RESUMO
@#The present study compares the in vitro effects of nanoparticles loaded pentamidine drug and conventional pentamidine on Leishmania tropica. Herein, pentamidine-loaded chitosan nanoparticles (PTN-CNPs) have been synthesized through an ionic gelation method with sodium tripolyphosphate (TPP). Next, the physical characteristics of PTN-CNPs were determined through the surface texture, zeta potential, in vitro drug release, drug loading content (DLC), and encapsulation efficacy (EE) and compared its efficacy with free pentamidine (PTN) drug against promastigotes and axenic amastigotes forms of L. tropica in vitro. The PTN-CNPs displayed a spherical shape having a size of 88 nm, an almost negative surface charge (-3.09 mV), EE for PTN entrapment of 86%, and in vitro drug release of 92% after 36 h. In vitro antileishmanial activity of PTN-CNPs and free PTN was performed against Leishmania tropica KWH23 promastigote and axenic amastigote using 3-(4, 5- dimethylthiazol-2-yl)-2, 5-diphenyletetrazolium bromide (MTT) assay. It was observed that the effect of PTN-CNPs and free PTN on both forms of the parasite was dose and time dependent. Free PTN presented low efficacy even at higher dose (40 µg/ml) with 25.6 ± 1.3 and 26.5 ±1.4 mean viability rate of the promastigotes and axenic amastigotes, respectively after 72 hrs incubation. While PTN-CNPs showed strong antileishmanial effects on both forms of parasite with 16 ± 0.4 and 19 ± 0.7 mean viability rate at the same higher concentration (40 µg/ml) after 72 hrs incubation. Half maximal inhibitory concentration (IC50) values of PTN-CNPs toward promastigotes and amastigotes were obtained as 0.1375 µg/ml and 0.1910 µg/ml, respectively. In conclusion, PTN-CNPs effectively inhibited both forms of the L. tropica; however, its effect was more salient on promastigotes. This data indicates that the PTN-CNPs act as a target drug delivery system. However, further research is needed to support its efficacy in animal and human CL.
RESUMO
OBJECTIVE@#To investigate in vitro larvicidal and antioxidant enzymes potential of the medicinal plants Ginkgo biloba (G. biloba), Stevia rebaudiana (S. rebaudiana) and Parthenium hysterophorous (P. hysterophorous) against Anopheles stephensi (An. stephensi) 4th instars larvae.@*METHODS@#For evaluation of larvicidal potential, the ethanolic, methanolic and dichloromethane leaves extracts of three different plants were used in dose-dependent experiments in two media, while the antioxidant enzymes activities were investigated using four different methods viz., superoxide dismutase, peroxidase, ascorbate and catalase.@*RESULTS@#An. stephensi has developed resistance to various synthetic insecticides, making its control increasingly difficult. The comparative performance of ethanolic extracts (65%-90%) was found better than the methanolic extract (70%-87%) and dichloromethane extract (60%-70%). Among the three plants extracts tested in two media, S. rebaudiana exhibited higher larvicidal activity with LC(50) (24 h) in methanolic extract than P. hysterophorous and G. biloba. G. biloba and P. hysterophorous exhibited the strongest antioxidative enzymes activity and S. rebaudiana were less active and no significant difference was observed.@*CONCLUSIONS@#These three plants exhibit larvicidal potential and can be further used for vector control alternative to synthetic insecticide due to eco-friendly and diseases control, furthermore these plant species have potent antioxidative enzyme activities, therefore, making them strong natural candidate particularly for diseases which are caused due to free radicals.