Comparative efficacy of extract delivery PEG--PCL, niosome, and their combination against genotype T4: characterization, inhibition, anti-adhesion, and cytotoxic activity.

Background: spp. is a waterborne, opportunistic protozoan that can cause amebic keratitis and granulomatous amebic encephalitis. is a native tree in Malaysia, and its extracts possess a broad range of biological activities. Niosomes are non-ionic surfactant-based vesicle formations and suggest a future targeted drug delivery system. Copolymer micelle (poly(ethylene glycol)-block-poly(-caprolactone); PEG--PCL) is also a key constituent of niosome and supports high stability and drug efficacy. To establish extract (KRe) loading in diverse nanocarriers niosome, PEG--PCL micelle, and their combination and to study the effect of all types of nanoparticles (NPs) on viability, adherent ability, elimination of adherence, and cytotoxicity.

Methods: In this study, we characterized niosomes, PEG--PCL, and their combination loaded with KRe and tested the effect of these NPs on stages. KRe-loaded PEG--PCL, KRe-loaded niosome, and KRe-loaded PEG--PCL plus niosome were synthesized and characterized regarding particle size and charge, yield, encapsulation efficiency (EE), and drug loading content (DLC). The effect of these KRe-loaded NPs on trophozoite and cystic forms of was assessed through assays of minimal inhibitory concentration (MIC), using trypan blue exclusion to determine the viability. The effect of KRe-loaded NPs was also determined on trophozoite for 24-72 h. Additionally, the anti-adhesion activity of the KRe-loaded niosome on trophozoites was also performed on a 96-well plate. Cytotoxicity activity of KRe-loaded NPs was assessed on VERO and HaCaT cells using MTT assay.

Results: KRe-loaded niosome demonstrated a higher yielded (87.93 ± 6.03%) at 286 nm UV-Vis detection and exhibited a larger size (199.3 ± 29.98 nm) and DLC (19.63 ± 1.84%) compared to KRe-loaded PEG--PCL (45.2 ± 10.07 nm and 2.15 ± 0.25%). The EE (%) of KRe-loaded niosome was 63.67 ± 4.04, which was significantly lower than that of the combination of PEG--PCL and niosome (79.67 ± 2.08). However, the particle charge of these NPs was similar (-28.2 ± 3.68 mV and -28.5 ± 4.88, respectively). Additionally, KRe-loaded niosome and KRe-loaded PEG--PCL plus niosome exhibited a lower MIC at 24 h (0.25 mg/mL), inhibiting 90-100% of trophozoites which lasted 72 h. KRe-loaded niosome affected adherence by around 40-60% at 0.125-0.25 mg/mL and removed adhesion on the surface by about 90% at 0.5 mg/mL. Cell viability of VERO and HaCaT cells treated with 0.125 mg/mL of KRe-loaded niosome and KRe-loaded PEG--PCL plus niosome exceeded 80%.

Conclusion: Indeed, niosome and niosome plus PEG--PCL were suitable nanocarrier-loaded KRe, and they had a greater nanoparticle property to test with high activities against on the reduction of adherence ability and demonstration of its low toxicity to VERO and HaCaT cells.