Table 1.
In vitro performance of BNZ-based nanomedicines.a
| Type of nanomedicine/ composition | Physicochemical properties | In vitro assays | Outcome | Ref. |
|
| ||||
| vesicles, SLN, NLC and cyclodextrins (CDs) | vesicles: ≈200 nm CDs: 5–10 μm SLN: ≈170 nm, −21 mV ζ-potential NLC: ≈200 nm, −26 mV ζ-potential |
cytotoxicity on L-929 cells and HepG2 cells activity on epimastiotes, trypomastigotes, and amastigotes of CL strain, clone B5 |
SLN less active than BNZ, NLC less active and more toxic than CD vesicles low EE CDs best-balanced anti-trypanosoma activity /toxicity, (less cytotoxicity of BNZ-CDs than BNZ without reduction of trypanocidal activity) |
[33] |
| CaCO3 Nps | 42 ± 8 nm | cytotoxicity on LLC-MK2 cells activity on epimastigotes, trypomastigotes, and amastigote of Y strain |
less toxicity and higher selectivity, with anti-trypanosoma activity at 25 times lower concentrations of BNZ | [34] |
| mesoporous silica Nps (MCM-41) chitosan succinate covalently attached | −11.5 ± 0.5 mV ζ-potential | activity on epimastigotes of CL Brener strain | the same anti-trypanosomal effect as that of BNZ-MCM-41 at 30 times lower BNZ concentration | [35] |
| Nps based on Eudragit® RS PO and Eudragit® RL PO | 200–300 nm; 24–36 mV ζ-potential; EE: 78% DL: 18% w/w |
in vitro release in 0.1 N HCl (pH 1.2) | increased dissolution rate of drug from Nps | [41] |
| zeolitic imidazolate framework ZIF-8 (BNZ@ZIF-8) | in vitro release at pH 4.5 and 7.6 | at pH 4.5, BNZ@ZIF-8 showed a faster release with a burst effect, while, at pH 7.6, it showed prolonged and controlled release | [42] | |
| nanocrystals |
in vitro release in FaSSGF, FeSSIF, and FaSSIF integrity of tight junction dynamics and permeability on Caco-2 |
safety and increased permeation through the Caco-2 cells with minimal interactions with mucin glycoproteins | [43] | |
| lipid nanocapsules Lipoid S 100, Kolliphor® HS 15 and Labrafac® WL 1349 oil phase at three oil/surfactant ratios | 30, 50, and 100 nm; PDI < 0.07; −1.59 to −0.96 mV ζ-potential |
release in FaSSGF, FeSSIF, and FaSSIF with pancreatic enzymes permeability on Caco-2 |
NCPs protected BNZ in simulated gastric fluid and provided sustained release in a simulated intestinal fluid improved BNZ permeability |
[44] |
| NLC myristyl myristate/crodamol oil/poloxamer 188 |
150 nm; −13 mV ζ-potential; EE: 80% |
release at pH 6.8 haemolysis cytotoxicity on CHO and Vero cells activity on trypomastigotes and amastigotes of strain K98 |
biphasic drug release profile with an initial burst release followed by a prolonged phase trypanocidal activity similar to that of free BNZ, with lower cytotoxicity to mammalian cells |
[36] |
| NLC compritol, crodamol, Tween 80 and poloxamer 407 (P407) |
110 nm; PDI: 0.19 −18 mV ζ-potential; EE: 83%; DL: 1.64 |
haemolysis cytotoxicity on L929 cells activity on epimastigotes of Colombian strain |
NLC-BNZ had higher trypanocidal activity than free BNZ with low cytotoxicity to mammalian cells | [38] |
| Polymeric Nps cashew phthalate gum |
activity on epimastigotes and trypomastigotes cytotoxicity on macrophages |
Nps enhanced trypanocidal activity, and reduced cytotoxicity | [37] | |
aAbbreviations: DL – drug loading; EE – encapsulation efficiency; FaSSGF – fasted-state simulated gastric fluid; FaSSIF – fasted-state simulated intestinal fluid; FeSSIF – fed-state simulated intestinal fluid; NLC – nanostructured lipid carriers; PDI – polydispersity index; SLN – solid lipid nanoparticles.