1.Efficacy of pentamidine-loaded chitosan nanoparticles as a novel drug delivery system for Leishmania tropica
Khan, R.U. ; Khan, M. ; Sohail, A. ; Ullah, R. ; Iqbal, A. ; Ahmad, B. ; Khan, I.U. ; Tariq, A. ; Ahmad, M. ; Said, A. ; Ullah, S. ; Ali, A. ; Rahman, M.U. ; Zaman, A. ; Bilal, H.
Tropical Biomedicine 2022;39(No.4):511-517
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.
Result Analysis
Print
Save
E-mail