Hydrophilic-lipophilic Balance Values Research Articles

Characteristics and emulsifying properties of structured phospholipids from palm pressed fiber and omega-3 fatty acid concentrates from by-products of fish processing by enzymatic acidolysis.

The synthesis of structured phospholipids (SPLs) containing ω-3 fatty acids was carried out through enzymatic acidolysis reactions using lipase from Rhizomucor miehei between palm pressed fiber phospholipids (PPF PL) with four ω-3 fatty acid concentrates as different acyl sources. The purity of SPLs increased compared to original PPF PLs. The degree of ω-3 fatty acid incorporation to the SPLs was different that depended on the sources of acyl. The highest degree of incorporation was in PE (phosphatidylethanolamine). The phenomenon of acyl migration of EPA (eicosapentaenoic acid) and DHA (docosahexaenoic acid) was found from the sn-1 to the sn-2 position of the PE. This acyl migration occurred at all four SPLs. Modification of PLs made better emulsifying properties for oil in water emulsion system, compared to PPF PL. The increase in the HLB (hydrophilic-lipophilic balance) value, EAI (emulsifying activity index), and ESI (emulsion stability index) of SPLs compared to PPF PL was supposed to relate to an increase in polarity. The composition of more polar PLs (PC/phosphatidylcholine, PE, PG/phosphatidylglycerol, and PA/phosphatidic acid) in the four SPLs is higher than that of PPF PL. The sources of acyl also affected the emulsifying properties of four SPLs.

Preparation and characterization of the encapsulated myrtle extract nanoliposome and nanoniosome without using cholesterol and toxic organic solvents: A comparative study

Nanoliposome and nanoniosome formulations containing myrtle extract were prepared without using cholesterol and toxic organic solvents for the first time. The formulations had different concentrations of lecithin (5, 7, and 9% w/w) and Hydrophilic-Lipophilic Balance (HLB) values (6.76, 8.40, and 9.59). The physicochemical characterization results showed a nearly spherical shape for the prepared nanosamples. The particle sizes, zeta potentials and encapsulation efficiencies for the prepared nanoliposomes and nanoniosomes were at a range of 260–293 nm and 224–520 nm; −33.16 to − 31.16 mV and − 33.3 to − 10.36 mV; and 68–73% and 79–83%, respectively. The formulated nanoniosomes showed better stability during storage time. Besides, the encapsulation efficiency and in vitro release rate of myrtle extract could be controlled by adjusting the lecithin concentration and HLB value. The release of myrtle extract from nanovesicles showed a pH-responsive character. The FTIR analysis confirmed that the myrtle extract was encapsulated in nanovesicles physically.

Determination of optimum conditions to produce stearoyl glycerol enzymatically

Stearoyl glycerol is the result of the esterification of glycerol with stearic acid enzymatically using immobilized lipase as catalyst. The lipase is immobilized with chitosan matrix with entrapment method. This study aims were to determine the optimum condition of esterification of glycerol with stearic acid based on reaction time and temperature, and reactant mole ratio. The esterification reaction was carried out by varying reaction time (6, 12, 18, 24, 30) hours, reaction temperature (30, 35, 45, 50, 55) °C, and mole ratio of stearic acid : glycerol (1: 1, 1: 2, 1: 4, 1: 6, 1: 8), the optimum conditions were achieved through conversion percentage. The produced ester was identified by FTIR spectrophotometer and characterized by the value of Hydrophilic-Lipophilic Balance (HLB). The results showed that optimum conditions on reaction time 24 hours, reaction temperature 45°C and mole ratio of stearic acid:glycerol (1:2) produced stearoyl glycerol with conversion percentage of 41.04% and HLB values of 5.01 that was included in the w/o emulsifier type. In addition, the FTIR spectra showed a strong absorption at wave numbers 1703.03 cm−1 (C=O), 1043.02 cm−1(C-O), and 3402.20 cm−1 (O-H) which indicated the characteristic absorption of stearoyl glycerol.

Preparation and characteristics of W/O microemulsion stabilized with polyglycerylpolyricinoleate as a potential system for oral insulin delivery

Aim. The aim of the present work was to develop the composition and study the characteristics of water-in-oil microemulsion stabilized with polyglycerylpolyricinoleate — Tween 80 — ethanol mixture as a potential system for oral insulin delivery. Materials and methods. To determine the boundaries of the regions of existence of water-in-oil microemulsion in the pseudo-three component systems water — polyglycerylpolyricinoleate (PG-3-PR, Gobiotics BV, Netherlands)/ Tween 80/ethanol — paraffin oil, mixtures of paraffin oil and surfactants with oil — surfactant ratios from 9.5:0.5 to 0.5: 9.5 (wt.) were thoroughly mixed and titrated with an aqueous phase (distilled water).Compositions with the value of hydrophilic-lipophilic balance of the PG-3-PR — Tween 80 mixture equal to 6.15 were studied. Among several types of formed systems, a single-phase region corresponding to a homogeneous, optically transparent, liquid water-in-oil microemulsion was determined. The kinetic and thermodynamic stability of a number of compositions, including those containing insulin (Actrapid HM, Novo Nordisk А/С, Denmark), was studied. The values of the effective viscosity of microemulsions at different ratios of surfactant — oil and surfactant — co-surfactant were determined using a vibration viscometer. Based on the results obtained, a composition was selected to study the kinetics of insulin release into a model environment that simulated the environment of the small intestine. Insulin solution (the control sample) and the insulin-containing microemulsion were placed in the dialysis bags and immersed in 50 mL of PBS (pH 7.4) in a shaking incubator at 180 rpm and 37 ° С. At predetermined intervals, the aliquots of dissolution media were withdrawn, and the concentration of the released peptide was determined by the Bradford assay using a UV spectrophotometer at 595 nm. Results. The composition with 9:1 surfactant — co-surfactant ratio, containing 10 % of the aqueous phase (an insulin solution with a concentration of 100 IU / ml), which remained stable both during three cycles of freezing/thawing and heating/cooling, and after long-term storage at room temperature, was selected to study the kinetics of in vitro release of the peptide into the model medium. The effective viscosity of the sample was 2.4±0.04 Pa.s. The microemulsion sample demonstrated a prolonged release of insulin within 48 hours of the experiment (43 %). Conclusions. As a result, the boundaries of the existence of microemulsion regions in pseudo-three — component systems water — polyglycerylpolyricinoleate / Tween 80 / ethanol — paraffin oil were established, as well as the values of the effective viscosity of a number of compositions were determined. The study of the kinetic and thermodynamic stability of the obtained systems, including those containing insulin, as well as the study of the kinetics of the release of biologically active substance from the microemulsion into the model medium, allowed us to determine the optimal composition for further development of nanoscale dosage forms intended for prolonged delivery of insulin to the gastrointestinal tract.

Evalution of surface activity of hydrophobic modified nanocrystalline cellulose

Nanocrystalline cellulose (NCC) prepared via sulfuric acid hydrolysis was used as raw material. The nanocrystalline cellulose was graft-modified by long-chain fatty acids including lauric acid, palmitic acid, and stearic acid in a FeSO4/H2O2 oxidation–reduction system at low temperature. Modified nanocrystalline cellulose (MNCC) was obtained through above process. Crystalline structure and microstructure of the MNCC were analyzed and characterized. To explore the surface activities of the MNCC, contact angle, surface tension, critical micelle concentration (CMC) and hydrophile–lipophile balance (HLB) values were tested. Results showed that water contact angles of lauric acid-, palmitic acid-, and stearic acid-nanocrystalline cellulose were 79.3°, 82.5° and 84.8°, and HLB values were 15.78, 16.29 and 16.81, respectively. The CMC of the MNCC was 12.5 mg/L. The MNCC had good hydrophilic and lipophilic properties. It was a kind of non-ionic natural macromolecule surfactants and could replace traditional surfactants as emulsifiers and solubilizers.

Influence of the hydrophilic moiety of polymeric surfactant on their surface activity and physical stability of pesticide suspension concentrate

Polymeric surfactant has explored as an efficient dispersant for improving the physical stability of pesticide suspension concentrate. However, the influence of the hydrophilic monomer on the surface-active property of polymeric surfactant and its application performance in pesticide formulation is rare investigated. Herein, three kinds of random polymers were designed and synthesized via polymerization reaction of styrene (St), methacrylic acid (MAA) with 2-hydroxyethyl acrylate (HEA), 2-hydroxypropyl acrylate (HPA) and vinyl sulfonate sodium (VS), respectively. A series of surface-active parameters, including critical aggregation concentration (CMC), saturation surface excess concentration (Γmax), minimum area per molecule (Amin) and standard Gibbs free energy ΔGm0 values were obtained from surface tension measurement. The results showed that CMC increased and ΔGm0 decreased with the increase of the hydrophilicity of the third monomer. The results of foamability measurement indicated that the polymeric surfactant with VS as the third monomer had the best foam producing ability and foam stability. When HPA served as the third monomer, the surfactant had the lowest hydrophile lipophile balance (HLB) value and the O/W emulsion prepared by it had the worst stability. Besides, the influence of synthesized polymeric surfactants as dispersant on zeta potential, viscosity and suspension rate of 430 g/L tebuconazole suspension concentrate were investigated. The results showed that poly(styrene-co-methacrylic acid-co-2-hydroxypropyl acrylate) performed best in improving the physical stability of the formulations. From SEM imagines of tebuconazole particle, it was found the increase of particle size in tebuconazole suspension concentrate were caused by aggregation or Ostwald ripening after thermal storage.

Enhanced β-carotene encapsulation and protection in self-assembled lyotropic liquid crystal structures

The aim of this study was to form liquid crystalline structures for retaining and protecting β-carotene (β-c). Tween 40-Span 20 (TxSy) were blended for obtaining target hydrophilic-lipophilic balance (HLB) values ranging from 9 to 15. TxSy were mixed with canola oil (O) as carrier and water (W) as solvent and incubated for 10 days at 37 °C. The formation of lyotropic liquid crystals (LLC) was visually monitored. Pseudo-ternary phase diagrams were constructed to identify the region of LLC formation, which occurred only at HLB values of 11 and 12, the formation region being significantly larger in the former case. The experiments at HLB = 11 were repeated but substituting 0.7% of O by β-carotene (β-c) to produce LLC loaded with β-c (LLC β-c). Finally, LLC β-c were stored in darkness at 25 °C during five weeks. Best LLC β-c yield occurred for an O+β-c:TxSy:W ratio of 40:40:20 (p < 0.05), but the lowest degradation of β-c (17.26%) happened for an O+β-c:TxSy:W ratio of 36:54:10 (p < 0.05). This work provides a procedure for obtaining LLC systems for efficient protection, retention and/or release of nutraceuticals or bioactive compounds such as vitamins, antioxidants and smell substances, which may be used for developing novel food products with desired properties.

FORMULATION AND EVALUATION OF IVABRADINE HYDROCHLORIDE LOADED TRANSFERSOMAL GEL FOR TRANSDERMAL DELIVERY

Objective: Aim of this study was to develop the topical delivery containing ivabradine hydrochloride (IVH) loaded transpersonal gel for symptomatic treatment of chronic stable angina pectoris in coronary artery disease.&#x0D; Methods: Different hydrophilic-lipophilic balance (HLB) values of surfactants-tween-80, span-80 and sodium deoxycholate (SDC) were investigated to prepare transfersomes (TFs)respectively, with different concentration of soya phosphatidylcholine and 10% v/v ethanol in phosphate buffer solution (pH 6.8) by conventional rotary evaporation sonication method. The prepared formulations were evaluated for percentage entrapment efficiency (%EE), deformability index (DI), turbidity, vesicle shape and size, in vitro drug release study and stability. SEM was done on selected formulation F8 and liposome formulation (LF). Gel was prepared by using carbopol-940 as a gelling agent with propylene glycol, polyethylene glycol solution as permeation enhancer by 32 factorial design optimization methods. The developed gel was evaluated for pH, viscosity, drug content, ex-vivo permeation studies and stability studies of TFs-gel. This was compared with LF-gel prepared by same procedure.&#x0D; Results: Maximum % EE (78.4±0.94), suitable vesicular size (128.6 nm) and maximum DI (34.9±1.9) was found in TFs-TW-80 and selected for gel development. In vitro drug release data from TFs-TW-80, plain drug solution and liposomal formulation (LF) revealed that % cumulative drug released in TFs-TW-80 was found maximum (89.5±0.12 %) in 20 min than others. It was 2.1 times higher than LF and 3.3 times higher than the plain drug. SEM study showed spherical shape of vesicles. The drug contents in the TFs and LF gels were found to be 92 to 95%w/w. Partition coefficient for TFs-loaded gel was 1.04±0.03. Ex vivo permeation study from hairless rat skin showed that permeation of drug is described by firstly first-order kinetics than zero-order kinetics. The drug released from TFs-gel was found to be 1.7 times higher than LF-gel and about 1.9 times higher than plain drug. Flux from TFs-gel was 2.04 times greater than LF-gel and 3.28 times more than plan drug. Stability studies indicated that suitable storage condition for developed gel was temperature 25 °C or less, where the pH, potency and therapeutic efficacy of formulations remain constant.&#x0D; Conclusion: Thus, transdermal route has become one of the most successful and innovative focus for research in drug delivery of IVH loaded TFs-TW-80 to increase stability and bioavailability.

Nonionic Surfactant Properties of Amphiphilic Hyperbranched Polyglycerols.

The surfactant properties of amphiphilic hyperbranched polyglycerols (HPGs) were investigated. The HPGs were prepared by ring-opening multibranching polymerization of glycidol using hydrophobic initiators of varying size and structure. The cloud points for all HPG surfactants were found to be >80 °C in deionized water with >1 wt % NaCl. The HPG surfactants with hydrophilic-lipophilic balance values between 16 and 18 were found to form stable octanol/water (o/w) emulsions within a 24 h period. Several surface properties, including critical micelle concentration (CMC), efficiency of surface tension reduction (pC20), effectiveness of surface tension reduction (γCMC), surface excess concentration at the CMC (Γmax), minimum area/molecule at the interface (Amin), and the CMC/C20 ratio of the HPG surfactants were measured in deionized water at 22.6 °C. In general, increasing HPG size was marked by an increase in minimum surface area per molecule (Amin) at the aqueous liquid/air interface. This increase in size also led to lower CMC and greater pC20 values of HPG surfactants prepared with Tergitol 15-S-7 initiator (HPG 5a-5d), a commercially available ethylene glycol oligomer with a branched hydrophobic tail.

Synthesis of highly stable κ/ι-hybrid carrageenan micro- and nanogels via a sonication-assisted microemulsion route

Novel carrageenan micro- and nanogels were developed via a sonication-assisted microemulsion processing route. The diameter of the dry samples ranged 197.3 −421.35 nm whereas the diameter of the samples suspended in water ranged 467.8–605.9 nm. Hybrid κ/ι-carrageenan, rather than κ- or ι-carrageenan was used for the first time for the preparation of micro- and nanogels. KCl was used as a cross-linking agent and Tween 80 was used as surfactant. The micro- and nanogels suspended in water were found to simultaneously exhibit a lower diameter, and a lower swelling ratio with higher Tween 80 content. The micro- and nanogel suspension yields a zeta potential value of −50.5 mV, superior to values reported elsewhere for pure κ- or ι-carrageenan micro- and nanogels. The high stability was attributed to the high hydrophile-lipophile balance (HLB = 15) value of Tween 80. These results suggest that hybrid κ/ι-carrageenan micro- and nanogels are promising candidates for smart therapeutics applications.

Nonionic Surfactant Blends to Control the Size of Microgels and Their Catalytic Performance during Glycoside Hydrolyses

In a proof of concept study, a series of nonionic surfactant blends derived from Tween 80 and Span 80 were used to prepare catalytic microgels from stabilized droplets in miniemulsions. The goal of this study is to optimize the catalytic efficiency of microgels by decreasing their particle size with surfactants that are custom-made for the respective prepolymerization mixture. The effectiveness of the approach is examined by evaluating the catalytic efficiency of the resulting microgels in comparison to their counterparts made in the presence of ionic sodium dodecyl sulfate (SDS) solution. Spherical particles with hydrophilic–lipophilic balance (HLB) value dependent mean hydrodynamic diameters between 99 and 200 nm are obtained. Addition of Cu(II) ions and selected other transition metal ions activated the dormant catalysts for cleavage of glycosidic bonds in 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid (HEPES) buffer at pH 7.00 and 37 °C using a fluorescent model substrate. The highest proficiency for the catalytic hydrolysis was observed for Cu(II)-containing microgels (kcat/KM × knon = 870 000) with the lowest diameter indicating an almost twofold better stabilization of the transition state compared to a microgel prepared in the presence of ionic SDS solution. The study establishes a correlation of the HLB value of the nonionic surfactant blend used during material synthesis to the particle size and catalytic performance of the resulting microgels.

Preparation of stable inverse emulsions of hydroxyethyl methacrylate and their stability evaluation by centrifugal coefficient

Several inverse emulsions were prepared with different hydrophilic-lipophilic balance (HLB) values using different water/oil ratios, temperatures and monomer and emulsifier concentrations by uniform stirring for more than 30 min. The stability of inverse emulsion was characterized by centrifugal coefficient. The emulsion form, either oil/water (O/W) or water/oil (W/O) was characterized by optical microscope and conductivity measurements. The results showed that HLB value, water/oil ratio and temperature could have an effect on the emulsion stability and emulsion form. When the HLB value of emulsifier is about 8.4, the water to oil ratio is about 1:1 and the temperature is at about 25 °C, inverse emulsion in the form of water in oil (W/O) was found to be the most stable. Here, the stablilty of emulsions was studied in relation to temperature and we found that 25 °C (room temperature) is the best for obtaining the most stable inverse emulsion, which is also most suitable for the redox initiation in this system. In the present study, we showed that temperature has a significant influence on the structure morphology and stability of inverse emulsion and hence, it is necessary to select the appropriate reaction temperature for inverse emulsion polymerization. This is a novel result. A decrease of the content of hydroxyethyl methacrylate in aqueous solution with an increase of emulsifier concentration in emulsion was found to elevate the stability of inverse emulsion. The addition of trace electrolytes in the emulsion, however, led to greatly reduced stability of the inverse emulsion.

Exploring the Impact of Surfactant Type and Digestion: Highly Digestible Surfactants Improve Oral Bioavailability of Nilotinib.

The scientific rationale for selection of the surfactant type during oral formulation development requires an in-depth understanding of the interplay between surfactant characteristics and biopharmaceutical factors. Currently, however, there is a lack of comprehensive knowledge of how surfactant properties, such as hydrophilic-lipophilic balance (HLB), digestibility, and fatty acid (FA) chain length, translate into in vivo performance. In the present study, the relationship between surfactant properties, in vitro characteristics, and in vivo bioavailability was systematically evaluated. An in vitro lipolysis model was used to study the digestibility of a variety of nonionic surfactants. Eight surfactants and one surfactant mixture were selected for further analysis using the model poorly water-soluble drug nilotinib. In vitro lipolysis of all nilotinib formulations was performed, followed by an in vivo pharmacokinetic evaluation in rats. The in vitro lipolysis studies showed that medium-chain FA-based surfactants were more readily digested compared to long-chain surfactants. The in vivo study demonstrated that a Tween 20 formulation significantly enhanced the absolute bioavailability of nilotinib up to 5.2-fold relative to an aqueous suspension. In general, surfactants that were highly digestible in vitro tended to display higher bioavailability of nilotinib in vivo. The bioavailability may additionally be related to the FA chain length of digestible surfactants with an improved exposure in the case of medium-chain FA-based surfactants. There was no apparent relationship between the HLB value of surfactants and the in vivo bioavailability of nilotinib. The impact of this study's findings suggests that when designing surfactant-based formulations to enhance oral bioavailability of the poorly water-soluble drug nilotinib, highly digestible, medium chain-based surfactants are preferred. Additionally, for low-permeability drugs such as nilotinib, which is subject to efflux by intestinal P-glycoprotein, the biopharmaceutical effects of surfactants merit further consideration.

Investigation Utilizing the HLB Concept for the Development of Moisturizing Cream and Lotion: In-Vitro Characterization and Stability Evaluation

The current study aims to utilize the concept of the hydrophilic–lipophilic balance (HLB) value of ingredients for the development of a stable emulsion-based moisturizing cream and lotion for cosmetic application. The combination of a hydrophilic and lipophilic emulsifier such as glyceryl stearate (HLB value 3.8) and PEG-100 stearate (HLB value 18.8) were found to be effective to emulsify the chosen oil phase system at a specific concentration to achieve the required HLB for the development of the stable emulsion-based system. The developed formulation was characterized for pH, viscosity, spreadability, rheology, and droplet morphology. The influence of carbopol® ETD 2020 and the concentration of the oil phase on the rheology of the product was investigated and found to be significant to achieve the required thickening to convert the lotion into a cream. The formulation system developed through utilizing the concept of HLB was compared to a product developed through the conventional approach. It was observed that the utilization of the HLB method for the development of an emulsion-based product is a promising strategy compared to the conventional method. The physical stability and thermodynamic stability tests were carried out under different storage conditions. It was observed that the developed formulation was able to retain its integrity without showing any signs of instability during storage.

Investigation the Stability of Water in Oil Biofuel Emulsions Using Sunflower Oil

Targets to reduce CO2 emissions by 75% and NOx emissions by 90% by 2050 in aviation have been set by The Advisory Council for Aviation Research and Innovation in Europe. Sustainable fuels, e.g., emulsified biofuel, have demonstrated promise in reducing emissions and greenhouse gases. The aim of this project is to investigate the stability of a water in oil emulsion using sunflower oil. The primary objective is to achieve an emulsion which is stable for at least 4 days, and the secondary objective is to investigate how altering the emulsification parameter values of the surfactant hydrophilic-lipophilic balance (HLB), energy density and sonotrode depth in an ultrasonication procedure can impact the stability. The stability of each emulsion was measured over a period of 14 days. The main outcome is that two of the 14 emulsions made remained stable for at least 14 days using a surfactant HLB of five, which proved to be the optimum value from those tested. The results also show that, by using the sonotrode in a higher starting position, emulsions achieved a greater stability. Furthermore, over-processing of the emulsion was determined, with the point of over-processing lying between an energy density of 75 and 200 W.s/mL.

Development of nanoemulsion formulation of mustard oil, its chemical characterization and evaluation against post harvest anthracnose pathogens

Oil-in-water nanoemulsion (NE) formulations of mustard oil known for prominent antimicrobial activities have been prepared, characterized and tested against anthracnose pathogens Colletotrichum musae and Colletotrichum capsici. Physico-chemical properties viz., appearance, stability, pH, centrifugation, storage-stability, thermodynamic stress, persistent foam, droplets size and zeta potential were tested for the NE formulations. The NE formulations were prepared using low energy emulsification process with the optimized composition (w/w) of mustard oil (5%), Tween 20 and sodium dodecyl benzene sulfonate emulsifiers blend (20–30%), co-surfactants (4%), and de-ionized water. The required hydrophile-lipophile balance value for emulsifier blends was determined as 11.39–11.74. Only 3 (viz., NF2, NF3 and NF6) out of 15 NE formulations with transparent faint yellow color (pH 6.3) passed all the physico-chemical parameters tested. Among these, NF2 (foam height < 1 mL) was selected for further study. The average diameter (23 nm), polydispersity index (0.38) and zeta potential (− 12 mV) of mustard oil droplets in NF2 indicated the formation of a stable and homogeneous NE formulation. Application of NF2 exhibited low level of sensitivity to C. capsici and C. musae with maximum growth inhibition (6.2–7.3%) at 1.0% dose. Out of 18 phytochemicals detected in mustard oil by gas chromatography-mass spectrometry, 11 have been reported with antifungal properties including trans-13-octadecenoic acid with the highest relative abundance. The observed antifungal activity may be attributed to the presence of at least some or all the identified phtytochemicals in mustard oil. Further bio-assay on sensitive plant pathogenic fungi is underway to explore the application of the developed NE formulation.

A promising approach to develop nanostructured lipid carriers from solid lipid nanoparticles: preparation, characterization, cytotoxicity and nucleic acid binding ability

We aimed to develop nanostructured lipid carriers (NLCs) displaying similar characteristics – particle size, polydispersity index, and zeta potential – with the model solid lipid nanoparticles (SLNs) for better comparability. By considering the hydrophilic-lipophilic balance values of solid and liquid lipids, five out of six NLCs and eight out of eight cationic NLCs (cNLCs) were successfully prepared with similar characteristics to their precursor SLN and cationic SLNs (cSLNs), respectively. Among cationic formulations, two cSLNs containing different surfactant/co-surfactant concentrations (4% and 8% S/CoS; w/w) and their cNLC versions prepared with Labrafac lipophile WL 1349 (LWL) or Labrafac PG were selected to compare cytotoxicity, stability, and nucleic acid binding ability. All formulations are well-tolerated by L-929 cells, cSLNs being least toxic. The formulations containing 4% S/CoS had higher stability after 24-months. All nanoparticles formed complexes with pDNA (Binding ability: cNLCs > cSLNs). cSLN and LWL-cNLC containing 4% S/CoS showed the highest pDNA binding capacity in each group, and their spherical/oval shape was revealed by electron microscopy. However, they did not form complexes with siRNA. The developed approach has the potential to simplify the production of (c)NLCs having similar physicochemical properties with the optimum (c)SLN and may provide better insight for (c)SLN vs. (c)NLC comparison studies.

Comprehensive Screening of Drug Encapsulation and Co-Encapsulation into Niosomes Produced Using a Microfluidic Device

Microfluidics is a very facile and fast method of particulate production. Besides, it enables the manufacturing of size tuned particulate systems. Niosomes due to structural similarities have importance as alternative drug delivery systems to liposomes. Niosomes can be encapsulated or co-encapsulated with hydrophilic and lipophilic drugs. The research presented here includes the optimization of method parameters for niosome production as well as evaluation of the efficiency of microfluidics to encapsulate and co-encapsulate the drugs. For this purpose, metformin (MET) and garcinol (GC) were the model drugs. Two different non-ionic surfactants (NIS), namely Tween-20 and Span-60 with significant difference in hydrophilic-lipophilic balance (HLB) value, were chosen to analyze their efficiency to form niosomes and encapsulate one or more drugs.

Formation and stability of Eucommia ulmoides Oliver seed oil-loaded inverse microemulsion formed by food-grade ingredients and its antioxidant activities.

Eucommia ulmoides Oliver seed oil (E.u oil) as a functional oil is rich in many natural active components such as α-linolenic acid (56% to 63%), vitamin E, aucubin, and so on. In this study, water-in-oil (W/O) microemulsions composed of Eucommia ulmoides Oliver seed oil, distilled water, a blend of Sorbitan monooleate 80 (Span 80) and Polysorbate (20) sorbitan monooleate (Tween 80), and propylene glycol were prepared for improving the compatibility of Eucommia ulmoides Oliver seed oil. Pseudoternary phase diagrams were built to illustrate the phase behavior of the microemulsions, based on hydrophilic-lipophilic balance values, cosurfactant type, the proportion of cosurfactant, and the changing environmental stress. Dynamic light scattering, transmission electron microscopy, and electrical conductivity measurements were performed to characterize the microstructural aspects. The optimum process conditions at which the Eucommia ulmoides Oliver seed oil-loaded microemulsion had good tolerance to pH and salinity were: Propylene glycol served as cosurfactant, water-Propylene glycol, and Span 80-Tween 80 ratios separately kept constant at 1:1 and 6:4. These microemulsions with narrow size distribution, nanoscale particle size (below 60nm), transparent appearance had a wide range of oil phase content and free-radical scavenging capacity toward DPPH and ABTS radicals with half-maximal inhibitory concentration (IC50 ) values of 49.20 and 33.43mg/mL, respectively. PRACTICAL APPLICATION: This nanostructure, environmental stability, and antioxidant activity of microemulsions containing Eucommia ulmoides Oliver seed oil is a potential delivery system as an alternative to α-linolenic acid and can be used for the delivery of peptides, proteins, antioxidants, and water-soluble nutrients.

Microemulsions based on polyglycerol polyricinoleate as drug delivery systems

The aim of the work is to develop composition of reverse microemulsion stabilized by the surfactant from a number of polyglycerol polyricinoleates for encapsulating water-soluble biologically active substance (BAS) and studying the kinetics of its release into the medium simulating the medium of the small intestine. Materials and methods. Possible stable (equilibrium) phases of the reverse microemulsion in the pseudoternary system water–PG-3-PR/Tween 80–paraffin oil were determined by titration of surfactant/co-surfactant mixtures–oil in water with hydrophilic-lipophilic balance (HLB) values of the surfactant mixture ranging from 4.0 to 7.0. Stability of a number of compositions during storage at 20 °C for 6 months was studied. Based on the obtained data, a composition was selected for encapsulating methylene blue (MS) dye as a model of a water-soluble biologically active substance. Microemulsion was obtained by mixing paraffin oil and surfactants with selected mass ratio followed by the addition of an aqueous phase. Reverse microemulsion morphology was evaluated with transmission electron microscopy (TEM). To evaluate the in vitro drug release rate, aliquots of an aqueous dye solution (control sample) and MB-containing microemulsions were placed in dialysis bags and immersed in 0.01 M phosphate-buffered saline (PBS) (pH 7.4) in a thermostatic shaking incubator at 180 rpm and 37 °C. Aliquots of the release medium were selected at predetermined time intervals and the concentration of MB dye was determined using a UV spectrophotometer at 660 nm. Results. Composition containing 13.5 wt% paraffin oil, 76.5 wt% mixture of PG3-PR/Tween 80 (HLB 5.5) and 10 wt% water was chosen to encapsulate the biologically active agents. Number average droplet diameter in the dispersed phase of the obtained microemulsion was 55 nm. Dye-loaded microemulsion sample showed a prolonged release of biologically active substances within 48 hours of the experiment (15.2%) and low initial release rate. Conclusion. Possible stable phases of reverse microemulsion in the pseudoternary system water–PG-3-PR/Twin 80–paraffin oil were determined in the course of the work and optimal microemulsion composition for encapsulating medicinal substances was found. It was shown that the resulting microemulsion system provides a sustained release of methylene blue as a model of a water-soluble biologically active substance in a medium simulating medium of the small intestine. The obtained data allow to consider this composition as a potential nanoscale system for the sustained delivery of water-soluble drugs.