Properties Of Solid Lipid Nanoparticles Research Articles

Effect of alginate coating activated by solid lipid nanoparticles containing Zataria multiflora essential oil on chicken fillet’s preservation

The current study aimed to assess the chemical, microbial, and sensory properties of Solid Lipid Nanoparticles (SLNs) in chicken fillets stored at 4 ± 1 °C for 12 days. As a result, the optimized ZEO-SLNS sample exhibited a spherical morphology with a droplet size of 251.51 ± 1.11 nm and a PDI of 0.34 ± 0.01 under transmission electron microscopy (TEM). The encapsulation efficiency (EE) and zeta potential were approximately 55.4 % and −20.87 ± 1.39 mV, respectively. Furthermore, encapsulating ZEO in SLNS enhanced antibacterial and antioxidant activity compared to pure ZEO. As a result, the application of alginate-loaded ZEO-SLNS extended the storage time of fresh chicken fillets. Thus, the application of this edible coating showcased a remarkable ability to substantially decelerate both microbial and chemical changes in chicken fillets during cold storage conditions. This finding underscores the potential of the edible coating as an effective means to enhance the safety and quality of chicken products.

Enhanced stability and skin permeation of ibuprofen-loaded solid lipid nanoparticles based binary solid lipid matrix: Effect of surfactant and lipid compositions

HypothesisThe type of emulsifier selected has an impact on the physicochemical properties of solid lipid nanoparticles (SLNs). This study was designed to compare the effects of emulsifiers on the physicochemical properties and in vitro skin performance of SLNs prepared from a binary mixture of Softisan® 378 (S378) and cetyl palmitate (CP) to those of SLNs prepared from only CP and S378. ExperimentsSLNs were prepared from CP, S378, or a binary mixture of CP and S378 (1:1 w/w) as the lipid phase and stabilized with Tego®Care 450 (TG450) or poloxamer 188 (P188) containing 1.0% w/w ibuprofen loading. The physicochemical properties including the particle size, polydispersity index (PDI), zeta potential (ZP), encapsulation efficiency (E.E.), crystallinity (%CI), and polymorphism were determined after production and after storage for 180 days under different conditions. In addition, in vitro drug release and permeation through human skin was studied after production and storage at room temperature for 180 days. FindingThe particle sizes of ibuprofen-loaded SLNs (IBSLNs) stabilized with P188 (IBSLN-P188) were smaller than those of SLNs stabilized with TG450 (IBSLN-TG450) (p < 0.05). After 180 days, the particle sizes of the IBSLNs were slightly increased compared to those at the initial time but were <250 nm. The IBSLN-TG450 sample showed a higher %CI than IBSLN-P188 prepared with similar propotions of CP and S378, and ibuprofen crystals were observed in the IBSLN1-TG450 sample after storage at 4 °C for 180 days. Based on the result of the in vitro release study and the in vitro skin permeation test, the addition of S378 into the CP-matrix modified ibuprofen release and skin permeation both permeated ibuprofen through the epidermis and retained ibuprofen in the epidermis. In addition, the storage time affected the release and skin permeation of ibuprofen from the SLNs, which depended on the composition of the IBSLNs.

Influence of Lipid Type and Storage Conditions on the Properties of Solid Lipid Nanoparticles Containing Peppermint Essential Oil

Influence of Lipid Type and Storage Conditions on the Properties of Solid Lipid Nanoparticles Containing Peppermint Essential Oil

Surface structural characteristics of some colloidal lipid systems used in pharmaceutics

Surface properties of solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC), and nanoemulsions (NE) are determinant to understand their structural characteristics and their behavior as drug delivery systems; however, there is still limited knowledge in this respect. As a contribution, this paper reports the study of some surface properties of these colloidal systems which were prepared with binary mixtures of trimyristin and medium-chain triglycerides (MCT) and stabilized with Poloxamer 188 (P188). Particle sizes and polydispersity indexes decrease in the order SLN > NLC > NE suggesting that the addition of MCT to trimyristin reduces the particle asymmetry. ζ potentials range from −6 mV to −10 mV and the P188 layer is ~20 nm; thus, steric stabilization seems to predominate. The amount of P188 on the surface of the drops in the NE was less than that on the surface of the particles in the SLN and NLC and decreases as the proportion of MCT decreases. Finally, depending on the physical state of the lipid matrix, hydrophobic molecules could be adsorbed on the particle surface and located at the interface between the particle and the P188 layer or absorbed inside the matrix.

SOLID LIPID NANOPARTICLES (SLNs) AS NANO DRUG DELIVERY CARRIERS: PREPARATION, CHARACTERIZATION AND APPLICATION

Over the last few years, there has been a significant consideration of solid lipid nanoparticles (SLNs) as an alternative method to other colloidal dispersion methods for drug delivery. Special consideration has been given to the use of SLNs as a drug carrier in recent years. SLNs are aqueous dispersions in which the colloidal particles consist of solid lipids that are biodegradable. As a result of their physical stability, the protection of the entrapped drug from decomposition, the provision of controlled drug release, and the exceptional acceptability, SLNs have several advantages over other drug carriers. This article focuses on the techniques of SLNs preparation and characterization, the effect of formulation variables on SLNs properties, the routes of administration, and the pharmaceutical applications. The data used for this review was collected by searching on Google Scholar and PubMed using the following keywords during the period from 2010 to date.

Development and characterization of solid lipid nanoparticles (SLNs) made of cocoa butter: A factorial design study

The present study is motivated by the development of solid lipid nanoparticles (SLNs) for food applications. A focus of the study is the use of a factorial design to optimize the preparation variables. SLNs were prepared by hot homogenization at 60 °C. Cocoa butter was used to form the lipid core and the surfactant blend used to emulsify and stabilize the system was a mixture of sodium stearoyl-2-lactylate (SSL) and mono- and diglycerides of fatty acids (MDG). The particle characteristics and stability of obtained SLN-suspensions were investigated. Moreover, the effect of various cooling conditions on the properties of SLNs and the storage stability during a period of three months were examined. Results proved that cocoa butter is suitable to prepare SLNs with a food-grade quality where the optimized preparation variables resulted in a particle size of 112.7 nm.

Effect of binary solid lipid matrix of wax and triglyceride on lipid crystallinity, drug-lipid interaction and drug release of ibuprofen-loaded solid lipid nanoparticles (SLN) for dermal delivery

HypothesisThe physicochemical properties of solid lipid nanoparticles (SLN) depend on lipid compositions. An addition of secondary solid complex triglycerides (Softisan 378; S378) into solid wax (cetyl palmitate; CP) is expected to influence the properties of obtained SLN compared to SLN prepared from sole CP. ExperimentsIbuprofen-loaded SLN (IBSLN-TG) composed of different ratios of CP and S378 were prepared and evaluated in term of size, zeta potential (ZP), entrapment efficiency (E.E.), crystallinity, lipid-drug interaction and in vitro drug release. FindingsAfter production, all developed IBSLN-TG prepared from different ratios of CP and S378 had the particle size in the nanometer range (180–200nm) with the ZP values of higher than |−40mV| and possessed approximately 100% E.E. The release of IBSLN-TG demonstrated the biphasic pattern with a fast release followed by sustained release, which was fitted to Higuchi’s kinetics. The addition of S378 into CP-matrix led to a slight decrease in particle size and surface charge, and distortion of CP crystallization. The results from 1H-NMR indicated the formation of tiny liquid S378 nanocompartments within CP-matrix. The localization of ibuprofen in the S378 nanocompartments and the interaction between ibuprofen and S378 had an impact on the release profiles of IBSLN-TG depending on the ratios of CP and S378.

Acyclovir Loaded Solid Lipid Nanoparticle Based Cream: A Novel Drug Delivery System

Objective of the present investigation was enthused by the possibility to develop solid lipid nanoparticles (SLNs) of hydrophilic drug acyclovir. Also study vitro and vivo drug delivery. Methods: Drug loaded SLNs (ACV-SLNs) were prepared by high pressure homogenization of aqueous surfactant solutions containing the drug-loaded lipids in the melted or in the solid state with formula optimization study (Different lipid concentration, drug loaded, homogenization / stirring speed and compritol 888ATO: drug ratio). ACV - SLN incorporated in cream base. The pH was evaluated and rheological study. Drug release was evaluated and compared with simple cream- drug, ACV – SLN with compritol 888ATO and marketed cream. The potential of SLN as the carrier for dermal delivery was studied. Results: Particle size analysis of SLNs prove small, smooth, spherical shape particle ranged from 150 to 200 nm for unloaded and from 330 to 444 nm for ACV loaded particles. The EE% for optimal formula is 72% with suitable pH for skin application. Rheological behavior is shear thinning and thixotropic. Release study proved controlled drug release for SLNs especially in formula containing compritol88 ATO. Stability study emphasized an insignificant change in SLNs properties over 6 month. In-vivo study showed significantly higher accumulation of ACV in stratum corneum, dermal layer, and receptor compartment compared with blank skin. Conclusion: AVC-loaded SLNs might be beneficial in controlling drug release, stable and improving dermal delivery of antiviral agent(s).

Development of a nanogel formulation for transdermal delivery of tenoxicam: a pharmacokinetic–pharmacodynamic modeling approach for quantitative prediction of skin absorption

This study investigates potentials of solid lipid nanoparticles (SLN)-based gel for transdermal delivery of tenoxicam (TNX) and describes a pharmacokinetic–pharmacodynamic (PK–PD) modeling approach for predicting concentration–time profile in skin. A 23 factorial design was adopted to study the effect of formulation factors on SLN properties and determine the optimal formulation. SLN-gel tolerability was investigated using rabbit skin irritation test. Its anti-inflammatory activity was assessed by carrageenan-induced rat paw edema test. A published Hill model for in vitro inhibition of COX-2 enzyme was fitted to edema inhibition data. Concentration in skin was represented as a linear spline function and coefficients were estimated using non-linear regression. Uncertainty in predicted concentrations was assessed using Monte Carlo simulations. The optimized SLN was spherical vesicles (58.1 ± 3.1 nm) with adequate entrapment efficiency (69.6 ± 2.6%). The SLN-gel formulation was well-tolerated. It increased TNX activity and skin level by 40 ± 13.5, and 227 ± 116%, respectively. Average Cmax and AUC0–24 predicted by the model were 2- and 3.6-folds higher than the corresponding values computed using in vitro permeability data. SLN-gel is a safe and efficient carrier for TNX across skin in the treatment of inflammatory disorders. PK–PD modeling is a promising approach for indirect quantitation of skin deposition from PD activity data.

Enhancement of stability and controlled drug release of lipid nanoparticles by modified solvent-evaporation method

The purpose of this study was to improve the physicochemical properties of solid lipid nanoparticles (SLNs) by modified solvent-evaporation methods. Stearylamine, Tween 80, egg phosphatidylcholine, and docetaxel were used to prepare SLNs. In the conventional method, the lipid is heated to 5–10°C above its melting point; however, the samples prepared using the modified method were heated to twice the lipid melting point. The particle size, polydispersity index (PdI), and zeta potentials were measured to compare the physicochemical characteristics of SLNs prepared using the conventional and modified methods. The morphologies of the SLNs were observed using scanning electron microscopy (SEM) and the crystal forms confirmed using DSC thermograms. The aqueous stability of the SLNs was evaluated by examining changes in mean particle size and polydispersity during storage at 4°C. An in vitro drug release test was conducted to study the release patterns of each SLN formulation. mSLN particles were smaller and more uniform than those of cSLNs in dynamic light-scattering (DLS) and SEM measurements. The particle size and PdI were 321±15.5nm, 0.208±0.0208 for mSLNs and 403.2±24.7nm, 0.486±0.0138 for cSLNs, respectively. The zeta potentials of mSLNs and cSLNs were +26.2±2.01 and +24.1±0.83, respectively. Docetaxel was incorporated in both SLNs with about 80% encapsulation efficiency. Mean particle diameters and PdI of mSLNs were maintained throughout the observation period. However, in cSLNs, extensive particle growth and gelation were observed when the cSLNs were stored at 4°C. The in vitro drug release test showed that mSLNs had a more sustained release pattern. In conclusion, the stability and controlled drug release of SLNs can be enhanced by fabrication using modified solvent-evaporation methods.

Effect of liquid-to-solid lipid ratio on characterizations of flurbiprofen-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for transdermal administration

The aim of this study is to evaluate the effect of liquid-to-solid lipid ratio on properties of flurbiprofen-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), and to clarify the superiority of NLCs over SLNs for transdermal administration. Particle size, zeta potential, drug encapsulation efficiency, in vitro occlusion factor, differential scanning calorimetry, X-ray diffractometry, in vitro percutaneous permeation profile, and stability of SLNs and NLCs were compared. Particle size, zeta potential, drug encapsulation efficiency, in vitro occlusion factor, and in vitro percutaneous permeation amount of the developed NLCs were all <200 nm, < −20 mV, >78%, >35, and >240 μg/cm2, respectively, however, for SLNs were 280 nm, −29.11 mV, 63.2%, 32.54, and 225.9 μg/cm2, respectively. After 3 months storage at 4 °C and 25 °C, almost no significant differences between the evaluated parameters of NLCs were observed. However, for SLNs, particle size was increased to higher than 300 nm (4 °C and 25 °C), drug encapsulation efficiency was decreased to 51.2 (25 °C), in vitro occlusion factor was also decreased to lower than 25 (4 °C and 25 °C), and the cumulative amount was decreased to 148.9 μg/cm2 (25 °C) and 184.4 μg/cm2 (4 °C), respectively. And DSC and XRD studies indicated that not only the crystalline peaks of the encapsulated flurbiprofen disappeared but also obvious difference between samples and bulk Compritol® ATO 888 was seen. It could be concluded that liquid-to-solid lipid ratio has significant impact on the properties of SLNs and NLCs, and NLCs showed better stability than SLNs. Therefore, NLCs might be a better option than SLNs for transdermal administration.

Shea butter solid nanoparticles for curcumin encapsulation: Influence of nanoparticles size on drug loading

In the present work, shea butter solid lipid nanoparticles (SLN) were prepared by sonication using nonionic surfactants as stabilizers without organic solvent. The mixture design methodology enabled to control particles size from 50 nm to more than 1 μm according to the mixture composition. Then, curcumin, a natural polyphenol, has been encapsulated in nanoparticles with a wide range of diameters (50–230 nm) and the encapsulation efficiency has been related to the particles sizes. The bigger the nanoparticles, the lower the encapsulation efficiency. The lipid structure at non dispersed state and under SLN form has been studied by differential scanning calorimetry and X‐ray diffraction. From the obtained results, encapsulated curcumin did not affect the lipid properties at the SLN state unlike at non dispersed state. The localization of the curcumin in the outer shell of the lipid nanoparticles explained the evolution of the encapsulation efficiency according to the nanoparticles size.Practical applications: Solid lipid nanoparticles (SLN) can be used for the delivery of both hydrophobic and hydrophilic drugs. Preparing such nanovectors with natural, non‐expensive materials and easily available (i.e., shea butter) will promote their potential use in several applications like oral, parenteral, dermal or ocular delivery. Controlling the particles size from the formulation composition and also the drug loading from SLN properties is of main importance to optimize the use of SLN as colloidal carrier.Mixture design of experiments methodology allowed the control of shea butter solid lipid nanoparticles size upon system composition. The influence of SLN size on the encapsulation efficiency of curcumin was studied.

Comparison of solid lipid nanoparticles for encapsulating paclitaxel or docetaxel

The aim of this study was to compare physicochemical properties of solid lipid nanoparticles (SLNs) on drug nature. These SLNs were fabricated for formulating paclitaxel (PTX) or docetaxel (DTX). To make small, and highly encapsulated SLNs, the SLNs consisted of compritol 888 ATO (glyceryl behenate) as lipid matrix, poloxamer 188 or solutol HS 15 as surfactant and soya lecithin as co-surfactant. The SLNs were characterized by particle size, zeta potential, in vitro release study and cytotoxicity study. In this study, SLNs showed different physicochemical properties and release profiles according to used solid lipid. In case of particle size, PS1 and DS1 showed bigger particle size than those of PS2 and DS2. Encapsulation efficiency (%) of DTX-loaded SLNs exhibited higher than that of PTX-loaded SLNs. And, DTX-loaded SLNs showed prolonged release up to 24 h. We found that SLN using solutol HS 15 as surfactant exhibited enhanced cellular uptake on MCF-7/ADR cells. These results suggest that different drugs and surfactant effect on physicochemical properties regardless same composition.

Synthesis of sub-10 nm solid lipid nanoparticles for topical and biomarker detection applications

Solid lipid nanoparticles (SLNs) are a promising platform for sensing in vivo biomarkers due to their biocompatibility, stability, and their ability to carry a wide range of active ingredients. The skin is a prominent target organ for numerous inflammatory and stress-related biomarkers, making it an excellent site for early detection of physiological imbalance and application of sensory nanoparticles. Though smaller particle size has generally been correlated with increased penetration of skin models, there has been little attention paid to the significance of other nanoparticle synthesis parameters with respect to their physical properties. In this study, we demonstrate the synthesis of sub-10 nm SLNs by the phase inversion temperature (PIT) method. These particles were specifically designed for topical delivery of hydrogen peroxide-detecting chemiluminescent dyes. A systematic design of experiments approach was used to investigate the role of the processing variables on SLN form and properties. The processing variables were correlated with the SLN properties (e.g., dye solubility, phase inversion temperature, particle size, polydispersity, melting point, and latent heat of melting). Statistical analysis revealed that the PIT method, while allowing total control over the thermal properties, resulted in well-controlled synthesis of ultra-small particles, while allowing great flexibility in the processing conditions and incorporated compounds.

ChemInform Abstract: Solid Lipid Nanoparticles for Oral Delivery of Poorly Soluble Drugs

AbstractReview: 45 refs.

Influence of lipids on the properties of solid lipid nanoparticles from microemulsion technique

Solid lipid nanoparticles (SLN) are colloidal lipid carriers widely employed as efficient drug delivery systems. In this report, SLN were produced by microemulsion technique, and the influence of lipid composition on the physical properties of SLN was evaluated. Lipids with different molecular structures in carbon number of the fatty acid residue and their polarity were selected (i.e., glyceryl trimyristate, glyceryl tripalmitate, glyceryl tristearate, stearic acid, and glyceryl monostearate). A warm oil‐in‐water microemulsion containing 7% lipid, 30% water, and 63% surfactant mixture (polysorbate 80:1‐butanol 4:1) was prepared by simple mixing at 60°C, following its dilution in cold water at various ratios at constant stirring. The obtained SLN were analyzed for appearance, particle size, zeta potential, and sedimentation rate. The chemical structure of the selected lipids affected both the microemulsion formation and the physical characteristics of SLN. From the obtained results, a dilution ratio of 1:50 was selected for the production of SLN composed of glyceryl trimyristate as solid lipid matrix. The obtained particles were of 154.9 ± 0.7 nm mean particle size, with a polydispersity index (PI) of 0.274 and zeta potential of −7.46 ± 0.68 mV.Practical applications: The methodology presented here describes the application of microemulsion technique on processing different lipid compositions, to develop and produce an optimal SLN formulation using pseudoternary phase diagrams. Microemulsion technique is well‐known for preparation SLN by adding a warm oil‐in‐water microemulsion, which can be spontaneously formed, when diluted in a large volume of cold water. The data presented in this paper show that the molecular structures of lipids influenced both the microemulsion formation and the physical characteristics of the resulting SLN. The optimal SLN formulation could be developed.

Effect of lipid on physicochemical properties of solid lipid nanoparticle of paclitaxel

The aim of this study was to compare physicochemical properties of solid lipid nanoparticles (SLN) made from different lipids. To make small, stable, uniform and highly encapsulated SLNs, many factors such as the components (lipid, stabilizer) and preparation condition (sonication time, power) can be considered. Out of those, we selected solid lipid as lipid matrix to investigate an effect on SLNs. The SLNs were characterized by particle size, zeta potential, solubility and in vitro release study. In this study, SLNs showed different physicochemical properties and release profiles according to used solid lipid. In case of particle size, M-SLN showed biggest particle size (412.5 ± 29.4 nm) and highest encapsulation efficiency (61.2 ± 4.8 %). And, B-SLN showed highest cumulative drug percentage (85.0 ± 1.7 %, 24 h) in release study. These results suggest that lipids type affect physicochemical properties and release profile of SLN.

RES and brain targeting stavudine-loaded solid lipid nanoparticles for AIDS therapy

Cells of the reticuloendothelial system (RES, e.g., macrophages) play an important role in the immunopathogenesis of Acquired Immunodeficiency Syndrome (AIDS). The objective of the present study was to investigate the possibility of specifically targeting antiviral drugs Stavudine to RES (like Liver, Spleen etc.) and brain using solid lipid nanoparticles (SLNs) as colloidal drug carriers. Various lipids like stearic acid, cetyl palmitate, glyceryl behenate and phospholipid in combination have been used and effect of lipid on properties of SLNs has been investigated. The SLNs of Stavudine were prepared by double emulsion solvent evaporation method.The diameter of SLNs was determined and found in range of 175 ± 6.027 to 393 ± 2.309 nm depending on the type of lipid used. Percentage drug entrapment was found to be influenced by the concentration and type of lipid used, which was found in the range of 18.1 to 65.2%. The drug release behavior was studied by dialysis bag method and the release pattern of drug was found to follow Higuchi model. Results of stability evaluation showed a relatively long-term stability after storage at 4°C for 1 month. Stavudine-loaded SLNs were successfully prepared, optimized and effectively targeted to RES and brain. SLNs of Stavudine have been shown to be taken up by brain 11 fold greater as compared to pure Stavudine. This finding is more important since Human Immunodeficiency Syndrome (HIV) infect the central nervous system.

In vitro penetration properties of solid lipid nanoparticles in intact and barrier-impaired skin

Treatment of skin diseases implies application of a drug to skin with an impaired epidermal barrier, which is likely to affect the penetration profile of the drug substance as well as the carrier into the skin. To elucidate this, the effect of skin barrier damage on the penetration profile of a corticosteroid applied in solid lipid nanoparticles (SLN) composed of different lipids, varying in polarity, was studied. The studies were carried out in vitro using impaired and intact porcine ear skin, and the SLN were compared with a conventional ointment. It was shown that a significantly higher amount of corticosteroid remained in the skin, intact as well as barrier impaired, when SLN was used as a vehicle. In general, the penetration profile of the drug substance into the skin was affected by the type of lipid used in the formulation and related to lipid polarity and drug substance solubility. When formulated in SLN and applied to intact skin, the permeation of the drug substance across the skin was significantly reduced, as compared to the ointment. Altogether, in both barrier-impaired and intact skin, a higher amount of drug substance remained in the skin during application of SLN for 6, 16, and 24 h, as compared to the ointment. These results emphasize the applicability of SLN to create a drug reservoir in skin, with the drug localized distinctively in the stratum corneum.

Nanopartículas de lipídios sólidos: métodos clássicos de produção laboratorial

Solid lipid nanoparticles have been extensively investigated as drug delivery systems. These colloidal systems have major advantages compared to others more traditional. Reported advantages include sustained release, ability to solubilize lipophilic drugs, increased physical and chemical stability of labile molecules, decreased unwanted side-effects showing lower toxicity, and scale up facilities. This paper aims at reviewing the traditional methods of solid lipid nanoparticles production, such as fusion-emulsification (hot and cold), solvent evaporation-emulsification and microemulsion, dealing with the main technological parameters that influence the quality properties of solid lipid nanoparticles.