Taste masking and rheology improvement of drug complexed with beta-cyclodextrin and hydroxypropyl-β-cyclodextrin by hot-melt extrusion. (1st April 2018)

• Record Type: Journal Article
• Authors: Malaquias, Lorena F.B.; Sá-Barreto, Lívia C.L.; Freire, Daniel O.; Silva, Izabel C.R.; Karan, Kapish; Durig, Thomas; Lima, Eliana M.; Marreto, Ricardo N.; Gelfuso, Guilherme M.; Gratieri, Tais; Cunha-Filho, Marcilio
• Is Part Of: Carbohydrate polymers. Volume 185(2018)
• Page Start: 19
• Page End: 26
• Publication Date: 2018-04-01
• Subjects: Cyclodextrin -- Hot-melt extrusion -- Rheology -- Palatability -- E-tongue -- Antifungal assay; Polysaccharides -- Periodicals; Polysaccharides -- Periodicals; Polysaccharides -- Périodiques; Electronic journals; 547.78
• DOI: 10.1016/j.carbpol.2018.01.011
• Languages: English
• ISSNs: 0144-8617

Abstract

Highlights: Fluconazole-cyclodextrin inclusion complex were produced using hot melt extrusion. Inclusion complexes were obtained with high complexation efficiency. Improvements on drug rheology, palatability and dissolution rate were achieved. Abstract: This study aimed to mask fluconazole (FLU) taste and improve its rheological properties by an efficient process of cyclodextrin complexation. For this, hot-melt extrusion (HME) was used to obtain extrudates composed of FLU, hydroxypropylcellulose, and one of two different cyclodextrins (β-cyclodextrin or hydroxypropyl-β-cyclodextrin) maintaining the drug:cyclodextrin molar ratio at 1:0.3 or 1:0.2, respectively. Samples were characterized by physicochemical tests, palatability using e-tongue and antifungal assays. Drug stability was preserved after HME, according to spectroscopy test (correlation coefficient >0.9) and HPLC-assay (100–107%). Flowability was improved in HME systems with compressibility of <12%. Similarly, floodability exhibited significant enhancement (dispersibility <10%). Whereas extrudates of FLU containing only the polymeric matrix led to a slow drug dissolution efficiency (18.6%) and a partial drug taste masking; extrudates containing cyclodextrin accelerated FLU dissolution (dissolution efficiency approx. 30%) and provided a complete drug taste masking. Moreover, HME process could produce drug complexes with high complexation efficiency and preserve its antifungal activity.