M/M/M) for TP/CP/OA, respectively. NLC formulations, both in the absence and presence of LCD, were characterized by combined dynamic light scattering, electron microscopy, atomic force microscopy, and differential scanning calorimetry. The size and zeta potential of the NLC formulations were found in the range 200–350 nm and −12 to −18 mV, respectively. Encapsulation efficiency and release kinetics of CHR and LCD when loaded into NLC were also evaluated. LCD exhibited maximum incorporation, drug‐loading capacity, and sustained release because of its enhanced hydrophobicity. Superior incorporation efficiency and sustained‐release profile of LCD were able to enhance their anticancer activity against human neuroblastoma cell lines, compared to CHR, making them promising agents in combating cancer. [ABSTRACT FROM AUTHOR]

Epidermal growth factor receptor variant III (EGFRvIII) is the most common variant of the EGF receptor in many human tumors. This variant is tumor specific and highly immunogenic, thus, it can be used as a target for targeted drug delivery toward tumor cells. The major aim of this study was to develop an EGFRvIII-mediated drug delivery system by anti-EGFRvIII monoclonal antibody (MAb) conjugated to doxorubicin (Dox)-loaded nanostructured lipid carriers (NLC) to enhance the targeting specificity and cytotoxic effect of Dox on EGFRvIII-overexpressing cell line. In our study, Dox was chosen as a hydrophobic cytotoxic drug and drug-loaded nanostructured lipid carriers (Dox-NLC) was prepared by solvent emulsification/evaporation method. In order to conjugate anti-EGFRvIII MAb to Dox-NLC, DSPE-PEG2000-NHS (1,2-distearoylphosphatidylethanolamine–polyethylene glycol 2000–NHS) was used as a linker. Physicochemical characteristics of antibody conjugated Dox-NLC (MAb-Dox-NLC), including particle size, zeta potential, entrapment efficiency andin vitroDox release were investigated. Cytotoxicity of MAb-Dox-NLC against NIH-3T3 and HC2 20d2/c (EGFRvIII-transfected NIH-3T3) cell lines was evaluated. The MAb-Dox-NLC appeared to enhance the cytotoxic activity of targeted NLC against HC2 20d2/c cells. The cellular uptake percentage of targeted NLC by HC2 20d2/c cells was higher than that of NIH-3T3 cells, indicating that EGFRvIII can specifically target HC2 20d2/c cells. In conclusion, anti-EGFRvIII MAb-targeted NLC may be considered as an effective nanocarrier for targeted drug delivery. [ABSTRACT FROM AUTHOR]

Cardamom essential oil (CEO) loaded food grade nanostructured lipid carriers (NLCs) were produced using cocoa butter (as solid lipid) and Tween 80 (as surfactant) for application in aqueous-based foods. The results demonstrated that the developed NLCs had fine size (<150 nm) and high entrapment efficiency (>90%). Differential scanning calorimetry (DSC) results showed a less-ordered crystalline structure leading to high loading capacity. All samples exhibited perfect type crystal (or β-modification crystal) and a less crystalline state in X-ray diffractograms. Few changes were detected in the turbidity of systems after storage time, demonstrating that the NLCs did not show significant aggregation. Antimicrobial activity of CEO emulsion and CEO loaded NLC formulations were investigated by Broth Macrodilution method and confirmed that, encapsulation was able to protect the antimicrobial activity of CEO. The results showed that CEO-loaded NLC could be used as food supplements. [ABSTRACT FROM AUTHOR]

Conveyor systems in thermal power stations cater the need of fuel flow from mines to thermal power stations for power generation. Conveyors are seen virtually in the coal handling plant (CHP) that are having number of conveyors. The conveyor system has many combinational conveyor sequences. The control systems used for these conveyors are important for the safe operation the plants. In order to ensure the safe belt conveyor operation a reliable, centralized monitoring and controlling is necessary. The conveyor scheme operational system has enormous control components to achieve a starting logic, stopping logic, tripping logic. The control components are mostly electromagnetic relays, timers and indicating lamps etc. Also the system has many other indicating, sensing components for its monitoring and protection purpose. The system has limitation for future modification due to the complexity of hard wired circuit. In order to overcome the above complexity problem and achieve better optimized result, PLC is proposed to control the conveyor system. PLC is automatic controller device which minimizes more number of requirements of electromagnetic relay, timers etc. and it can be programmed to accept the operational logic in a minimal time. [ABSTRACT FROM AUTHOR]

Lipid nanocarriers show occlusive properties that may be related to their ability to improve skin hydration. The aim of this work was to evaluate the relationship between in vitro occlusion factor and in vivo skin hydration for three types of lipid nanocarriers: nanoemulsions (NEs), solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs). These lipid nanocarriers were loaded with trans-resveratrol (RSV) and incorporated in gel vehicles. In vitro occlusion factor was in the order SLNs > NLCs > NEs. Gels containing unloaded or RSV loaded lipid nanocarriers were applied on the back of a hand of 12 healthy volunteers twice a day for one week, recording skin hydration changes using the instrument Soft Plus. An increase of skin hydration was observed for all lipid nanocarriers (SLNs > NLCs > NEs). RSV loading into these nanocarriers did not affect in vitro and in vivo lipid nanocarriers effects. A linear relationship (r2 = 0.969) was observed between occlusion factor and in vivo increase of skin hydration. Therefore, the results of this study showed the feasibility of using the occlusion factor to predict in vivo skin hydration resulting from topical application of different lipid nanocarriers loading an active ingredient with no inherent hydrating activity. [ABSTRACT FROM AUTHOR]

Periodontitis treatment is usually focused on the reduction or eradication of periodontal pathogens using antibiotics against anaerobic bacteria, such as metronidazole (MTR). Moreover, recently the correlation between periodontal diseases and overexpression of reactive oxygen species (ROS) led to the introduction of antioxidant biomolecules in therapy. In this work, bioadhesive buccal tablets, consisting of a hydrophilic matrix loaded with metronidazole and lipophilic nanoparticles as a vehicle of curcumin, were developed. Curcumin (CUR)-loaded nanostructured lipid carriers (NLC) were prepared using glycyrrhetic acid, hexadecanol, isopropyl palmitate and Tween®80 as a surfactant. As method, homogenization followed by high-frequency sonication was used. After dialysis, CUR-NLC dispersion was evaluated in terms of drug loading (DL, 2.2% w/w) and drug recovery (DR, 88% w/w). NLC, characterized by dynamic light scattering and scanning electron microscopy (SEM), exhibited a spherical shape, an average particle size of 121.6 nm and PDI and PZ values considered optimal for a colloidal nanoparticle dispersion indicating good stability of the system. Subsequently, a hydrophilic sponge was obtained by lyophilization of a gel based on trehalose, Natrosol and PVP-K90, loaded with CUR-NLC and MTR. By compression of the sponge, matrix tablets were obtained and characterized in term of porosity, swelling index, mucoadhesion and drugs release. The ability of the matrix tablets to release CUR and MTR when applied on buccal mucosa and the aptitude of actives to penetrate and/or permeate the tissue were evaluated. The data demonstrate the ability of NLC to promote the penetration of CUR into the lipophilic domains of the mucosal membrane, while MTR can penetrate and permeate the mucosal tissue, where it can perform a loco-regional antibacterial activity. These results strongly support the possibility of using this novel matrix tablet for delivering MTR together with CUR for topical treatment of periodontal diseases.

Ice particles populating noctilucent clouds and being responsible for polar mesospheric summer echoes exist around the mesopause in the altitude range from 80 to 90 km during polar summer. The particles are observed when temperatures around the mesopause reach a minimum, and it is presumed that they consist of water ice with inclusions of smaller mesospheric smoke particles (MSPs). This work provides estimates of the mean size distribution of MSPs through analysis of collision fragments of the ice particles populating the mesospheric dust layers. We have analyzed data from two triplets of mechanically identical rocket probes, MUltiple Dust Detector (MUDD), which are Faraday bucket detectors with impact grids that partly fragments incoming ice particles. The MUDD probes were launched from Andøya Space Center (69°17'N, 16°1'E) on two payloads during the MAXIDUSTY campaign on 30 June and 8 July 2016, respectively. Our analysis shows that it is unlikely that ice particles produce significant current to the detector, and that MSPs dominate the recorded current. The size distributions obtained from these currents, which reflect the MSP sizes, are described by inverse power laws with exponents of k∼ [3.3 ± 0.7, 3.7 ± 0.5] and k∼ [3.6 ± 0.8, 4.4 ± 0.3] for the respective flights. We derived two k values for each flight depending on whether the charging probability is proportional to area or volume of fragments. We also confirm that MSPs are probably abundant inside mesospheric ice particles larger than a few nanometers, and the volume filling factor can be a few percent for reasonable assumptions of particle properties. [ABSTRACT FROM AUTHOR]

The use of lipidic nanoparticles can overcome the limitations of skin penetration of hydrophilic charged materials. Oleic acid as an ion pairing agent was used to enhance the encapsulation of positively charged arginine into lipophilic nanostructured lipid carrier (NLC). Histological study on the male hamsters was performed to assess the efficiency of drug delivery on hair growth. The accumulation of NLCs in the hair follicles was verified andin vivostudies showed more new hair follicle growth by utilizing arginine-loaded NLCs than arginine aqueous solution. It was concluded that employing ion pairing agent could enhance drug encapsulation into NLCs structure. [ABSTRACT FROM AUTHOR]

The aim of this study was to determine the effect of lipid ratio of stearic acid and oleic acid on the physical characteristics as well as the entrapment efficiency of diethylammonium diclofenac with Nanostructure Lipid Carrier (NLC) system. Diethylammonium diclofenac (DETA) is Non-Steroid Anti- Inflamatory Drugs (NSAIDs) that has been widely used in the treatment of osteoarthritis and rheumatoid arthritis. In the formulation of NLC-DETA, three different lipid ratios were used, which the ratio of stearic acid:oleic acid were 60:40, 70:30, and 80:20, respectively. In this NLC system, DETA served as the active drug, stearic acid as solid lipid, oleic acid as liquid lipid, and Tween 80 as surfactant components. NLC were characterized for organoleptic characteristics, pH, viscosity, particle morphology, particle size and polydispersity index (PI), profiles of Fourier Transform Infra-Red (FTIR) and Differential Thermal Analysis (DTA), and drug entrapment efficiency. The particle shape and morphology were determined by Transmission Electron Microscopy (TEM). The results showed that the different ratios of oleic acid lipids and stearic acid had no significant effects on the viscosity and entrapment efficiency of NLC-DETA. On the other hand, it affected the pH of all formulas, which were significantly different. Increasing the amount of liquid lipid in the formulations reduced the size of NLC-DETA particles. [ABSTRACT FROM AUTHOR]

Nowadays sigma-1 receptors are considered as new therapeutic objectives for central nervous system neurodegenerative diseases. Among different molecules, alpha lipoic acid has been identified as a natural potent antioxidant drug, whose therapeutic efficacy is limited by its many drawbacks, such as fast metabolism, poor bioavailability and high physico-chemical instability. Alfa-lipoic acid derivatives have been recently developed demonstrating their neuroprotective activity and effectiveness in different types of oxidative stress. In this work, two derivatives containing an amide or an ester functional group with different lipophilicity, were selected for their important affinity for sigma-1 receptors. Herein, in order to improve the in vitro stability and antioxidant effectiveness of alpha-lipoic acid derivatives, we focused our efforts in the nanoencapsulation strategies. Aqueous-core nanocapsules for the delivery of the hydrophilic compound and nanostructured lipid carrier for the lipophilic derivative, were properly designed and prepared using a direct or inverse eco-friendly organic solvent-free procedure. All nanosystems were characterized in terms of mean size, polydispersity, stability, morphology, encapsulation efficiency and in vitro release profiles. In order to evaluate the nanocarriers biocompatibility and antioxidant effectiveness, in vitro biological studies (cell viability, total antioxidant capacity and total oxidative status) were developed on primary human whole blood cell cultures, on both unloaded and derivatives-loaded nanodevices. [ABSTRACT FROM AUTHOR]

Purpose: An optimized methodology for the development of a new generation of lipid nanoparticles, the multiple lipid nanoparticles (MLN) is described. MLN have characteristics between nanostructured lipid carriers (NLC) and multiple emulsions (W/O/W), but without the outer aqueous phase. Methods: The production is based on a hot homogenization method combined with high shear and ultrasonication. The antiretroviral agent lamivudine (3TC), was loaded in the MLN. For comparison purposes, NLC-3TC formulation was also developed and physico-chemically characterized by the same parameters as MLN-3TC. The development and optimization of MLN and NLC formulations were supported by a Quality by Design (QbD) approach. Results: The MLN-3TC formulation exhibited a size of about 450 nm, polydispersity <0.3 and negative zeta potential > −20 mV. Furthermore, the morphology assessed by TEM showed a structure with multiples aqueous vacuoles. MLN-3TC was physically stable for at least 45 days, had low cytotoxicity and drug release studies showed a sustained and controlled release of 3TC under gastric and plasma-simulated conditions (at pH 7.4 for about 45 h). Conclusions: The optimized formulations present suitable profiles for oral administration. Overall, the results reveal that MLN present higher loading capacity and storage stability than NLC. [ABSTRACT FROM AUTHOR]

This study aims at developing an optimised nanostructured lipid carrier (NLC) of lycopene for efficient absorption following oral administration. The optimised formulation showed an average particle size of 121.9 ± 3.66 nm, polydispersity index (PDI) 0.370 ± 0.97 and zeta potential −29.0 ± 0.83 mV. Encapsulation Efficiency (% EE) and drug loading (% DL) was found to be 84.50% ± 4.38 and 9.54% ± 2.65, respectively.In vitrorelease studies demonstrated the burst release within 4–9 h followed by sustained release over 48 h. The IC50value of lycopene extract and optimised NLC for ABTS+•were found to be 172.37 μg Trolox equivalent and 184.17 μg Trolox equivalent whereas, for DPPH•, 117.76 μg Trolox equivalent and 143.08 μg Trolox equivalent respectively.Ex vivostudies and MTT assay revealed that the NLC had better permeation and cause sufficiently more cytotoxicity as compared to drug extract due to higher bioavailability and greater penetration. [ABSTRACT FROM AUTHOR]

Purpose: Due to the antimicrobial property, menthol have significant potential for food preservation and foodstuff shelf life improvement. Nevertheless, menthol instability, insolubility, and rapid crystallization in aqueous media make it unsuitable for used in food products. This work was aimed to prepare menthol-loaded nanostructured lipid carriers (NLCs) to enhance its antimicrobial activity. Methods: Morphology, particle size and size distribution, encapsulation efficiency percent (EE%), and physical stability of the optimized formulation, prepared by hot melt homogenization method, were characterized by scanning electron microscopy, particle size analyzing, gas chromatography, and X-ray diffraction (XRD) methods. Minimum inhibitory concentration and minimum bactericidal concentration of menthol-loaded NLCs were evaluated and compared with conventional menthol emulsion against various Gram-positive (Staphylococcus aureus, Bacillus cereus) and Gram-negative bacteria (Escherichia coli), as well as one fungus (Candida albicans). Results: Menthol-loaded NLCs were spherically shaped nanosized (115.6 nm) particles with narrow size distribution (PDI = 0.2), suitable menthol EE% (98.73%), and appropriate physical stability after 90 days of storage period. XRD results indicated that menthol was in the amorphous form in the nanoparticles matrix. Antibacterial assay results revealed that the menthol-loaded NLCs exhibited significantly higher in vitro antimicrobial property than conventional menthol emulsion. The results also indicated that menthol-loaded NLCs had better effect on fungi than bacteria, and furthermore, antibacterial efficiency on Grampositive bacteria was higher than Gram-negative bacteria. Conclusion: In conclusion, NLCs could be a promising carrier for improvement of antimicrobial activity and preservation efficacy of essential oils in foodstuffs. [ABSTRACT FROM AUTHOR]