Preparation and Characterization of Spherical Amorphous Solid Dispersion with Amphotericin B

• Published in: Pharmaceutics Vol. 10; no. 4; p. 235
• Main Authors: Mehenni, Lyes, Lahiani-Skiba, Malika, Ladam, Guy, Hallouard, François, Skiba, Mohamed
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 16.11.2018; MDPI
• Subjects: Aluminum; amorphous solid dispersions; amphotericin B; Chemical Sciences; cyclodextrins polymers; Drug dosages; Efficiency; Galenic pharmacology; Life Sciences; Medicinal Chemistry; Nanoparticles; Pharmaceutical sciences; Pharmaceuticals; Polymers; spray-drying; France; United States > US; Switzerland; Germany; amphotericin B; cyclodextrins polymers; amorphous solid dispersions; spray-drying
• ISSN: 1999-4923; 1999-4923
• DOI: 10.3390/pharmaceutics10040235

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.