Self-assembled Amphotericin B Pharmacosome-like Vesicles Derived from Lipid-based Microtubes: A Model Carrier to Further Explore

SALERNO C.; CUESTAS M.; MANCO K.; CHIAPPETTA D.; LUCANGIOLI S.

Micro and nanosystems

Bentham Science Publishers

Año: 2021

1876-4029

Abstract: Background: Self-assembled drug delivery systems are of much interest since they can be produced by simple low cost and solvent-free procedures. Pharmacosomes are supramolecular- structured nanocarriers with benefits for drug stability and targeting delivery. Amphotericin B (AmB) still remains an important agent for the treatment of invasive mold infections, e.g invasive aspergillo- sis, although the challenge for new formulations is still prevailing due to high rates of toxicity. Objective: We have previously reported the incorporation of AmB into 12-hydroxystearic acid lipid- based microtubes (MTs) for topical use, herein we report the ability of AmB-MTs to self-assemble in- to vesicles upon dilution. Methods: AmB-MTs with different drug concentrations (1, 3, 5 mg/ml) were prepared, and size de- termination was carried out for different dilutions. Morphology was evaluated by microscopy. In vitro cytotoxicity was evaluated in Vero cells and in vitro activity against Aspergillus fumigatus and Asper- gillus flavus was assessed. Results: AmB-MTs closed upon dilution to form vesicles ranging from 200 nm to 1µm. AmB MIC (Minimum inhibitory concentration) for both Aspergillus species was 0.0625 and 0.125 µg/ml for dis- persion and reconstituted lyophilized, respectively. Conclusion: AmB pharmacosome-like vesicles are smaller structures than MTs may thus be favoura- ble for other delivery routes. We assume that this kind of pharmacosomes-like carrier is a promising model for the obtention of new vesicular carriers based on lipid MTs.