Posaconazole/hydroxypropyl-β-cyclodextrin host–guest system: Improving dissolution while maintaining antifungal activity. (20th May 2016)

• Record Type: Journal Article
• Authors: Tang, Peixiao; Ma, Xiaoli; Wu, Di; Li, Shanshan; Xu, Kailin; Tang, Bin; Li, Hui
• Is Part Of: Carbohydrate polymers. Volume 142(2016)
• Page Start: 16
• Page End: 23
• Publication Date: 2016-05-20
• Subjects: Posaconazole (PubChem CID: 468595) -- Methanol (PubChem CID: 887) -- Acetone (PubChem CID: 180) -- Hydroxypropyl-beta-cyclodextrin (PubChem CID: 14049689) -- Heavy water (PubChem CID: 24602); Posaconazole -- Hydroxypropyl-β-cyclodextrin -- Inclusion complex -- Characterization -- Dissolution -- In vitro anti-fungal; Polysaccharides -- Periodicals; Polysaccharides -- Periodicals; Polysaccharides -- Périodiques; Electronic journals; 547.78
• DOI: 10.1016/j.carbpol.2016.01.042
• Languages: English
• ISSNs: 0144-8617

Abstract

Highlights: Experimental methods and theoretical study are used to explore the HP-β-CD–POS complex. The water solubility of POS was increased by 82 times. Almost 90% of the loaded POS released after 10 min in the three dissolution media. The HP-β-CD–POS complex maintains high antifungal activities. Abstract: This study aimed to prepare and characterize the inclusion complex between posaconazole (POS) and hydroxypropyl-β-cyclodextrin (HP-β-CD). Phase solubility study was conducted to investigate the drug/CD interaction in solution, including the stoichiometry and apparent stability constant. The solid complex (HP-β-CD–POS) obtained was characterized through Fourier transform infrared spectroscopy, powder X-ray diffraction, 1 H and ROESY 2D nuclear magnetic resonance, differential scanning calorimetry, and scanning electron microscopy. These approaches confirmed the formation of the inclusion complex. The HP-β-CD–POS inclusion complex exhibited better water solubility and higher dissolution rate than the free POS did; the water solubility of POS was increased by 82 times and almost 90% of the loaded drug dissolved after 10 min in the dissolution media. In addition, preliminary in vitro antifungal susceptibility testing revealed that HP-β-CD–POS maintains a high level of antifungal activities. Therefore, the HP-β-CD complex may be useful in the delivery of posaconazole.