Abstract
In the present study, new polymer microspheres of amphotericin B (AmB) were prepared by a spray drying technique using cyclodextrin polymers (Poly-CD) to improve the solubility and dissolution of AmB, to prevent in vivo toxic AmB aggregations. Formulations were characterized through scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), thermal analysis, Raman spectroscopy, particle size, drug purity test and in vitro release studies. The analysis indicated that the chemical structure of AmB remained unchanged in the amorphous solid dispersion, but the structure was changed from crystalline to amorphous. AmB was completely release from such optimized formulations in dissolution media in 40 min. This work may contribute to a new generation of spherical amorphous solid dispersion using a cyclodextrin polymer, which has implications for the possibility of drug development for oral utilization or as powder aerosols for pulmonary administration.
Highlights
Amphotericin B [amphotericin B (AmB)] is considered as an old drug with antifungal properties
AmB is used for the treatment of deep or systemic fungal development induced by an immunosuppressive state of patient which is one of the major causes of mortality [2]
The results showed a good pulmonary deposition and a lower rate of active substance in the kidney leading to a reduction of drug nephrotoxicity and an improvement of fungal activity, approximately 1.5-times better than the marketed intravenous preparations
Summary
Amphotericin B [AmB] is considered as an old drug with antifungal properties. This active pharmaceutical ingredient was extracted from Streptomyces nodosus and its chemical synthesis was discovered in 1970 [1]. AmB belongs to class IV in the Biopharmaceutical Classification System, presenting low solubility (about 1 μg/mL in water) and low membrane permeability [3]. This low solubility is due to the self-association of AmB molecules above a critical micellar concentration at about 0.2 mg/mL [4]. The long polyene chain measuring 21 Å is responsible for the high absorption between 300 and 450 nm allowing its dosage using an ultra-violet [UV] spectrophotometer
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