Development of a Nanotechnology Matrix-Based Citronella Oil Insect Repellent to Obtain a Prolonged Effect and Evaluation of the Safety and Efficacy.

Mosquito-borne diseases affect millions of people worldwide each year, and the use of a topically applied insect repellent is an economically viable preventative health practice. The general objective of this work was to encapsulate citronella oil (CO) in a nanostructured lipid carrier (NLC) to formulate a topical repellent with a long duration of efficacy on the skin and a good safety profile based on minimizing skin penetration. In the studied CO, the main chemical constituents of geraniol, citronellal, and citronellol were identified and subsequently used as markers for the in vitro skin permeation testing (IVPT). An optimal NLC encapsulating CO formulation was developed and had an average particle size of 350 nm. The NLC was then formulated in combination with CO at ratios of 2:1, 1:1, and 1:2 CO:NLC-CO as oil-in-water (O/W) emulsions and compared to CO in the same O/W emulsion base (all at 10% CO in the final O/W topical formulation). The markers geraniol, citronellol, and citronellal were detected in all samples tested F1 (10% CO in O/W emulsion) and F3 (10% CO/NLC-CO 1:1 in O/W emulsion). Even the percentages of F3 markers were higher than F1. The recovery of the percentage balance (based on the total remaining on the skin surface, on the skin, and penetrated through the skin to the receptor) of geraniol, citronellol, and citronellal markers for F1 and F3 was 7.70% and 11.96%; 25.51% and 31.89%; and 5.09% and 4.40%, respectively. The nanoparticle lipid solid forms a repellent reservoir on the skin surface, releasing the active ingredients slowly through volatilization, extending the repellent action, and reducing permeation through the skin. It is possible to assume that the remaining 92.30% and 88.03%; 74.49% and 68.11%; and 94.10% and 95.60% of geraniol, citronellol, and citronellal markers of F1 and F3, respectively, were lost to evaporation. In the in vivo efficacy test carried out with the Aedes aegypti mosquito, F3 was the optimal formulation, providing the greatest repellent action compared to free oil in O/W emulsion. Thermal analysis showed that the NLC-CO raised the boiling point of the encapsulated CO compared to the free oil, suggesting that the controlled release of the CO was a possible mechanism for its prolonged effect. We concluded that the nanocarriers developed with CO were stable and provided improved mosquito-repellent efficacy with minimal skin penetration of the CO actives over 24 h. Indeed, regardless of whether the CO was applied as free oil, a 1:1 mixture of CO (pure/free oil) or NLC-CO applied in an O/W emulsion can be considered safe for topical application due to minimal skin penetration.

Topical Mosquito Repellent Formulations for Enhanced Repellency Time and Reduced Toxicity.

Mosquito-borne diseases such as dengue, malaria, yellow fever, chikungunya and Zika virus affect millions of people worldwide each year. Vector control and personal protection are very important to minimize the spread of diseases, and the use of repellent is an economic practice to prevent them. The application of repellent, which acts on the skin to form a vapor layer with a repellent odor to mosquitos, is recommended as an economic prevention and practice. The natural botanical product Citronella is an effective mosquito repellent due to the high concentrations of active chemical constituents present, notably terpenic alcohols. However, citronella tends to evaporate quickly from the skin surface, resulting in a rapid loss of activity. Strategies to increase repellency time, while at the same time minimizing toxicity, are major focuses of research and development in natural repellent products. Here we highlight the role of extended-release systems (ERS) of citronella oil in this approach.

Urea incorporated into ordered mesoporous silica for potential cosmetic application

Urea's thermal instability and burning on sensitive skin can cause problems for cosmetic formulations. To overcome these drawbacks, urea was incorporated into ordered mesoporous silica (SBA-15). SBA-15 was synthesized using tetraethyl orthosilicate and Pluronic® P123 in an acid medium. Urea (20 wt.%) was incorporated into calcined SBA-15 by the incipient wetness impregnation method. Several techniques were used to characterize the samples. Skin hydration and transepidermal water loss were measured using Corneometer® CM 825 PC and Tewameter® 300 TM. Results showed that the structural properties of SBA-15Urea were similar to pure SBA-15, indicating that SBA-15 remained structured even after urea incorporation. Nitrogen physisorption data showed the volume and surface area of the pores in SBA-15Urea were much lower than those in SBA-15, demonstrating that urea was deposited inside the mesopores. In vivo moisturization studies revealed that SBA-15Urea was not able to reduce transepidermal water loss compared to the other products and control, while forming a non-occlusive surface film on the skin. We conclude that incorporation of urea in the pores of the inorganic SBA-15 matrix is a promising approach to enhancing its stability and providing a prolonged moisturizing effect.

Immunological and microbiological activity of Davilla elliptica St. Hill. (Dilleniaceae) against Mycobacterium tuberculosis.

Mycobacterium tuberculosis is responsible for over 8 million cases of tuberculosis (TB) annually. Natural products may play important roles in the chemotherapy of TB. The immunological activity of Davilla elliptica chloroform extract (DECE) was evaluated in vitro by the determination of hydrogen peroxide (H2O2), nitric oxide (NO), and tumor necrosis factor-alpha (TNF-alpha) release in peritoneal macrophages cultures. DECE was also tested for its antimycobacterial activity against M. tuberculosis using the microplate alamar blue assay. DECE (50, 150, 250 microg/ml) stimulated the production of H2O2 (from 1,79 +/- 0,23 to 7,27 +/- 2,54; 15,02 +/- 2,86; 20,5 +/- 2,1 nmols) (means +/- SD), NO (from 2,64 +/- 1,02 to 25,59 +/- 2,29; 26,68 +/- 2,41; 29,45 +/- 5,87 micromols) (means +/- SD) and TNF-alpha (from 2,44 +/- 1,46 to 30,37 +/- 8,13; 38,68 +/- 1,59; 41,6 +/- 0,90 units/ml) (means +/- SD) in a dose-dependent manner and also showed a promising antimycobacterial activity with a minimum inhibitory concentration of 62,5 microg/ml. This plant may have therapeutic potential in the immunological and microbiological control of TB.

Immunological and microbiological activity of Davilla elliptica St. Hill. (Dilleniaceae) against Mycobacterium tuberculosis

Mycobacterium tuberculosis is responsible for over 8 million cases of tuberculosis (TB) annually. Natural products may play important roles in the chemotherapy of TB. The immunological activity of Davilla elliptica chloroform extract (DECE) was evaluated in vitro by the determination of hydrogen peroxide (H2O2), nitric oxide (NO), and tumor necrosis factor-alpha (TNF-alpha) release in peritoneal macrophages cultures. DECE was also tested for its antimycobacterial activity against M. tuberculosis using the microplate alamar blue assay. DECE (50, 150, 250 mug/ml) stimulated the production of H2O2 (from 1,79 ± 0,23 to 7,27 ± 2,54; 15,02 ± 2,86; 20,5 ± 2,1 nmols) (means ± SD), NO (from 2,64 ± 1,02 to 25,59 ± 2,29; 26,68 ± 2,41; 29,45 ± 5,87 mumols) (means ± SD) and TNF-alpha (from 2,44 ± 1,46 to 30,37 ± 8,13; 38,68 ± 1,59; 41,6 ± 0,90 units/ml) (means ± SD) in a dose-dependent manner and also showed a promising antimycobacterial activity with a minimum inhibitory concentration of 62,5 mug/ml. This plant may have therapeutic potential in the immunological and microbiological control of TB.