Determination of the Real Influence of the Addition of Four Thickening Agents in Creams Using Rheological Measurements

This study aimed to characterize different emulsions obtained by the addition of four thickening agents, using rheological measurements, beyond analyzing the emulsions by polarized light microscopy looking for liquid crystals on them. The addition of these four thickening agents did not modify the base emulsion rheology, only an improvement in the sensory of the formulation was verified. The polarized light microscopy showed the formation of liquid crystalline structures in all the formulations, thus, the thickening agents did not influence in this parameter too. However, the emulsions could be considered appropriated for cosmetic purposes, probably being highly physically stable.     

Surfactant-Free Multiple Pickering Emulsions Stabilized by Combining Hydrophobic and Hydrophilic Nanoparticles

A series of W/O/W or O/W/O emulsion stabilized solely by two different types of solid nanoparticles were prepared by a two-step method. We explored the option of particular emulsifiers for the multiple Pickering emulsions, and a variety of nanoparticles (silica, iron oxide, and clay) only differing in their wettability was used. The primary W/O emulsion was obtained by the hydrophobic nanoparticles, and then the hydrophilic nanoparticles were used as emulsifier in the secondary emulsification to prepare the W/O/W emulsion. In a similar way, the primary O/W emulsion of the O/W/O emulsion was stabilized by the hydrophilic nanoparticles, while the secondary emulsification to prepare the O/W/O emulsion was effected with the hydrophobic nanoparticles. The resultant multiple Pickering emulsion was stable to coalescence for more than 3 months, except the W/O/W emulsions of which the secondary emulsion stabilized by clay nanoparticles became a simple O/W emulsion in a day after preparation. Moreover, the temperature and pH sensitive poly(N-isopropylacrylamide-co-methacrylic acid) (P(NIPAm-co-MAA)) microgels were introduced as an emulsifier for the secondary emulsification to obtain the stimulus-responsive multiple W/O/W emulsion. Such microgel-stabilized multiple emulsions could realize the efficient controlled release of water-soluble dye, Rhodamine B (RB) on demand in a multiple-emulsion delivery system.      

Poloxamer-Stabilized Topical Miconazole Nitrate-Loaded Microemulsion: Formulation Design and Characterization

Miconazole nitrate-loaded microemulsion based on Tween 80 and propylene glycol, castor oil and water with and without Poloxamer 407 was prepared and characterized with respect to drug content, stability, antifungal, and physicochemical properties and ex vivo drug release using a modified Franz diffusion apparatus. Results obtained revealed homogeneous and stable microemulsions with excellent physicochemical properties, permeation coefficients and fluxes, and increased in vitro antifungal activity (～1.2 times) against clinically isolated Candida albicans when compared to a commercial topical miconazole (Fungusol) solution. Poloxamer-stabilized microemulsion could offer a better and more reliable approach of delivering miconazole than both the unstabilized and Fungusol formulations.      

Development of Ciprofloxacin HCl-Based Solid Lipid Nanoparticles Using Ouzo Effect: An Experimental Optimization and Comparative Study

This study was performed to develop solid lipid nanoparticles of water soluble drug ciprofloxacin HCl using quick solvent diffusion evaporation technique (ouzo effect). A statistical central composite rotatable design was used to study the effect of independent variables. In the subsequent step, optimized SLN were further compared with nanostructured lipid carriers and nanoemulsion for particle size, zeta potential, drug entrapment, drug release, and stability. Comparative study revealed that the drug encapsulation efficiencies were enhanced by adding the Capmul MCM C8 into the solid lipid nanoparticles. The in vitro drug release study of all three formulations showed rapid release for nanoemulsion while controlled release for SLN. Stability study of all the formulation proved that nanostructured lipid carrier and SLN could prevent the drug expulsion during the storage period. Results of the study suggested that the SLN and nanostructured lipid carriers produced by the principle of ouzo effect could potentially be exploited for better drug entrapment efficiency and controlled drug release of water soluble actives.     

Polyacrylic Acid Modifies Local and Lateral Mobilities in Lipid Membranes

Polyacrylic acid (PAA) is a promising polymer for engineering lipid-based drug-delivery vesicles. Its unique properties allow lowering drug dose and delivery the drug close to the site of its release. To design a successful delivery scheme, however, it is important to understand on the molecular scale how the polymer interacts with lipids under various conditions in the human body. Some aspects of the PAA-lipid interaction can be revealed using physical methods, such as differential scanning microscopy, nuclear magnetic resonance spectroscopy, NMR-diffusometry, and infrared spectroscopy. This work discusses the use of these techniques as well as the peculiarities of preparing vesicular and microscopically aligned PAA-lipid systems.      

Lyotropic Liquid Crystal Formed in Oleyl Polyoxyethylene Solutions by Adding Different Additives: NaDC,Tween 80, Alkyl Esters

Lyotropic liquid crystalline of oleylpolyoxyethylene(20)(AEO₂₀)/oil/water system was investigated at 25°C. The phase behavior, microstructure, and rheological properties of liquid crystalline were investigated by rheological techniques and polarizingoptical microscopy in the presence of various additives including Tween 80, sodium deoxycholate (NaDC), isoamylacetate, butyl acetate, isopropyl myristate. Diagrams show that cubic phase transforms to hexagonal phase when a shorter chain length oil is applied or NaDC or Tween 80 is added to the system.Flow experiments indicate the shear-thinning properties and a plastic behavior. The turning points of flow curves of the system AEO₂₀ and system AEO₂₀/NaDC were found. The dynamic modulus increase with increase in water content however the tendency is weaken by adding NaDC. Frequency dependence of experimental G ′ and G ′ were fitted using the multiple Maxwell model the cubic LLCs described by three relaxation times while hexagonal LLCs described by 5–8 elements. When AEO₂₀ mixes with Tween 80, the hexagonal have a monotonic decrease distribution of relaxation times without valleys.     

In situ gelling hexagonal phases for sustained release of an anti-addiction drug

In this study, fluid precursor formulations for subcutaneous injection and in situ formation of hexagonal phase gels upon water absorption were developed as a strategy to sustain the release of naltrexone, a drug used for treatment of drug addiction. Precursor formulations were obtained by combining BRIJ 97 with propylene glycol (PG, 5-70%, w/w). To study the phase behavior of these formulations, water was added at 10-90% (w/w), and the resulting systems were characterized by polarized light microscopy. Two precursor formulations containing BRIJ:PG at 95:5 (w/w, referred to as BRIJ-95) and at 80:20 (w/w, referred to as BRIJ-80) were chosen. Naltrexone was dissolved at 1% or suspended at 5% (w/w). Precursor formulations were transformed into hexagonal phases when water content exceeded 20%. Water uptake followed second-order kinetics, and after 2-4h all precursor formulations were transformed into hexagonal phases. Drug release was prolonged by the precursor formulations (compared to a drug solution in PBS), and followed pseudo-first order kinetics regardless of naltrexone concentration. The release from BRIJ-80 was significantly higher than that from BRIJ-95 after 48 h. The relative safety of the precursor formulations was assessed in cultured fibroblasts. Even though BRIJ-95 was more cytotoxic than BRIJ-80, both precursor formulations were significantly less cytotoxic than sodium lauryl sulfate (considered moderate-to-severe irritant) at the same concentration (up to 50 μg/mL). These results suggest the potential of BRIJ-based precursor formulations for sustained naltrexone release.     

Synergetic Effect of Reactive Surfactants and Clay Particles on Stabilization of Nonaqueous Oil-in-Oil (o/o) Emulsions

Although surfactants and particles are often used together in stabilization of aqueous emulsions, the contribution of each species to such stabilization at the oil-water interface is poorly understood. The situation becomes more complicated if we consider the nonaqueous oil-oil interface, i.e, the stabilization of nonaqueous oil-in-oil (o/o) emulsions by solid particles and reactive surfactants which, to our knowledge, has not been studied before. We have prepared Pickering nonaqueous simple (o/o) emulsions stabilized by a combination of kaolinite particles and a nonionic polymerizable surfactant Noigen RN10 (polyoxyethylene alkylphenyl ether). Different pairs of immiscible oils were used which gave different emulsion stabilities. Using kaolinite with equal volumes of paraffin oil/formamide system gave no stable emulsions at all concentrations while the addition of Noigen RN10 enhanced the emulsion stability. In contrast, addition of Noigen RN10 surfactant to silicon oil-in-glycerin emulsions stabilized by kaolinite resulted in destabilization of the system at all concentrations. For all systems studied here, no phase inversion in simple emulsion was observed by altering the volume fraction of the dispersed phase as compared to the known water-based simple Pickering emulsions.      

Biocompatible lipidic formulations: phase behavior and microstructure

Biocompatible systems formulated for use in the food, cosmetic, and pharmaceutical fields are characterized. Ternary phase diagrams of mixtures of natural lipids (glycerol trioleate, glycerol monooleate, diglycerol monooleate, and lecithin) and water were investigated by means of optical microscopy in polarized light and by multinuclear NMR spectroscopy. All systems showed a microemulsion region at high oil content and a large area of coexistence of two liquid crystalline (hexagonal and lamellar) phases. 1H and 13C NMR self-diffusion measurements were used to characterize microstructural features of the microemulsions. On water dilution, the two-phase liquid crystalline region transforms into a creamy emulsion area where the droplets of water are stabilized by both the lamellar and the hexagonal phases, as indicated by 2H NMR measurements. Due to the very effective dispersing action of the two liquid crystalline phases, these emulsions show a high stability toward phase separation.     

Multi-Walled Carbon Nanotubes as a Cosurfactant for Highly Concentrated Emulsions

The role of multi-wall carbon nanotubes (MWCNT) as a solid surfactant in highly concentrated water-in-oil emulsions was investigated. MWCNT were dispersed in the oil phase. These suspensions are viscoplastic fluids with the yield stress increasing by more than 1000 times with addition of 2% MWCNT, which demonstrates intensive “structurizing” ability. After emulsion preparation, MWCNT were concentrated at the interface, stabilizing emulsions. The dependence of the inversion point on MWCNT concentration was found. Emulsions containing up to 94 wt% of the aqueous phase can be prepared only when MWCNT is combined with conventional surfactant. Rheological properties of such compositions were measured. It was established that emulsions stabilized by a combined surfactant were more stable in comparison to conventional surfactant stabilized emulsion.     

Removal of Mercury by Emulsion Liquid Membranes: Studies on Emulsion Stability and Scale Up

Emulsion liquid membranes (ELM) have received significant attention in the separation of various metal ions from industrial wastewater. Still efforts are needed to get the desired level of stability to overcome the hindrance in the application of ELM at industrial scale. In this paper, the effects of various parameters such as emulsification speed, concentration of cosurfactant, surfactant, carrier and impeller speed during extraction on the stability of an emulsion liquid membrane are studied. Dispersion destabilization of w/o emulsion is checked by Turbiscan. Drop size distribution and photomicrographs of the emulsions are also analyzed to evaluate stability of the emulsion. Instability of emulsion liquid membrane during extraction process is measured in terms of membrane breakage. A stable emulsion is used for the extraction of mercury from aqueous solution in small scale as well as in large scale.     

Curcumin-Encapsulated Hexagonal Liquid Crystalline Formed by Brij 97/NaDC Mixtures

The phase diagram of a five-components Brij 97-NaDC/IPM-PEG 400/H₂O system was determined at 25°C. The hexagonal liquid crystalline phase (H₁) was found in this system. By use of small-angle x-ray scattering (SAXS), polarization microscopy, and rheology techniques, the influence of composition, temperature, and addition of curcumin on H₁ phase was studied. It is shown that: 1) the investigated hexagonal liquid crystals exhibit a strong shear thinning behavior and viscoelasticity and the strength of the network of H₁ phase becomes weaker with increasing oil content; 2) the frequency-dependent moduli of H₁ samples decreases as the temperature increases and the steady-state limiting viscosity of the hexagonal samples shows an Arrhenius-like dependence on temperature; and 3) samples in H₁ phase containing curcumin retained their organized hexagonal structure. The SAXS results show that the curcumin molecules may be solubilized both into the apolar core of cylinders together with IPM and in the polar domain coexisting with PEG 400 between the cylinders. When curcumin is encapsulated in samples with low oil content, there is a significant decrease in the frequency-dependent moduli. The tendency of frequency behavior for samples incorporating curcumin as a function of temperature is weakened.     

Preparation and Characterization of Polymeric Nanocapsules Produced by in Situ Polymerization From Nanoemulsions Produced by Direct Emulsification

Polymeric nanoparticles constitute an important drug delivery system with controlled release profile. This article describes a new way to produce polymeric nanocapsules using a vegetable oil nanoemulsion as template. The process occurs in two steps: First, a nanoemulsion was obtained with a low-energy method based on phase inversion emulsification, using 2-ethylhexyl acrylate as lipophilic monomer. The in situ polymerization of the nanoemulsion droplets is induced by the addition of polymerization catalyzers. The mean size of the polymeric nanoparticles was evaluated by photon correlation spectroscopy and atomic force microscopy. Both techniques showed the formation of polymeric nanocapsules with a mean particle size less than 300 nm.     

Influence of Mixing Speed in Liquid Crystal Formation and Rheology of O/W Emulsions Containing Vegetable Oils

The process parameters are important in the development of emulsions containing liquid crystals. Thus, we studied the influence of the mixing speed in microscopic and rheological features. Oil-in-water emulsions using vegetable oils and nonionic surfactant were developed employing gradual raise of the mixing speed. It decreased the liquid crystal formation and the density values, and increased apparent viscosity values. The most suitable mixing speed was 600 rpm, since it allowed the attainment of emulsion with better performance and presence of lamellar liquid crystals. However, all emulsions were stable in these experimental conditions and presented pseudoplastic behavior and tixotropy.     

Using Nanoparticle Tracking Analysis (NTA) to Decipher Mucoadhesion Propensity of Curcumin-Containing Chitosan Nanoparticles and Curcumin Release

Real-time nanoparticle tracking analysis (NTA) was used to evaluate the propensity of curcumin-containing chitosan nanoparticles (CUR-CS-NP) to muco adhere and release curcumin under simulated colon conditions. This novel procedure is relatively simple and fast and does not require use of animals, but more importantly, it permits the correlation of physical changes to the CUR-CS-NP with the observed behavior under simulated conditions in realtime. The CUR-CS-NP formed spontaneous aggregates in response to exposure to mucin. This observation correlated with curcumin release from CUR-CS-NP was observed in phosphate buffer (pH 7.4) where, 81% of curcumin was released within 6 hours. Atomic force microscopy imaging CUR-CS-NP exposed to mucin solution revealed a decorated surface of the CUR-CS-NP by mucin, consistent with expected electrostatic interactions between the two. The use of NTA, thus, provided us with a means of ascertaining the performance of the CUR-CS-NP under simulated colonic conditions and we propose that this prototype delivery system could be the basis for an effective colon mucoadhesive drug delivery system.      

Formation of Particle Coated Fusiform Droplets via Lowering Interface Tension with Polyaluminum Sulfate

It was found that the interface tension between water and alkenyl succinic anhydride (ASA) was significantly reduced by polyaluminum sulfate (PAS), increased considerably though by TiO₂ nanoparticle. PAS with basicity of 0.75 (PAS-0.75) reduced the interface tension to a larger extent than PAS with basicity of 0.3 (PAS-0.3). By reducing interface tension with PAS-0.75, ASA-in-water emulsion bearing fusiform geometries was constructed. The emulsion stabilized by PAS-0.3 and TiO₂ nanoparticle bore spherical shapes with the exception when mass fraction of TiO₂ nanoparticle was low, in which case fused nonspherical drops were formed. Forming nonspherical emulsion crucially depends on ASA-water interface tension, where a critical interface tension was identified to be 0.6–0.7 mN/m. The fusiform geometries were transformed into spherical shapes when interface tension was higher than 0.7 mN/m. Both the lowering mechanism of the interface tension and the formation mechanism of the fusiform emulsion were proposed.      

Natural Brazilian Raw Material to Develop O/W Emulsions Containing Lamellar Gel Phase (Development and Analysis of Emulsion with Vegetable Oils)

Oil-in-water emulsions were developed employing the HLB system and emulsion phase inversion (EPI) method. X-ray diffraction revealed that the anisotropic structures around the inner phase globules were lamellar gel network phases. The calculated distances between the lamellae made after preparation and 3 month latter showed that there was no swelling of the lamellar gel network indicating good stability and few changes during storage. The developed emulsions were stable and have potential to be employed for cosmetic and pharmaceutical purposes. The gel phase network and vegetal components seemed to be contributing factors.