Cetyl Palmitate Research Articles

Physicochemical and biological characterization of the lipid particles with bovine serum albumin corona

Diacylglycerol–based nanoparticles are promising bioactive delivery systems. However, limited understanding of their interaction with biological entities restricts their clinical use. This study investigated the protein corona formed on medium and long chain diacylglycerol (MLCD)-based solid lipid nanoparticles (NPs) modified by Polyoxethylene stearate (PEG) and compared to glyceryl tristearate (TG) and cetyl palmitate (CP) nanoparticles. Bovine serum albumin (BSA) formed corona with MLCD NPs through hydrophobic interactions and hydrogen bonding, contributing to a decrease in α–helix, an increase in β–sheet and a change in the microenvironment of Tyr residues. Owing to higher lipid hydrophilicity, MLCD NPs showed a much lower affinity for BSA than TG and CP NPs, and the binding constant with BSA was increased for larger NPs. PEG modification and the protein corona reduced the uptake of NPs by macrophages but exerted little influence on B16 cell. Among the NPs with different lipid core, the MLCD NPs showed a lower macrophages cell uptake but higher B16 cell uptake, suggesting a longer circulation time in blood but higher cancer cell internalization. This work shed light on the interactions between MLCD NPs and proteins, which is significant for application as nanocarriers with improved biological efficacy.

Microencapsulation for the delivery of terazosin hydrochloride: design, development, and characterization

The aim of the work. Terazosin HCL, which is a selective alpha-1 antagonist, has been recommended for the treatment of benign prostatic hyperplasia-related medical conditions, including hypertension and urinary tract disorders. The purpose of this research was to create microparticles that would have a prolonged release of terazosin hydrochloride (TZ). However, TZ is a medicine that is readily soluble and has a high capability of dissolving in water. Materials and methods. A validated HPLC method was established to assess TZ. The TZ microparticles were produced using the process of melt dispersion by utilising cetyl palmitate (CP), myristic acid (MA), Glycerol monostearate 4055 (type II) or Kolliwax® GMS II (GMS), polyethylene glycol 400 (PEG 400) as a plasticizer, and tween 80 as a stabilizing agent. Different formulations of TZ microparticles were evaluated with regard to particle size, zeta potential, and release, and morphological scanning was performed. Results. A zeta potential that falls between -22.9 and -29.4 mV is possessed by TZ microparticles. Furthermore, the size of TZ microparticles falls between 2.11 and 5.60 µm, and the polydispersity index (PDI) was between 0.24 to 0.41. In addition, the formula (F4) that included CP, GMS, PEG 400, and Tween 80 in the proportions of 0.8:0.2:1:0.5 had the highest zeta potential (ZP) and dissolved more than 85 % of TZ after 8 hours. Therefore, F4 was chosen for the purpose of conducting morphological research. Conclusion. Employing the use of CP, GMS, PEG 400, and Tween 80 in a ratio of 0.8:0.2:1:0.5 could result in the generation of microparticles of TZ that are the most acceptable

Fresh Carrier for an Old Topical Local Anesthetic: Benzocaine in Nanostructured Lipid Carriers.

Nanostructured lipid carriers (NLC) have emerged as innovative drug delivery systems, offering distinct advantages over other lipid-based carriers, such as liposomes and solid lipid nanoparticles. Benzocaine (BZC), the oldest topical local anesthetic in use, undergoes metabolism by pseudocholinesterase, leading to the formation of p-aminobenzoic acid, a causative agent for allergic reactions associated with prolonged BZC usage. In order to mitigate adverse effects and enhance bioavailability, BZC was encapsulated within NLC. Utilizing a 23 factorial design, formulations comprising cetyl palmitate (solid lipid), propylene glycol monocaprylate (liquid lipid), and Pluronic F68 as surfactants were systematically prepared, with variations in the solid/liquid lipid mass ratios (60:40-80:20%), total lipid contents (15-25%), and BZC concentrations (1-3%). The optimized formulation underwent characterization by dynamic light scattering, differential scanning calorimetry, Raman imaging, X-ray diffraction, small-angle neutron scattering, nanotracking analysis, and transmission electron microscopy (TEM)/cryo-TEM, providing insights into the nanoparticle structure and the incorporation of BZC into its lipid matrix. NLCBZC exhibited a noteworthy encapsulation efficiency (%EE = 96%) and a 1 year stability when stored at 25 °C. In vitro kinetic studies and in vivo antinociceptive tests conducted in mice revealed that NLCBZC effectively sustained drug release for over 20 h and prolonged the anesthetic effect of BZC for up to 18 h. We therefore propose the use of NLCBZC to diminish the effective anesthetic concentration of benzocaine (from 20 to 3% or less), thus minimizing allergic reactions that follow the topical administration of this anesthetic and, potentially, paving the way for new routes of BZC administration in pain management.

Lipase-Catalyzed Synthesis of Cetyl Palmitate in the Presence of n-Hexane and Ethyl Ether

Cetyl palmitate was produced by the esterification of palmitic acid with cetyl alcohol using n-hexane and ethyl ether as solvents and a commercial lipase as a catalyst. The effect of solvents to reagents mass ratio (0.5 : 1–3 : 1), percentage of n-hexane in the solvent mixture (0–100%), and reaction temperature (25–55°C) on the reaction rate were evaluated for a fixed amount of enzyme (1 wt% related to the total mass of substrates) in an equimolar mixture of palmitic acid and cetyl alcohol. Temperature and n-hexane percentage in the solvent had positive effects on the reaction rate. The total solvent-to-reagent mass ratio showed a negative effect on the reaction rate when a solvent mixture rich in ethyl ether was used. The higher the concentration of n-hexane, the lower the effect of the mass ratio of solvents to reagents on the reaction rate. Although the amount of ethyl ether in the solvent mixture had a negative effect on the reaction rate, it had a positive effect on the solubility of the system, that is, the more ethyl ether in the mixture, the lower the solvent to reagents mass ratio required to ensure a homogeneous mixture. A ping-pong bi-bi mechanism-based model was proposed to represent the system kinetics and was well fitted to the experimental data.

Effect of Functional Groups in Lipid Molecules on the Stability of Nanostructured Lipid Carriers: Experimental and Computational Investigations.

Lipid nanoparticles have been used as drug carriers for decades. Many lipid types have been screened for both solid lipid nanoparticles and nanostructured lipid carriers (NLCs). Specifically, for NLCs that are composed of lipids in the solid form mixed with lipids in the liquid form, compatibility of lipid combination and phase behavior play a significant role in the NLC quality. In this study, stearic acid (STA) and cetyl palmitate (CTP) were used as solid lipids, and oleic acid (OLA), isopropyl palmitate (IPP), and caprylic/capric triglycerides were used as liquid lipids. NLCs were prepared at solid:liquid ratios of 50:50, 70:30, and 90:10, respectively. The characteristics and stability of the prepared NLCs were investigated. Laboratory results showed that the solid lipid had a greater influence on the particle size than the liquid lipid. Meanwhile, cetyl palmitate, an ester compound, provides higher NLC stability compared to stearic acid, a carboxylic acid compound. A MARTINI-based coarse-grained molecular dynamics simulation was used to simulate the lipid droplet in water. The distribution of lipid molecules in the droplet was characterized by the polar group density distribution. Different spatial arrangements of the lipid headgroup and lipid molecules, when CTP or STA was used as solid lipids, might contribute to the different stabilities of prepared NLCs. The understanding of mixed lipid systems via simulations will be a significant tool for screening the type of lipids for drug carriers and other pharmaceutical applications.

Small-angle X-ray scattering unveils the internal structure of lipid nanoparticles

Lipid nanoparticles own a remarkable potential in nanomedicine, only partially disclosed. While the clinical use of liposomes and cationic lipid-nucleic acid complexes is well-established, liquid lipid nanoparticles (nanoemulsions), solid lipid nanoparticles, and nanostructured lipid carriers have even greater possibilities. However, they face obstacles in being used in clinics due to a lack of understanding about the molecular mechanisms controlling their drug loading and release, interactions with the biological environment (such as the protein corona), and shelf-life stability. To create effective drug delivery carriers and successfully translate bench research to clinical settings, it is crucial to have a thorough understanding of the internal structure of lipid nanoparticles. Through synchrotron small-angle X-ray scattering experiments, we determined the spatial distribution and internal structure of the nanoparticles' lipid, surfactant, and the bound water in them. The nanoparticles themselves have a barrel-like shape that consists of coplanar lipid platelets (specifically cetyl palmitate) that are covered by loosely spaced polysorbate 80 surfactant molecules, whose polar heads retain a large amount of bound water. To reduce the interface cost of bound water with unbound water without stacking, the platelets collapse onto each other. This internal structure challenges the classical core-shell model typically used to describe solid lipid nanoparticles and could play a significant role in drug loading and release, biological fluid interaction, and nanoparticle stability, making our findings valuable for the rational design of lipid-based nanoparticles.

Development of a Versatile Lipid Core for Nanostructured Lipid Carriers (NLCs) Using Design of Experiments (DoE) and Raman Mapping.

The objective of this study was to develop a versatile lipid core for the 'brick-dust type of drugs' (poorly water-soluble and poorly lipid-soluble drugs). In the first step, excipients of different polarities were classified according to their behavior in aqueous solutions. Subsequently, binary mixtures were prepared with cetyl palmitate (Crodamol™ CP pharma, Campinas, São Paulo, Brazil) as the solid lipid, and its miscibility with other excipients was evaluated using Raman mapping and classical least squares (CLS). Based on the results, the excipients Crodamol™ CP pharma (hydrophobic), Super Refined™ DMI (dimethyl isosorbide; hydrophilic, Mill Hall, PA, USA), and Super Refined™ Lauryl Lactate (lauryl lactate, medium polarity, Mill Hall, PA, USA) were chosen to compose the lipid core. The ideal proportion of these excipients was determined using a mixture design and the standard deviation (STD) of image histograms as the response variables. After statistical evaluation of the DoE results, the final composition was determined, and drugs with different logP (0 to 10) and physicochemical characteristics were evaluated in the optimized mixture. The drugs butamben (Sigma-Aldrich Co., Spruce Street, St. Louis, MO, USA), tacrolimus (NutriFarm, São Paulo, Brazil), atorvastatin calcium, and resveratrol (Botica da Terra, Campinas, Brazil) presented a homogeneous distribution in the optimized lipid core, indicating that this is a promising system to be used in nanostructured lipid carrier (NLC) formulations of such types of drugs.

Natural-Origin Betaine Surfactants as Promising Components for the Stabilization of Lipid Carriers.

In the present work, we demonstrate studies involving the influence of the formulation composition on the physicochemical properties of nanocarriers: solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs). Novel lipid-origin platforms were prepared using two "green" betaine-based surfactants, cocamidopropyl betaine (ROKAmina K30) and coco betaine (ROKAmina K30B), in combination with three different solid lipids, cetyl palmitate (CRODAMOL CP), trimyristin (Dynasan 114), and tristearin (Dynasan 118). Extensive optimization studies included the selection of the most appropriate lipid and surfactant concentration for effective SLN and NLC stabilization. The control parameters involving the hydrodynamic diameters of the obtained nanocarriers along with the size distribution (polydispersity index) were determined by dynamic light scattering (DLS), while shape and morphology were evaluated by atomic force microscopy (AFM) and transmission electron microscopy (TEM). Electrophoretic light scattering (ELS) and turbidimetric method (backscattering profiles) were used to assess colloidal stability. The studied results revealed that both betaine-stabilized SLN and NLC formulations containing CRODAMOL CP as lipid matrix are the most monodisperse and colloidally stable regardless of the other components and their concentrations used, indicating them as the most promising candidates for drug delivery nanosystems with a diverse range of potential uses.

Development of astaxanthin-loaded nanostructured lipid carriers using a combination of cetyl palmitate and soybean oil

Development of astaxanthin-loaded nanostructured lipid carriers using a combination of cetyl palmitate and soybean oil

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.

Development of lipid nanoparticles with nystatin for an antifungal action

Fungal diseases currently affect about a quarter of the population worldwide. Fungi infections caused by Candida albicans have been described as a significant concern to public health. The spectrum of clinical diseases caused by this fungi species range between vulvovaginal candidiasis, oral candidiasis, candidemia and mucositis. The emergence of resistance mechanisms towards antifungal therapy greatly hampers successful management of illness and patient outcome. Nystatin, an antifungal drug, is categorized as a class IV of Biopharmaceutical Classification System, presenting low aqueous solubility and low intestinal permeability. Nowadays, the emerging platform of nanotechnology and lipid nanoparticles, notably solid lipid nanoparticles (SLN), has been subject to growing attention over recent past, owing to the promising properties of vectorization among a substantial variety of pharmaceutical drugs. Due to its hydrophobic proprieties, nystatin was encapsulated in SLN. Thus aiming to understand the relationship between the use of nanosystems and the improvement of the therapeutic effect. The aim of this work was to formulate SLN with nystatin by different methods (high speed homogenization and ultrasonication) with optimization of several parameters and formulation of 2 gels (one of them containing nanoparticles).&#x0D; Initially, 3 lipids were used: Compritol® 888 ATO, cetyl palmitate and Precirol® ATO 5 and, after the study of several parameters (size, encapsulation efficiency (EE) and polymorphic behaviour of the lipids), Precirol® ATO 5 was chosen as the lipid with the most satisfactory results. The results of the present work showed that the assay method of nystatin was linear, specific and presented repeatability. The average diameter of empty nanoparticles (NPs) and with drug (Precirol-NYS NPs) was, respectively, 306 nm and 260 nm and an EE of 67.8%. Regarding stability, SLN with drug proved to be more stable than SLN without drug. The polymer used for formulation of gels was the polymer commonly known by the trade name Carbopol® 940. The yield of 0.5% Carbopol® gel preparations and 0.5% Carbopol® gel + 10% Precirol-NYS NPs were 87.2% and 91.39%, respectively.

Cannabidiol-Loaded Nanostructured Lipid Carriers (NLCs) for Dermal Delivery: Enhancement of Photostability, Cell Viability, and Anti-Inflammatory Activity

The aim of this study was to encapsulate cannabidiol (CBD) extract in nanostructured lipid carriers (NLCs) to improve the chemical stability and anti-inflammatory activity of CBD for dermal delivery. CBD-loaded NLCs (CBD-NLCs) were prepared using cetyl palmitate (CP) as a solid lipid and stabilized with Tego® Care 450 (TG450) or poloxamer 188 (P188) by high-pressure homogenization (HPH). The CBD extract was loaded at 1% w/w. Three different oils were employed to produce CBD-NLCs, including Transcutol® P, medium-chain triglycerides (MCT), and oleic acid (OA). CBD-NLCs were successfully prepared with an entrapment efficiency (E.E.) of 100%. All formulations showed particle sizes between 160 and 200 nm with PDIs less than 0.10. The type of surfactant and oil used affected the particle sizes, zeta potential, and crystallinity of the CBD-NLCs. CBD-NLCs stabilized with TG450 showed higher crystallinity after production and storage at 30 °C for 30 days as compared to those with P188. Encapsulation of the CBD extract in NLCs enhanced its chemical stability after exposure to simulated sunlight (1000 kJ/m2) compared to that of the CBD extract in ethanolic solution. The CBD-NLCs prepared from MCT and OA showed slower CBD release compared with that from Transcutol® P, and the kinetic data for release of CBD from CBD-NLCs followed Higuchi's release model with a high coefficient of determination (>0.95). The extent of CBD permeation through Strat-M® depended on the oil type. The cytotoxicity of the CBD extract on HaCaT and HDF cells was reduced by encapsulation in the NLCs. The anti-inflammatory activity of the CBD extract in RAW264.7 cell macrophages was enhanced by encapsulation in CBD-NLCs prepared from MCT and OA.

Contribution of Chevreul to lipid chemistry

Michel Eugène Chevreul entered at 17 the laboratory of Vauquelin, at the Museum. He began his investigations on animal fats in 1811. They appear as yet the most complete and the best executed experiments found in all chemistry. For the first time, he combined fractional solution, crystallization, distillation, melting point determination, and ultimate analysis. All started with the isolation of an acid and solid substance, “margaric acid”, the first of a long list of fatty acids isolated from various fats. Studying saponification, he determined that “anhydrous glycerine” was combining with water. After studying human gallstones, he discovered “cholesterine” (cholesterol). From whale spermaceti, he described “cetin” (mainly cetyl palmitate), containing no glycerol. He isolated from sheep fat a new acid he named “stearic acid”. This component was proposed in a joint patent by Chevreul and Gay-Lussac (1825) for the fabrication of very efficient candles. He discovered several volatile fatty acids in cow and goat butter (from C4 to C10). His master work (Recherches chimiques sur les corps gras d’origine animale, 1823b) contains his experimental procedures and his theoretical conclusions on the nature of fats, it may be considered as the first treatise on lipochemistry.

Hybrid Lipid/Clay Carrier Systems Containing Annatto Oil for Topical Formulations.

Nanocomposites formed by clay and lipid carriers (NLCs) show a high potential for providing controlled release and specific delivery of bioactive molecules and have recently gained attention in the pharmaceutical sector due to their ability to transport hydrophilic and hydrophobic drugs. Recent studies have recognized the biological activity of the oil of Bixa orellana L. (AO) with regards to its healing, antioxidant, antibacterial, and anti-leishmanial properties. Therefore, the purpose of this study is the preparation and characterization of hybrid systems based on lipid nanocarriers and laponite for the delivery of AO. NLCs were prepared by the fusion-emulsification method, using cetyl palmitate (CP) or myristyl myristate (MM), AO, and Poloxamer 188. The morphology, hydrodynamic diameters, zeta potential (ZP), polydispersity index (PDI), thermal analysis, X-ray diffraction analysis (XRD), viscosity behavior, and cytotoxicity testing of the hybrid systems were performed. The thermal study and X-ray diffraction analyses (XRD) revealed polymorphic structural changes compatible with the amorphization of the material. Rheological assays highlighted a typical pseudoplastic behavior in all systems (MM and CP with LAP). The hybrid systems’ morphology, size diameters, and PDIs were similar, preset spherical and monodisperse structures (≈200 nm; <0.3), without significant change up to sixty days. The ZP values differed from each other, becoming higher with increasing AO concentration. XEDS spectra and elemental X-ray maps show peaks of lipids (organic components, C and O) and inorganic components O, Mg, and Si. All samples showed cell viability above 60%. The results indicated a stable, biocompatible hybrid system that can be an alternative for topical application.

Digestion of lipid excipients and lipid-based nanocarriers by pancreatic lipase and pancreatin

The digestion behaviour of lipid-based nanocarriers (LNC) has a great impact on their oral drug delivery properties. In this study, various excipients including surfactants, glycerides and waxes, as well as various drug-delivery systems, namely self-emulsifying drug delivery systems (SEDDS), solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were examined via the pH-stat lipolysis model. Lipolysis experiments with lipase and pancreatin revealed the highest release of fatty acids for medium chain glycerides, followed by long chain glycerides and surfactants. Waxes appeared to be poor substrates with a maximum digestion of up to 10% within 60 min. Within the group of surfactants, the enzymatic cleavage decreased in the following order: glycerol monostearate > polyoxyethylene (20) sorbitan monostearate > PEG-35 castor oil > sorbitan monostearate. After digestion experiments of the excipients, SEDDS, SLN and NLC with sizes between 30 and 300 nm were prepared. The size of almost all formulations was increasing during lipolysis and levelled off after approximately 15 min except for the SLN and NLC consisting of cetyl palmitate. SEDDS exceeded 6000 nm after some minutes and were almost completely hydrolysed by pancreatin. No significant difference was observed between comparable SLN and NLC but surfactant choice and selection of the lipid component had an impact on digestion. SLN and NLC with cetyl palmitate were only digested by 5% whereas particles with glyceryl distearate were decomposed by 40–80% within 60 min. Additionally, the digestion of the same SLN or NLC, only differing in the surfactant, was higher for SLN/NLC containing polyoxyethylene (20) sorbitan monostearate than PEG-35 castor oil. This observation might be explained by the higher PEG content of PEG-35 castor oil causing a more pronounced steric hindrance for the access of lipase. Generally, digestion experiments performed with pancreatin resulted in a higher digestion compared to lipase. According to these results, the digestion behaviour of LNC depends on both, the type of nanocarrier and on the excipients used for them.

Physicochemical Characteristics, Stability, and Irritability of Nanostructured Lipid Carrier System Stabilized with Different Surfactant Ratios

Background: One of the vital variables affecting the stability and the characteristics of the Nanostructured Lipid Carrier (NLC) is the surfactant concentration. Using the two combinations of surfactants can cause higher stability and a better characteristic of NLC. Tween 80 and Span 20 are anionic surfactants whose combination has not been studied for use in NLC systems. Objective: Determine the effect of different surfactant ratios of Tween 80 and Span 20 on the physicochemical characteristics, stability, and irritability of NLC using the High Shear Homogenization (HSH) method. Methods: Four different surfactant ratios were used in the NLC formulation, in which the ratio of Tween 80:Span 20 were 5:5, 6:6, 7:7, and 8:8, respectively. In this NLC system, cetyl palmitate served as solid lipid, medium-chain triglyceride (CrodamolTM) as liquid lipid, Tween 80, and Span 20 as surfactant components. NLC was characterized for organoleptic, viscosity, pH, zeta potential, particle morphology, particle size, and polydispersity index (PDI), then evaluated for stability using the real-time and freeze-thaw method, and irritability effect. Results: The different ratios of Tween 80 and Span 20 had no significant effect on the particle size, PI, and irritation score of the NLC system. On the other hand, it influenced all formulas' pH value, viscosity, zeta potential, and stability. Conclusions: The different ratios of surfactant combination affect the characteristics and stability of the NLC system.

Stabilization of water‐in‐oil emulsions using a wax ester synthesized by a new homemade heterogeneous biocatalyst

AbstractBACKGROUNDCetyl palmitate is a wax ester naturally found in sperm whale spermaceti, and it is of importance in the cosmetics industry. International regulations prohibit the sale of sperm whale spermaceti, so it is now being replaced by pure cetyl palmitate obtained by a chemical route or from mixtures based on jojoba oil. Another alternative is to use an enzymatic route for wax ester synthesis. For such a purpose, a new heterogeneous biocatalyst was prepared by our research group via physical adsorption of Burkholderia cepacia lipase on aerogel modified with a protic ionic liquid (IB‐IL‐OPT). Its catalytic activity was compared with that of a biocatalyst prepared using a non‐chemically modified silica aerogel (IB‐Control). The objective of this work was to apply this homemade heterogeneous biocatalyst to cetyl palmitate synthesis via a direct esterification reaction in a solvent system and to test the final product as a stabilizing agent in water‐in‐oil emulsions.RESULTSIB‐IL‐OPT achieved maximum acid conversion of 95–100% under optimal experimental conditions established using a central composite rotational design: biocatalyst concentration of 14.8% (w/w), molar ratio of 1:1.3, 41 °C for 15 h of reaction under continuous mechanical agitation (200 rpm). The IB‐Control gave 58.8% acid conversion in similar conditions. IB‐IL‐OPT was successively reused for four cycles. The wax ester showed potential as a good emulsifier for virgin coconut oil.CONCLUSIONSThe cetyl palmitate obtained via an enzymatic route without further purification showed good emulsifying potential, forming Pickering emulsions. This opens new perspectives for study and applications in the cosmetics industry. © 2022 Society of Chemical Industry (SCI).

STABILITAS NANOSTRUCTURED LIPID CARRIER COENZYME Q10 DENGAN VARIASI WAKTU PENGADUKAN

ABSTRACTCoenzyme Q10 (Co-Q10) or Ubiquinone is an antioxidant that is unstable to light and is highly lipophilic causing instability during storage, so a Nanostructured Lipid Carrier (NLC) delivery system is needed that can improve stability. The manufacture of NLC uses the emulsification method by melting two types of lipids, namely solid lipid cetyl palmitate and liquid lipid alpha tocopherol with the help of stirring using a magnetic stirrer. The purpose of this study was to determine the characteristics and stability of NLC Co-Q10 at various stirring times. The results of testing the characteristics NLC Co-Q10, that stirring for 6 and 9 minutes, obtained pH values of 6,64 and 6,62 with particle sizes of 215.03 nm and 188.25 nm, the entrapment efficiency values were 75.57% and 77.96%, respectively. Increasing the speed and duration of stirring in the manufacture of the NLC Co-Q10 system will obtain high trapping efficiency values and be more stable in storage at room temperature for 28 days.Keywords: coenzyme Q10, emulsification, nanostructured lipid carriers, stability.

Design expert assisted formulation, characterization and optimization of microemulsion based solid lipid nanoparticles of repaglinide.

Repaglinide, a member of the meglitinide class of drugs, is a new anti-diabetic agent that is utilized as an oral hypoglycemic agent. Using glyceryl monostearate, cetyl palmitate, and tristearin as lipids and poloxamer 188 as a surfactant, repaglinide-loaded solid lipid nanoparticles were created. Solid lipid nanoparticles were prepared utilizing an o/w microemulsion technique, which included the lipids glyceryl monostearate and tristearin, as well as waxes such as cetyl palmitate and the surfactant poloxamer 188. The mean particle size of the solid lipid nanoparticles formed was around 339nm, with an entrapment efficiency of 82.20%. In-vitro release studies continued to be conducted using the dialysis bag diffusion technique. Within 12h, the cumulative drug release was 88.4%. The results indicate that repaglinide was released more slowly from solid lipid nanoparticles made from tristearin and glyceryl monostearate in an equal ratio. Tristearin found the controlled release and extreme entrapment from other lipid carriers like glyceryl monostearate and cetyl palmitate. Differential scanning calorimetry demonstrates that repaglinide is entangled in amorphous or molecular state within solid lipid nanoparticles. SEM microscopy revealed that the produced repaglinide solid lipid nanoparticles had a spherical shape. After one month of storage at 2-8°C, short-term stability testing revealed no significant alteration.

Annatto Oil Loaded Nanostructured Lipid Carriers: A Potential New Treatment for Cutaneous Leishmaniasis

Annatto (Bixa orellana L.) is extensively used as food pigment worldwide. Recently, several studies have found it to have healing and antioxidant properties, as well as effective action against leishmaniasis. Therefore, the purpose of this study was to incorporate the oil obtained from annatto seeds into a nanostructured lipid carrier (NLC) and evaluate its physicochemical properties and biological activity against Leishmania major. Nanoparticles were prepared by the fusion-emulsification and ultrasonication method, with the components Synperonic™ PE (PL) as the surfactant, cetyl palmitate (CP) or myristyl myristate (MM) as solid lipids, annatto oil (AO) (2% and 4%, w/w) as liquid lipid and active ingredient, and ultra-pure water. Physicochemical and biological characterizations were carried out to describe the NLCs, including particle size, polydispersity index (PDI), and zeta potential (ZP) by dynamic light scattering (DLS), encapsulation efficiency (EE%), thermal behavior, X-ray diffraction (XRD), transmission electron microscopy (TEM), Electron Paramagnetic Resonance (EPR), cytotoxicity on BALB/c 3T3 fibroblasts and immortalized human keratinocyte cells, and anti-leishmaniasis activity in vitro. Nanoparticles presented an average diameter of ~200 nm (confirmed by TEM results), a PDI of less than 0.30, ZP between −12.6 and −31.2 mV, and more than 50% of AO encapsulated in NLCs. Thermal analyses demonstrated that the systems were stable at high temperatures with a decrease in crystalline structure due to the presence of AOs (confirmed by XRD). In vitro, the anti-leishmania test displayed good activity in encapsulating AO against L. major. The results indicate that the oily fraction of Bixa orellana L. in NLC systems should be evaluated as a potential therapeutic agent against leishmaniasis.