Microencapsulation of Cymbopogon citratus D.C. Stapf Essential Oil with Spray Drying: Development, Characterization, and Antioxidant and Antibacterial Activities.

This study aimed to microencapsulate Cymbopogon citratus essential oil (CCEO) with spray drying using maltodextrin and gelatin. The effects of the operational conditions (inlet temperature (130-160 °C), CCEO concentration (5-15%), maltodextrin concentration (10-20%)) on the physicochemical stability and antioxidant and antibacterial activities of the CCEO microcapsules were determined. The CCEO microencapsulation process had yield and encapsulation efficiency values varying from 31.02 to 77.53% and 15.86-61.95%, respectively. CCEO microcapsules had antibacterial effects against Staphylococcus aureus and Escherichia coli with minimum inhibitory concentration varying from 10 to 20%, and total phenolic contents and antioxidant activities varying from 1632 to 4171.08 µg TE/g and 28.55-45.12 µg/g, respectively. CCEO microcapsules had average diameters varying from 5.10 to 10.11 µm, with spherical external structures without cracks and apparent pores. The best desirable process conditions for CCEO microencapsulation were process inlet temperature of 148 °C, maltodextrin concentration of 15%, and CCEO concentration of 10%. The results showed that CCEO microcapsules with increased stability and low degradation of active components can be prepared by spray drying using maltodextrin and gelatin with the production of microcapsules, which could be exploited as potential food preservatives.

Lemongrass (Cymbopogon citratus DC. Stapf) essential oil microparticles: Development, characterization, and antioxidant potential.

Maltodextrin (DE 20) and gelatin (4:1, w/w, respectively) were investigated as encapsulant materials for lemongrass (Cymbopogon citratus DC. Stapf) essential oil microencapsulation by freeze-drying. Three formulations were prepared: M1 (5% essential oil), M2 (10% essential oil), and M3 (15% essential oil), all in w/w. Microparticles were characterized by Fourier-transform infrared spectroscopy, scanning electron microscopy, water activity measurement, thermogravimetric and derivative thermogravimetric analysis, differential scanning calorimetry, and antioxidant activity analysis. Yield and microencapsulation efficiency were also determined. The results showed the promising potential of maltodextrin and gelatin as encapsulants and confirmed the feasibility of preparing C. citratus essential oil microparticles by freeze-drying. Microencapsulation improved the oil's thermal and oxidative stability, providing protection from volatilization and environmental conditions. Scanning electron microscopic examination of M1 revealed a closed, pore-free surface. M1 had higher yield and microencapsulation efficiency, showing great commercial potential for its reduced storage, transport, and distribution costs.

Microencapsulation of sweet orange essential oil (Citrus aurantium var. dulcis) by liophylization using maltodextrin and maltodextrin/gelatin mixtures: Preparation, characterization, antimicrobial and antioxidant activities.

This study evaluated maltodextrin (MD) and gelatin (GEL) in different ratios (SO1, MD only; SO2, MD and GEL = 2:1; and SO3, MD and GEL = 1:1, respectively) as wall materials to microencapsulation of sweet orange essential oil (SOEO, 10% w/w). SOEO microspheres were obtained by emulsification/lyophilization and characterized regarding the microencapsulation yield and efficiency, infrared spectroscopy, ultrastructural aspects (scanning electron microscopy, SEM), thermogravimetric (TG), derivative thermogravimetry (DTG) and differential exploratory calorimetry (DSC) and bioactive properties. Yield and SOEO microencapsulation efficiency (MEE) was of up to 90.19 and 75.75%, respectively. SEM analysis showed SO1, SO2 and SO3 microspheres with irregular shapes. Although improvements in thermal stability of all formulated microspheres were observed, TG and DTG curves indicated slower rates of volatilization and degradation of SOEO in SO1. DSC curves indicated that SO1, SO2 and SO3 microsphere formulations were effective in protecting SOEO, especially in relation to improvements in oxidative stability. Antibacterial and antioxidant properties, as well as total phenolic content of SOEO, were maintained in all formulated microspheres. SOEO microspheres can be prepared using MD and GEL and lyophilization, resulting in high yields, MEE, stability and preservation of antioxidant and antimicrobial properties.

Carnauba wax as a wall material for urea microencapsulation.

BACKGROUND: The high ureolytic activity of rumen microbiota is a concern when urea is used in ruminant feed, because it leads to fast urea conversion, resulting in possible intoxication and lower nitrogen utilization. This study intended to microencapsulate urea using carnauba wax to obtain slow-release systems in the rumen. The experiment was conducted in a randomized block design, arranged in a 3 × 2 factorial, with the urea encapsulated with carnauba wax in ratios of 1 : 2; 1 : 3, and 1 : 4 (UME 2; UME 3, and UME 4) and two particles sizes (small, PS ; and large, PL ). RESULTS: All formulations showed excellent properties, including inhibition of urea hygroscopicity. The formulation UME 2 exhibited the greatest yield (91.6%) and microencapsulation efficiency (99.6%) values, whereas the formulation UME 4 presented the greatest thermal stability (259.5 °C) and lowest moisture content (1.81%). The UME 2 formulation presented a slower release than the other UME formulations studied. CONCLUSION: The production of urea microspheres using carnauba wax was successful for all microencapsulated systems developed, evidencing the promising potential for use in ruminant animal diets. The UME 2 formulation with large particles is the most recommended because it permitted greater resistance to microbial attack, allowing a slower release of urea into the rumen, reducing the risk of intoxication or ruminal alkalosis. © 2018 Society of Chemical Industry.

In-vitro and in-vivo antileishmanial activity of inexpensive Amphotericin B formulations: Heated Amphotericin B and Amphotericin B-loaded microemulsion.

Amphotericin B (AmB) is effective against visceral leishmaniasis (VL), but the renal toxicity of the conventional form, mixed micelles with deoxycholate (M-AmB), is often dose-limiting, while the less toxic lipid-based formulations such as AmBisome® are very expensive. Two different strategies to improve the therapeutic index of AmB with inexpensive ingredients were evaluated on this work: (i) the heat treatment of the commercial formulation (H-AmB) and (ii) the preparation of an AmB-loaded microemulsion (ME-AmB). M-AmB was heated to 70 °C for 20 min. The resulting product was characterized by UV spectrophotometry and circular dichroism, showing super-aggregates formation. ME-AmB was prepared from phosphate buffer pH 7.4, Tween 80®, Lipoid S100® and Mygliol 812® with AmB at 5 mg/mL. The droplet size, measured by dynamic light scattering, was about 40 nm and transmission electron microscopy confirmed a spherical shape. Rheological analysis showed low viscosity and Newtonian behavior. All the formulations were active in vitro and in vivo against Leishmania donovani (LV9). A selectivity index (CC50 on RAW/IC50 on LV9) higher than 10 was observed for ME-AmB, H-AmB and AmBisome®. Furthermore, no important in vivo toxicity was observed for all the samples. The in-vivo efficacy of the formulations after IV administration was evaluated in Balb/C mice infected with LV9 (three doses of 1 mg/kg AmB) and no significant difference was observed between H-AmB, M-AmB, ME-AmB and AmBisome®. In conclusion, these two inexpensive alternative formulations for AmB showing good efficacy and selectivity for Leishmania donovani merit further investigation.

Development and Characterization of a Microemulsion System Containing Amphotericin B with Potential Ocular Applications.

BACKGROUND: Amphotericin B eye drops are widely used in the treatment of ocular infections. However, amphotericin's toxicity leads to low patient compliance and aggravation of symptoms. This work describes the development of a microemulsion system containing amphotericin B, aiming for its use in ocular applications. METHODS: The microemulsion was developed by the titration technique. The physicochemical characteristics were determined with both loaded and unloaded amphotericin B-microemulsion. The nanostructures were analyzed by polarized light microscopy. The microdilution method was used to establish the minimum inhibitory concentration against fungal strains, and, therefore, evaluate the microemulsion activity. Additionally, in order to evaluate the microemulsion toxicity an in vitro toxicity assay against red blood cells was performed. RESULTS: The performed studies showed that the presence of amphotericin B loaded into the system did not induce serious changes in the physicochemical properties of the microemulsion when compared to the unloaded system. The spectrophotometric studies depicted amphotericin B-self-associated species, which allow predicting its behavior in vitro. The high pressure liquid chromatography results revealed high drug content entrapment in the microemulsion droplet. Finally, the amphotericin B-microemulsion in vitro susceptibility test showed high activity against Candida strains and a low toxicity profile against red blood cells when compared to Fungizone®. CONCLUSION: The physicochemical characterization of the microemulsion demonstrated that its characteristics are compatible with the topical ocular route, making it eligible for consideration as a new and interesting amphotericin B-deliverydosage form to be used as eye drop formulation.

Physical factors affecting plasmid DNA compaction in stearylamine-containing nanoemulsions intended for gene delivery.

Cationic lipids have been used in the development of non-viral gene delivery systems as lipoplexes. Stearylamine, a cationic lipid that presents a primary amine group when in solution, is able to compact genetic material by electrostatic interactions. In dispersed systems such as nanoemulsions this lipid anchors on the oil/water interface confering a positive charge to them. The aim of this work was to evaluate factors that influence DNA compaction in cationic nanoemulsions containing stearylamine. The influence of the stearylamine incorporation phase (water or oil), time of complexation, and different incubation temperatures were studied. The complexation rate was assessed by electrophoresis migration on agarose gel 0.7%, and nanoemulsion and lipoplex characterization was done by Dynamic Light Scattering (DLS). The results demonstrate that the best DNA compaction process occurs after 120 min of complexation, at low temperature (4 ± 1 °C), and after incorporation of the cationic lipid into the aqueous phase. Although the zeta potential of lipoplexes was lower than the results found for basic nanoemulsions, the granulometry did not change. Moreover, it was demonstrated that lipoplexes are suitable vehicles for gene delivery.