Preparation and characterisation of amphotericin B-copolymer complex for the treatment of leishmaniasis

Self-assembled nanostructures of L-ascorbic acid alkyl esters support monomeric amphotericin B

“…The hypsochromic shift of the band I, which is more pronounced for ASC16 and ASC14 formulations at pH 4 (Table S1), is connected with the forming of H-type aggregated molecular structures (where molecules stack predominantly face-to-face), where the transition dipole moments of molecules are orientated parallel and the out of the plane of aggregate [ 50 ]. Notably, the ASC16/AmB formulation at pH8 shows a I/IV ratio of 0.6, which is comparable with that reported for AmB solubilised in GM1 micelles [ 25 ] and copolymers [ 26 , 30 ]. In our study, the I/V ratio for ASC16/AmB suspension at pH 8 is not statistically different than that obtained for AmB solubilised in methanol.…”

“…This formulation constitutes an aqueous-based (organic solvent-free) nanostructure, which appears as appealing for further tests for the treatment of cutaneous infections. The UV-visible and CD absorption spectroscopy studies indicated a predominance of the monomeric form of AmB, which has also been reported for other micellar-based formulations [ 25 , 26 , 30 ]. In this work, we relate ASC16 coagels capacity for maintaining the in-plane solubility of AmB, which may be responsible for its enhanced chemical stability.…”

“…Several studies also report that micellar [ 25 – 27 ] and nanostructured [ 1 , 28 , 29 ] AmB suspensions have been successful in maintaining the monomeric form of AmB and are promising as therapeutic formulations with putative low side effects. The results obtained using micellar formulations of polymers [ 26 , 30 ] and the natural glycolipid GM1 [ 25 ] are particularly interesting.…”

“…Heat treatment has been employed to reach super-aggregated forms of AmB with particular spectroscopic characteristics and with improved tolerance in clinical use [24]. Several studies also report that micellar [25][26][27] and nanostructured [1,28,29] AmB suspensions have been successful in maintaining the monomeric form of AmB and are promising as therapeutic formulations with putative low side effects. The results obtained using micellar formulations of polymers [26,30] and the natural glycolipid GM1 [25] are particularly interesting.…”

Activated Ester Containing Polymers: Opportunities and Challenges for the Design of Functional Macromolecules

“…As glycopolymers that are suited for specific binding or recognition events are mostly copolymers, the attachment of larger units, such as specific disaccharides , or trisaccharides for the synthesis of copolymers has been described. The group of Brocchini even reported the attachment of larger complexes, such as Amphotericin B …”