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1.
Sci Rep ; 12(1): 2180, 2022 02 09.
Artigo em Inglês | MEDLINE | ID: mdl-35140283

RESUMO

Mosquito-borne infections like dengue, malaria, chikungunya, etc. are a nuisance and can cause profound discomfort to people. Due to the objectional side effects and toxicity associated with synthetic pyrethroids, N,N-diethyl-3-methylbenzamide (DEET), N,N-diethyl phenylacetamide (DEPA), and N,N-di ethyl benzamide (DEBA) based mosquito repellent products, we developed an essential oil (EO) based mosquito repellent cream (EO-MRC) using clove, citronella and lemongrass oil. Subsequently, a formulation characterization, bio-efficacy, and safety study of EO-MRC were carried out. Expression of Anti-OBP2A and TRPV1 proteins on mosquito head parts were studied by western blotting. In-silico screening was also conducted for the specific proteins. An FT-IR study confirmed the chemical compatibility of the EOs and excipients used in EO-MRC. The thermal behaviour of the best EOs and their mixture was characterized by thermogravimetric analysis (TGA). GC-MS examination revealed various chemical components present in EOs. Efficacy of EO-MRC was correlated with 12% N,N-diethyl benzamide (DEBA) based marketed cream (DBMC). Complete protection time (CPT) of EO-MRC was determined as 228 min. Cytotoxicity study on L-132 cell line confirmed the non-toxic nature of EO-MRC upon inhalation. Acute dermal irritation study, acute dermal dose toxicity study, and acute eye irritation study revealed the non-toxic nature of EO-MRC. Non-target toxicity study on Danio rerio confirmed EO-MRC as safer for aquatic non-target animals. A decrease in the concentration of acetylcholinesterase (AChE) was observed in transfluthrin (TNSF) exposed Wistar rats. While EO-MRC did not alter the AChE concentrations in the exposed animals. Results from western blotting confirmed that Anti-OBP2A and TRPV1 proteins were inhibited in TNSF exposed mosquitoes. Mosquitoes exposed to EO-MRC showed a similar expression pattern for Anti-OBP2A and TRPV1 as the control group. In silico study revealed eight identified compounds of the EOs play significant roles in the overall repellency property of the developed product. The study emphasizes the mosquito repellent activity of EO-MRC, which could be an effective, eco-friendly, and safer alternative to the existing synthetic repellents for personal protection against mosquitoes during field conditions.


Assuntos
Repelentes de Insetos/química , Repelentes de Insetos/farmacologia , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Creme para a Pele/química , Creme para a Pele/farmacologia , Acetilcolinesterase/metabolismo , Animais , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Culicidae , Cymbopogon/química , Composição de Medicamentos , Olho/efeitos dos fármacos , Feminino , Humanos , Repelentes de Insetos/efeitos adversos , Masculino , Simulação de Acoplamento Molecular , Óleos Voláteis/efeitos adversos , Óleos de Plantas/química , Coelhos , Ratos Wistar , Pele/efeitos dos fármacos , Creme para a Pele/efeitos adversos , Testes de Irritação da Pele , Syzygium/química , Terpenos/química , Peixe-Zebra
2.
Acta Trop ; 210: 105573, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-32505595

RESUMO

Mosquitoes (Diptera; Culicidae) are a biting nuisance and are of economic and health importance, especially for people living in tropical countries like India. Given the environmental concerns and health hazards of synthetic insecticides, development of natural products for the control of mosquito and mosquito-borne diseases are needed. In view of this, an essential oil based novel liquid vaporizer formulation with citronella and eucalyptus oils has been developed using a computer aided Artificial Neural Network and Particle Swarm Optimization (ANN-PSO) algorithm approach, aiming to predict the best optimized formulation (OF). Following the development, OF was characterized by Fourier Transform-Infra Red (FT-IR) spectroscopy and gas chromatography-mass spectroscopy (GC-MS). The efficacy of the OF was assessed against two major mosquito vectors viz. Anopheles stephensi and Aedes albopictus using a Peet-Grady chamber. Finally, toxicological impacts of the OF following its inhalation were investigated as per the Organization for Economic Co-operation and Development (OECD) guidelines. The results revealed all the ideal characteristics of the OF which were found to provide a slow release of up to 450 h at room temperature. Most importantly, the OF, exhibited 50% mosquito knock down (KT50) within 11.49±1.34 and 14.15±2.15 min against An. stephensi and Ae. albopictus respectively. Toxicity assessment showed a non toxic nature of the OF following inhalation. Thus the present development would be beneficial for controlling both An. stephensi and Ae. albopictus without any associated health hazards.


Assuntos
Cymbopogon , Eucalyptus , Inseticidas/administração & dosagem , Controle de Mosquitos/métodos , Nebulizadores e Vaporizadores , Óleos Voláteis/administração & dosagem , Aedes , Animais , Anopheles
3.
Expert Opin Drug Deliv ; 17(6): 863-880, 2020 06.
Artigo em Inglês | MEDLINE | ID: mdl-32274951

RESUMO

BACKGROUND: Defense personnel utilize capsaicin-based ocular sprays as non-lethal agents for law implementation during instances of mob violence. This study involves the capsaicin antagonist Capsazepine and the investigation of whether Capsazepine's antagonistic approach can be favorably utilized for defense utilization to block capsaicin-initiated pain and inflammation via the ocular pathway. RESEARCH DESIGN AND METHODS: Ocular capsazepine in situ gels were prepared with polymers Pluronic F-127 and Chitosan; optimized formulation was quantified in ocular tissues chromatographically and by in vivo live ocular imaging; anti-inflammatory efficacy was determined by eye irritation testing, corneal and retinal imaging, ocular prostaglandin estimation, and by viability and proliferation testing using human ocular cell lines, etc. RESULTS: A physicochemically stable Capsazepine in situ gel was formulated which showed little ocular irritation, considerable transcorneal permeation; was precisely quantified in ocular tissues by gas chromatography and in vivo live ocular imaging; showed anti-inflammatory properties against capsaicin by eye imaging experiments, prostaglandin declination and showed acceptable cytocompatibility when studied using human ocular cell lines. CONCLUSIONS: The fabricated in situ Capsazepine gel system might be promising for ocular delivery as it appears a pharmacologically potent and safe development, suitable for utilization in the ocular clinical therapy, provided there is additional research to substantiate it.


Assuntos
Capsaicina/análogos & derivados , Capsaicina/toxicidade , Irritantes/toxicidade , Animais , Capsaicina/farmacologia , Quitosana/química , Córnea/metabolismo , Feminino , Géis/química , Humanos , Masculino , Poloxâmero/química , Coelhos , Ratos , Ratos Wistar
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