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

Author:

Higuchi Celio Takashi,Sales Caroline Cianga,Andréo-Filho NewtonORCID,Martins Tereza Silva,Ferraz Helena Onishi,Santos Yasmin Rosa,Lopes Patricia SantosORCID,Grice Jeffrey Ernest,Benson Heather Ann ElizabethORCID,Leite-Silva Vania Rodrigues

Abstract

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.

Funder

Fundação de Amparo à Pesquisa do Estado de São Paulo—FAPESP

Publisher

MDPI AG

Subject

Paleontology,Space and Planetary Science,General Biochemistry, Genetics and Molecular Biology,Ecology, Evolution, Behavior and Systematics

Reference62 articles.

1. Trends in Insect Repellent Formulations: A Review;Tavares;Int. J. Pharm.,2018

2. WMP (2022, November 16). What Are Mosquito-Borne Diseases?. Available online: https://www.worldmosquitoprogram.org/en/learn/mosquito-borne-diseases.

3. (2022, November 16). CDC Mosquito-Borne Diseases, Available online: https://www.cdc.gov/niosh/topics/outdoor/mosquito-borne/default.html#:~:text=Diseases%20that%20are%20spread%20to,from%20diseases%20spread%20by%20mosquitoes.

4. Resistance of Aedes Aegypti to Organophosphates in Several Municipalities in the State of Rio de Janeiro and Espírito Santo, Brazil;LIma;Am. J. Trop. Med. Hyg.,2003

5. Resistance of Aedes Aegypti from the State of São Paulo, Brazil, to Organophosphates Insecticides;Macoris;Mem. Inst. Oswaldo Cruz,2003

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前同舟云学术共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3