Amphotericin B-albumin conjugates: Synthesis, toxicity and anti-fungal activity

Development of dextrin-amphotericin B formulations for the treatment of Leishmaniasis

“…More specifically, both spectra feature the peaks corresponding to C_O and C_C stretching vibration, that suffer a slight shift from 1689.5 and 1558.3 cm −1 to 1716.5 and 1569.9 cm −1 , respectively, probably due to the interaction with the polysaccharide. Similar results, where characteristic peaks of AmB were still visible in the FTIR analysis, were reported in the literature after drug conjugation to bovine serum albumin (BSA) [38] or encapsulation in glutaraldehyde cross-linked BSA microparticles [42], formation of AmB nano-assemblies with Aloe vera leaf extract [43] and conjugation of AmB to oxidized sodium alginate [19] or oxidized polymannose [22]. Thermal studies are useful to ascertain the compatibility, stability and physical state of drugs conjugated to polymers or encapsulated in nanoparticles [36].…”

“…5 B and D shows that none of the Dex-AmB nanocomplexes promoted a reduction in HEK293T cell viability to levels under the 70% threshold even at the highest dose tested. The reduction of AmB toxicity after inclusion or conjugation to polysaccharides or encapsulation into polymeric nanoparticles was also reported in the literature [19,23,38,39,53]. As expected, Dex was safe at all the tested concentrations ( Fig.…”

“…polyene and C_O stretching vibration from the carbonyl ester group, respectively [38,39]. In addition, the peaks corresponding to C\ \H stretching (3012.5 cm −1 ), CH 2 and CH 3 symmetric stretching vibrations (2877.5 cm −1 ), C-C-H (chromophore) bending as well as CH bending (trans-polyene) (1010.6 cm −1 ), C_O asymmetric stretching vibrations (1068.4 cm −1 ) and C\ \H bending and CH 3 rocking vibrations due to the C_O asymmetric stretching vibrations (891.04 cm −1 ) are recognized [40,41].…”

“…The UV-vis spectrum of AmB is very sensitive to aggregation and characterized by four well-separated bands when in a monomeric state [53,54]. Moreover, the spectral modifications induced by the extent of AmB aggregation can be represented by the ratio of the first to the fourth peaks, being a value of b1 characteristic of the monomeric form [38] and a value of N2 to a supper-aggregated form [43]. Our results, showing four well-defined peaks at approximately 349 (I), 369 (II), 387 (III) and 408 nm (IV), indicates that free-AMB exists in monomeric form when firstly dissolved in 0.1 M borate buffer pH 11 and then diluted in dH 2 O (Fig.…”

“…Overall yield (%) [64] were described in the literature. Gurudevan et al [38] showed that AmB at 15.6 μg/mL was highly cytotoxic against HEK293T cell line, promoting N80% of cell death. In other studies, it was described that 7.8 μg/mL [22] or 10 μg/mL [19,23] of AmB promoted 50% or 90% of HEK293T cells death, respectively.…”