High Shear Homogenization Method Research Articles

Preparation of solid lipid nanoparticles and nanostructured lipid carriers containing zeaxanthin and evaluation of physicochemical properties

Zeaxanthin is a yellow carotenoid antioxidant concentrated in the macula. This pigment in many foods and beverages is very problematic due to its extreme hydrophobicity and poor chemical stability. Solid lipid nanoparticles (SLNs) and nanostructure lipid carriers (NLCs) were prepared using a combination of high shear homogenization and ultrasonic methods to load zeaxanthin and reduce its hydrophobicity. In this study, NLCs containing zeaxanthin were produced and optimal formulation was determined and their physicochemical properties were investigated. 20% percent of solid lipid was replaced with Medium-chain triglyceride (MCT) as a liquid lipid to produce NLCs. Results showed that the particle size (PS) of NLCs did not exceed 130 nm, but SLNs did show larger sizes. In addition, particle dispersion index (PDI) showed 0.23 ± 0.01 to 0.34 ± 0.01 and 0.23 ± 0.01 to 0.30 ± 0.01 for SLN and NLC, respectively. Zeta potential (ZP) represented −20.03 ± 0.48 to −12.11 ± 0.80 and −22.23 ± 0.41 to −16.88 ± 0.61 for SLN and NLC, respectively. Encapsulation efficiency and loading were higher for NLCs than SLNs. The morphological study of nanocarriers performed by scanning electron microscope (SEM) showed smooth spherical nanoparticles. Results of Fourier transform infrared spectroscopy (FTIR) analysis, and differential scanning calorimeter (DSC) showed that zeaxanthin was trapped in the nanocarriers without any chemical interaction with the coating material. Glycerol mono-stearate containing zeaxanthin showed phase separation after 60 days at 4 and 25 °C, while this was not observed in nanocarriers produced by glycerol distearate. Together, these nano-based carriers can be applied in many products, especially as nanocarriers for hydrophobic bioactive compounds in nutraceutical beverages.

Effect of rheological properties of catalyst slurry on the structure of catalyst layer in PEMFC

The dispersion process significantly influences the dispersion of catalyst slurry in proton exchange membrane fuel cells (PEMFCs). The particle size distribution and rheological properties of clusters in slurry directly affect the catalyst layer's coating state, surface morphology, and structure. This paper prepared four different catalyst slurries by high shear emulsification, homogenization, ball milling, and ultrasonic methods. The average particle sizes of clusters in slurry were 725, 337, 452, and 1098 nm, respectively. The rheological properties of catalyst slurry prepared by several dispersion processes are different. Amplitude scanning test demonstrates that yield stresses of slurries prepared by shear, homogenization, ball milling, and ultrasonic methods are 0.047, 0.185, 0.133, and 0.136 Pa, respectively. The viscosity of catalyst slurry is the lowest when prepared by the shear method and is the highest when prepared by the ultrasonic method, and the slurry prepared by homogenization and ball milling methods has the best thixotropy. By observing the catalyst layer, the slurry cluster prepared by the homogenization method has small particles, a strong network structure, and good thixotropy, producing a flat catalyst layer and fewer cracks. Electrochemical tests demonstrate that the catalyst layer with the smoothest surface morphology, the smallest cluster particles, and fewer cracks leads to higher polarization performance. The output voltage of the ink prepared by the homogenization method can reach 0.726 V under the condition of 1000 mA cm−2.

Formulation and Evaluation of Dolutegravir Sodium Nanoemulsion for the Treatment of HIV

The purpose of this research was to develop and evaluate the Nanoemulsion of Dolutegravir sodium. Nanoemulsion was made by the high-shear homogenization method. Materials and method: Oleic acid was used as the oil phase, Tween 80, and Acconon MC8-2 EP/NF (Smix; 1:1) were utilized as surfactant and co-surfactant respectively while distilled water was employed as an aqueous phase. The formulations were evaluated based on globule size, zeta potential, pH, viscosity, percentage transmittan

Comparison of the Release rate, Penetration and Physical stability of p-Methoxycinamic acid (PMCA) in Nanostructured Lipid Carriers (NLC), Solid Lipid Nanoparticle (SLN) and Nanoemulsion (NE) systems

Objective: The p-methoxycinnamic acid (PMCA) was known has antiinflamatory effect which is difficult to dissolve in water, to increase the penetration to the skin it’s was loaded in the nanostructured lipid carrier (NLC) delivery system used the combination of beeswax-cacao oleum and virgin coconut oil (VCO), compared with solid lipid nanoparticle (SLN) and nanoemulsion (NE) delivery systems. Material and Method: PMCA concentrations of 1% in each system were prepared by the high shear homogenization method, namely NLC-PMCA and SLN-PMCA; and was prepared by emulsification method namely NE-PMCA. Then all systems are characterized and tested for release rate, penetration into the rat skin, also were tested for physical stability. The results of this research: All systems have a pH value in the range of 4.2 - 4.5 which falls into the skin's pH range (4-6.5). The viscosity of the NLC-PMCA, SLN-PMCA and NE-PMCA systems are 30.03±6.29; 93.77± 6.11 and 3.43±0.16 cPs, respectively. The particle size of NLC-PMCA, SLN-PMCA and NE-PMCA are 423.6± 33.6; 830.7±71.3 and 57.1±1.6nm, respectively. The release rate of PMCA in the NLC-PMCA, SLN-PMCA and NE-PMCA system are 0.2210±0.0089; 0.1972±0.0145 and 0.4690±0.0228µg/cm2/minute, respectively. The depth of PMCA penetration in the NLC-PMCA, SLN-PMCA and NE-PMCA system at 30 minutes after application are 1173.0±37.8; 703.3±117.2; 1414.3±106.4µm, respectively and at 2 hours after application are 1268.8±111.9; 945.6±140.4; 1832.5±92.8μm, respectively. The NLC-PMCA has no physical changes in 14 days’ storage, whereas the SLN-PMCA consistency becomes thicker and the NE-PMCA becomes turbid. Conclusion: NLC-PMCA has better release rate and deeper penetration than SLN-PMCA, even though it is lower and shallower than NE-PMCA, but NLC-PMCA has better physical stability than SLN-PMCA and NE-PMCA.

Silibinin loaded Inhalable Solid lipid Nanoparticles for lung targeting

Aim: In the current study, efforts are being made to prepare Inhalable Silibinin loaded solid lipid nanoparticles (SLNs) with narrow size distribution with improved bioavailability. Methods: SLNs were formulated by high shear homogenization method SLNs were characterized, including Differential Scanning Calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), particle size analysis, entrapment efficiency with Aerodynamic behaviour.. The MTT assay was performed against A549 cell line, to measure their anticancer cell activity with Invio study. Results: Optimized formulation exhibited spherical surface with a mean particle size of 221 ± 1.251 nm, PI of 0.121 ± 0.081, zeta potential of -4.12 ± 0.744. Aerodynamic behaviour such as Mass median aerodynamic diameter (MMAD) and Geometric size distribution (GSD) were found to be 5.487 ± 0.072 and 2.321 ± 0.141 respectively proved formulation is suitable for inhalation. In vitro cellular efficacy against A549 cells, revealed that the optimized formulations were more effective and potent Conclusion: The Inhalable SLNs approach was successfully engineered and administered to the lungs safely without causing any problems.

Development, characterization in vitro and in silico of coenzyme Q10 loaded myristic acid with different liquid lipids nanostructured lipid carriers

Context: Nanostructured lipid carriers can enhance skin penetration of active substances. Coenzyme Q10 is a lipophilic antioxidant, that has poor skin penetration. This limitation is overcome by nanostructured lipid carriers. Aims: To developed coenzyme Q10 nanostructured lipid carriers using myristic acid with various liquid lipids as lipid matrix by in vitro studies and in silico approach for explaining the interaction of coenzyme Q10-lipid at the molecular level. Methods: The coenzyme Q10 nanostructured lipid carriers were prepared using myristic acid as solid lipid with oleic acid, isopropyl myristate, and isopropyl palmitate as liquid lipids using the high shear homogenization method. Then, they were evaluated in physicochemical characteristics by dynamic light scattering, differential scanning calorimetry, Fourier transforms infrared, scanning electron microscopy, spectrophotometry ultraviolet-visible, and pH meter. Furthermore, the in silico studies were conducted using AutoDock 4.2. Results: The coenzyme Q10 nanostructured lipid carriers using myristic acid-oleic acid, myristic acid-isopropyl myristate, and myristic acid-isopropyl palmitate as lipid matrix had the mean particle size, polydispersity index, entrapment efficiency, drug loading, and pH value were less than 300 nm, less than 0.3, more than 80%, about 10%, and about 5.0, respectively. Moreover, molecular docking of coenzyme Q10 and lipid showed hydrogen and hydrophobic bonds. These results supported differential scanning calorimetry and Fourier transforms infrared results. Conclusions: The coenzyme Q10 nanostructured lipid carriers were successfully prepared using myristic acid-oleic acid, myristic acid-isopropyl myristate, and myristic acid-isopropyl palmitate as lipid matrix as well as in silico study could be used for explaining of coenzyme Q10-lipid interaction.

Licochalcone A-loaded solid lipid nanoparticles improve antischistosomal activity in vitro and in vivo.

Aim: To isolate licochalcone A (LicoA) from licorice, prepare LicoA-loaded solid lipid nanoparticles (L-SLNs) and evaluate the L-SLNs in vitro and in vivo against Schistosoma mansoni. Materials & methods: LicoA was obtained by chromatographic fractionation and encapsulated in SLNs by a modified high shear homogenization method. Results: L-SLNs showed high encapsulation efficiency, with satisfactory particle size, polydispersity index and Zeta potential. Transmission electron microscopy revealed that L-SLNs were rounded and homogenously distributed. Toxicity studies revealed that SLNs decreased the hemolytic and cytotoxic properties of LicoA. Treatment with L-SLNs showed in vivo efficacy against S. mansoni. Conclusion: L-SLNs are efficient in reducing worm burden and SLNs may be a promising delivery system for LicoA to treat S. mansoni infections.

Statistical Optimization Amalgamated Approach on Formulation Development of Nano Lipid Carrier Loaded Hydrophilic Gel of Fluticasone Propionate

Abstract: Introduction: Formulation of a nano lipid carrier loaded hydrophilic gel of a corticosteroid, fluticasone propionate (FP) was investigated systemically with response surface model (RSM) for promising dermal delivery of the drug. Objectives: To achieve a better penetration of the drug and to overcome the generally associated adverse reactions of corticosteroids, the present study, explored the formulation and evaluation of nano lipid carriers (NLCs) of FP in a hydrophilic gel base. Methods: A central composite design was proposed to study the effect of processing materials on the physicochemical properties of the NLC. High shear homogenization method with stearic acid, isopropyl myristate and poloxamer 407 was used to make different batches of FP-NLCs. The model was optimized at a significance level of P<0.05. FTIR, DSC and surface morphology studies were carried out for the optimized product. The optimized product was incorporated in the Carbopol P940 gel base and was evaluated for its mechanical and rheological properties, ex-vivo permeation and skin irritation study. Results: It was observed that using the proposed model, a nano size (179 nm) stable (Zeta potential -26 mV) optimized product of FP-NLC with 85% entrapment efficiency was achieved. The nanogel exhibited a spreadability of 4.2 gm.cm/sec and a viscosity of 92.6 cp. Approximately 3.5 times improvement in ex-vivo permeation and no skin irritations on animals were reported on application of the nanogel of FP. Conclusion: Hence the investigation created a paradigm to explore the efficacy of nanogel of FP for dermal application with improved permeation and promising therapy for dermatitis. Key words: Fluticasone propionate, Niosome, Central composite design, Gel, Ex-vivo permeation.

Novel Curcumin-Resveratrol Solid Nanoparticles Synergistically Inhibit Proliferation of Melanoma Cells.

Polyphenols such as curcumin (Cur) and resveratrol (Res) have been recently shown to have potential to inhibit proliferation of highly aggressive melanoma cells. This study was designed to investigate the feasibility of a topical delivery system, using a solid lipid nanoparticles (SLNs) loaded delivery systems, that can enhance the skin penetration and anti-cancer efficacy of combination of these polyphenols. Negatively charged Cur-Res SLNs with a mean diameter of 180.2 ± 7.7nm were prepared using high shear homogenization method. Cur-Res SLNs were found to be stable up to 2weeks under 4°C. The in vitro release study showed that Res was released five time more than curcumin. The permeability of resveratrol was about 1.67 times that of curcumin from the SLN-gel formulation which was significantly (p < 0.05) lower than from SLN suspension. More than 70% of Cur-Res SLNs were bound to skin locally in a skin binding study suggesting potentially utility of Cur-Res SLNs in the treatment of localized melanoma. In fact, the electrical cell-substrate impedance sensing (ECIS) measurements suggested that Cur-Res combination has potential to stop cell migration of B16F10 melanoma cells. Furthermore, both, Cur-Res SLNs and Cur-Res solution at the ratio of 3:1 demonstrated a strong synergistic inhibition of SK-MEL-28 melanoma cell proliferation. Further evaluation of Cur-Res SLNs in vivo melanoma models are warranted to establish the clinical utility of Cur-Res formulations in melanoma therapy.

Preparation of Casein Biopeptide-Loaded Niosomes by High Shear Homogenization and Their Characterization.

The aim of this study was to develop a niosomal system to deliver milk bioactive peptides with potential for enhanced bioavailability. Milk casein was hydrolyzed with Flavourzyme, and the hydrolysates were ultrafiltered to obtain low-molecular-weight peptides with enhanced antioxidant activity. Biopeptide-loaded niosomes were prepared by a high shear homogenization method. Peptide-loaded niosomes exhibited a mean particle size of 37.64 ± 0.98 nm with narrow size distribution (PDI = 24.66 ± 0.008%) and high zeta potential (-23.36 mV). The niosomes encapsulated about 67% of peptides into the vesicles and showed controlled and sustained release under simulated gastrointestinal conditions as compared to free peptides. The antioxidant activity of the peptides was not affected due to their encapsulation into niosomes. Morphology of peptide-loaded niosomes was determined by scanning electron microscopy, transmission electron microscopy and atomic force microscopy, and the microstructural interactions analyzed by Fourier transform infrared clearly indicated the formation of peptide-loaded niosomes. High-performance liquid chromatography spectra of peptides in the niosomes and the free peptides were similar, thus confirming their entrapment into the niosomes.

EXPERIMENTAL DEVELOPMENT AND MOLECULAR DOCKING: NANOSTRUCTURED LIPID CARRIERS (NLCs) OF COENZYME Q10 USING STEARIC ACID AND DIFFERENT LIQUID LIPIDS AS LIPID MATRIX

Objective: To develop coenzyme Q10 (co-Q10) nanostructured lipid carriers (NLCs) using stearic acid (SA) and various liquid lipids with different lipophilicity as well as highlights the use of in silico studies for predicting and elucidating the interaction of drug-lipid used as carries in NLCs, at the molecular level.&#x0D; Methods: The co-Q10 NLCs were prepared using SA as solid lipid and oleic acid (OA), isopropyl myristate (IPM), as well as isopropyl palmitate (IPP) as liquid lipids by the high shear homogenization method. Firstly, the formulas were optimized by the appropriate required HLB (rHLB). The optimized NLCs were characterized in the particle size, distribution of particle size, zeta potential, crystallinity behavior, Fourier transform infrared (FT-IR) spectra, morphology, entrapment efficiency (EE), drug loading (DL), and pH value. The interaction of drug-lipids in silico was studied using the AutoDock Vina program.&#x0D; Results: The co-Q10 NLCs using SA and the various liquid lipid possessed the mean particle size, polydispersity index (PDI), zeta potential, EE, DL, and pH values were 180 to 350 nm,&lt;0.5,&lt;-30 mV, 83 to 88%, 10 to 11%, and 5.0 to 5.6, respectively. The EE and DL of co-Q10 NLCs increased with decreasing in binding energy (∆G) in silico.&#x0D; Conclusion: The co-Q10 NLCs using SA as solid lipid and OA, IPM, as well as IPP as liquid lipids were developed successfully. Furthermore, in silico study by molecular docking is a potential approach in predicting and elucidating the interaction of drug-lipid in the development of NLCs formulation.

Nanostructured lipid carriers as a strategy for encapsulation of active plant constituents: Formulation and in vitro physicochemical characterizations

Active plant constituents obtained from edible sources have manifested their pharmacological potential as a therapy against several diseases. But the lack of their desired physicochemical properties such as solubility, permeability ultimately leads to poor bioavailability. Two potent active plant constituents namely, quercetin and piperine having a problem with either solubility or permeability or both, and hence require an advanced lipid-mediated separate formulation system to improve their aforementioned concerns. Concerning advancement in nanoformulations, lipid-based nano-carriers systems have created their mark as a novel drug delivery system. Therefore, an advanced formulation like nanostructured lipid carriers (NLCs) has been formulated individually for both the active plant constituents/drugs through the solvent evaporation technique using high shear homogenization method followed by sonication. Compritol® 888 ATO, a solid lipid, and squalene as liquid lipid was used in their optimized ratios to formulate individual NLCs. Blank and individual drugs loaded NLCs were further characterized for their in vitro physicochemical properties. NLCs showed a negative surface charge with an average particle size below 200 nm. Electron microscopy images showed an anomalous structure of both the formulated NLCs with higher % drug encapsulation efficiency (DEE) with the desired in vitro drug release profile. In the case of quercetin-NLCs, 93.18 ± 5.5 % DEE was observed followed by drug release up to 45.0 ± 1.3 % within 12 h, while piperine-NLCs showed 91.80 ± 2.51 % DEE and drug release up to 38 ± 5.2 % at the same time. XRD and DSC plots showed the conversion of both the drugs into an amorphous structure encapsulated in a lyophilized NLCs matrix. Finally, the safety profile for formulated NLCs was confirmed by haemolysis assay. Hence, the developed active plant constituents enriched NLCs can further be delivered separately and/or in combination, and also may further be evaluated both in vitro and in vivo means.

Preparation of Ethanolic Butterfly Pea Extract Using Microwave Assisted Extraction and Loaded Nanostructured Lipid Carriers: Evaluation of Antioxidant Potential for Stabilization of Fish Oil

Fresh whole flowers of the butterfly pea were extracted with 95% ethanol and analyzed the antioxidant activity. The total phenolic content (TPC) of butterfly pea ethanolic extract (BE) was 26.90±1.12 mg gallic acid equivalents/g of dry weight and radical DPPH scavenging activity of ethanolic extract was. The ethanolic extract-loaded Nanostructured Lipid Carriers called BE-NLC were prepared by the high shear homogenization method using compritol 888 ATO, miglyol oil, poloxamer 188, extract and tween 80, respectively. Particle size, polydispersity index, zeta potential 27.78±0.12 mg Trolox equivalents/g of dry weight and entrapment efficiency (EE) were determined. The morphology of the BE-NLC was spherical. The entrapment efficiency of extract was 72.51±1.11% in NLC system. Antioxidant activity was evaluated by the estimation of peroxide values (PVs) of fish oil from catfish, treated with natural antioxidant (BE and BE-NLC) and compared with butylated hydroxy toluene (BHT) as synthetic antioxidant by incubating at 65 °C for a period of 12 days. BHT was found to have higher antioxidant activity than BE and BE-NLC in fish oil. Treatment containing BE-NLC and BHT in fish oil showed similar PVs after the 4 days. However, the antioxidant activity of BE-NLC in stabilization of fish oil is higher than that of BE.

Targeting Solid Lipid Nanoparticles with Anisamide for Docetaxel Delivery to Prostate Cancer: Preparation, Optimization, and In-vitro Evaluation.

The purpose of the current study was to prepare and characterize the targeted solid lipid nanoparticles (SLNs) containing docetaxel (DTX) for prostate cancer treatment. The goal has been achieved by locating anisamide (Anis) ligand on the surface of SLNs, which can interact with the overexpressed sigma receptor on the prostate cancer cells. DTX loaded SLNs were prepared by high shear homogenization and ultra-sonication method and optimized by applying experimental design. The average particle size and the entrapment efficiency of the optimum DTX-SLN were 174 ± 9.1 nm and 83 ± 3.34%, respectively. The results of differential scanning calorimetry showed that DTX had been dispersed as amorphous in the nanocarriers. Scanning electron microscopy (SEM) images confirmed the nanoscale size and spherical shape of the nanoparticles. The cytotoxicity studies have demonstrated that IC50 of free drug, DTX-SLN and DTX-SLN-Anis was 0.25 ± 0.01, 0.23 ± 0.02, 0.12 ± 0.01 nM on PC3 cell line and 20.9 ± 3.89, 18.74 ± 7.43, and 14.68 ± 5.70 nM on HEK293 cell line, respectively. Targeted DTX-SLN-Anis was acted more effectively on prostate cancer cells in comparison to DTX-SLN and free drug. The results of this study have depicted that the anti-cancer drug loaded in targeted SLNs can be a promising way for cancer treatment. In addition, performing in-vivo studies will be complementary to these findings.

Valsartan solid lipid nanoparticles integrated hydrogel: A challenging repurposed use in the treatment of diabetic foot ulcer, in-vitro/in-vivo experimental study

The article presents an experimental study on the possible repurposed use of valsartan (Val), in the local treatment of uncontrolled diabetic foot ulcer. Solid lipid nanoparticles (SLN), loaded with Val were prepared by applying 32 full factorial design using modified high shear homogenization method. The lipid phase composed of Precirol® ATO 5 (P ATO 5) and/or Gelucire 50/13 (G 50/13) in different ratios and a nonionic emulsifier, Pluronic 188 (P188), was used in different percentages. Optimized formulation was further integrated in hydroxyl propyl methyl cellulose (HPMC) gel for the ease of administration. In-vitro and in-vivo characterizations were investigated. The prepared nanoparticles showed small particle size, high entrapment efficiency and sustained drug release. Microbiologically, Val-SLN showed a prominent decrease in the biofilm mass formation for both gram-positive and gram-negative bacteria, as well as a comparable minimum inhibitory concentration level to levofloxacin alone. Diabetes was induced in 32 neonatal Sprague-Dawley rats. At 8 weeks of age, rats with blood sugar level >160 were subjected to surgically induced ulcer. Treatment with Val-SLN for 12 days revealed enhanced healing characteristics through cyclooxygenase-2 (COX-2), nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB), nitric oxide (NO), transforming growth factor-beta (TGF-β), matrix metalloproteinase (MMPs) and vascular endothelial growth factor (VEGF) pathways. Histological examination revealed re-epithelization in Val-SLN treated ulcer, as well as decrease in collagen using trichrome histomorphometric analysis.

PENGAMBANGAN SISTEM NANOSTRUCTURED LIPID CARRIER (NLC) DAUN Chrysanthemum cinerariifolium (Trev.) Vis DENGAN VARIASI KONSENTRASI LIPID

Ethanol extract 96% of Chrysanthemum cinerariifolium (Trev.) Vis leaves are proven to have anticancer activity. However, these compounds have low solubility in water and fat. To improve the bioavailability of preparations, the development of drug design in the form of Nanostructured Lipid Carrier (NLC) is carried out.The aim this study was to determine the effect of differences in lipid concentration of Monostearin and Oleic Acid in the formulation of the NLC system of Chrysanthemum cinerariifolium (Trev.) Vis leaves, which produced good physicochemical characteristics including organoleptic characteristics, pH, viscosity, particle size, and drug entrapment efficiency. Making is done using the High Shear Homogenization method. Organoleptic tests showed ideal results for the Nanostructured Lipid Carrier (NLC) system, the resulting pH values in formula 1 (7.0 ± 0.12), formula 2 (6.7 ± 0.17) and formula 3 (6.8 ± 0.2)), the viscosity value of formula 1 (55.66 ± 2.84 cPs), formula 2 (28.86 ± 3.91 cPs), and formula 3 (28.57 ± 16.85 cPs). Particle size of formula 1 (5530 ± 320.47 nm), formula 2 (5337 ± 671.44 nm) and formula 3 (4676 ± 2215.75 nm)). The entrapment efficiency value of formula 1 drugs (33.55%), formula 2 (38.77%), formula 3 (83.75%). Based on the characterization result, the best formula was obtained at a lipid concentration of 10%, which was used for the formula of the NLC system of Chrysanthemum cinerariifolium (Trev.) Vis leaves for oral anticancer preparations

Rifampin and Cis-2-Decenoic Acid Co-entrapment in Solid Lipid Nanoparticles as an Efficient Nano-system with Potent Anti-biofilm Activities

This study was performed to explore the physicochemical and anti-biofilm properties of rifampin (Rif) and cis-2-decenoic acid (C2DA) co-entrapped in solid lipid nanoparticles, Rif-C2DA-SLN, against staphylococcal biofilm. The formulation was prepared by high-shear homogenization and ultrasound methods and characterized for size, zeta potentials, encapsulation efficacy, drug lipid interaction studies (DSC), shape morphology (TEM), stability studies, and in vitro anti-biofilm activity against Staphylococcus aureus and S. epidermidis biofilm. The zeta potentials, particle sizes, and encapsulation efficacy of final formulations were 19.0 ± 7.64 mV, 127.2 ± 2.8 nm, and approximately 69% (Rif) and 46% (C2DA), respectively. SLN formulations were stable for 12 months. DSC studies showed no chemical interaction between drugs and lipids. SLN formulations showed better in vitro anti-biofilm activity than free forms especially in the stage of biofilm formation. Nanoparticles were not able to remove the formed biofilm. Simultaneous entrapment of Rif and C2DA by SLN is reported for the first time, and Rif-C2DA-SLN can be applied as an efficient nanoparticulate system with potential anti-biofilm activities. These data suggest that the combined strategies for delivery of both C2DA and Rif by nanoparticulate systems would pave the way toward developing the strategies to combat biofilms.

Moisturizing effects of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) using deionized and magnetized water by in vivo and in vitro methods.

Objective(s):The present study aimed to determine and compare moisturizing and occlusion effects of different solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) using magnetized water and deionized water.Materials and Methods:SLN formulations were prepared using various lipids, including Tripalmitin, Compritol®, Precirol®, and emulsifiers including Poloxamer and Tween 80. NLC formulations were also prepared with oleic acid and the same solid lipids. Two types of formulations were prepared; first with deionized water and then with magnetized water. Formulations were prepared using high shear homogenization and ultrasound methods. The products were analyzed by PSA (particle size analyzer), DSC (differential scanning calorimetry), and TEM (transmission electron microscopy). The moisturizing effect of formulations was determined by in vivo and in vitro methods. Results:Findings of the assessments demonstrated that in products prepared with magnetized water, 5% SLN Precirol® had the most moisturizing effect in vivo and 5% SLN Compritol® had the most moisturizing effect in vitro. The use of magnetized water in formulations can improve the effectiveness and increase the stability of moisturizing products.Conclusion:In this study, all products prepared with magnetized water showed more stability, smaller size, and more moisturizing effects compared with products prepared with deionized water.

Effect of nanostructured lipid carriers on transdermal delivery of tenoxicam in irradiated rats

Transdermal delivery of non-steroidal anti-inflammatory drugs (NSAIDs) is an effective route of drug administration, as it directs the drug to the inflamed site with reduced incidence of systemic adverse effects such as gastric hemorrhage and ulcers. Tenoxicam (TNX) is a member of NSAIDs that are marketed only as oral tablets due to very poor absorption through the skin. The current study intended to formulate and characterize a hydrogel loaded with nanostructured lipid carriers (NLCs) to enhance the transdermal delivery of TNX. Six formulations of TNX were formulated by slight modifications of high shear homogenization and ultrasonication method. The selected formula was characterized for their particle size, polydispersity index (PDI), zeta potential, entrapment efficiency (EE), in-vitro drug release and ex-vivo skin permeation studies. Moreover, the effectiveness of the developed formula was studied in-vivo using carrageenan-induced paw edema and hyperalgesia model in irradiated rats. Formula F4 was chosen from six formulations, as the average diameter was 679.4 ± 51.3 nm, PDI value of about 0.02, zeta potential of −4.24 mV, EE of 92.36%, globules nanoparticles without aggregations and absence of interactions in the developed formula. Additionally, the in-vivo study showed the efficacy of formula F4 (TNX-NLCs hydrogel) equivalent to oral TNX in reducing the exaggerated inflammatory response induced by carrageenan after irradiation. In conclusion, the present findings suggest that TNX-NLCs hydrogel could be a potential transdermal drug delivery system alternative to the oral formulation for the treatment of various inflammatory conditions.

Sea buckthorn extract loaded into solid lipid nanoparticles

The sea buckthorn extract used for this study was obtained from dry sea buckthorn berries. The aim of this study was to synthesize by high shear homogenization method and to characterize new solid lipid nanoparticles loaded with sea buckthorn extract, nanoparticles which show high antioxidant activity. The obtained solid lipid nanoparticles have been firstly characterized by particle diameter and physical stability using dynamic light scattering method. The particle morphology was examined by transmission electron microscopy and the properties of sea buckthorn extract-loaded nanoparticles have been evaluated by an appropriate in vitro analysis (chemiluminescence method). The antimicrobial properties of newly developed nano-materials were also evaluated.