Development and characterization of gelatin and ethylcellulose microparticles designed as platforms to delivery fluoride

• Published in: Drug development and industrial pharmacy 2013-11, Vol.39 (11), p.1644-1650
• Main Authors: de Francisco, Lizziane M. B, Cerquetani, Juliana A., Bruschi, Marcos L.
• Format: Article
• Language: English
• Subjects: Administration, Oral; Cariostatic Agents - administration & dosage; Cariostatic Agents - chemistry; Cellulose - analogs & derivatives; Cellulose - chemistry; Cellulose - ultrastructure; Delayed-Action Preparations - administration & dosage; Delayed-Action Preparations - chemistry; Diffusion; Drug Carriers - administration & dosage; Drug Carriers - chemistry; Drug Compounding; Emulsions; ethylcellulose; Fluoride; Fluorides - administration & dosage; Fluorides - chemistry; Fluorides, Topical - administration & dosage; Fluorides, Topical - chemistry; gelatin; Gelatin - chemistry; Gelatin - ultrastructure; Humans; in-vitro release; Kinetics; Mannitol - chemistry; microparticles; Microspheres; Particle Size; Phosphates - administration & dosage; Phosphates - chemistry; Sodium Fluoride - administration & dosage; Sodium Fluoride - chemistry; Solubility; Surface Properties; Sweetening Agents - chemistry
• ISSN: 0363-9045; 1520-5762
• DOI: 10.3109/03639045.2012.728610

Purpose: To develop and characterize microparticles containing fluoride sources (FS) from sodium fluoride, sodium monofluorophosphate (MFP) or aminofluoride and evaluate their characteristics as fluoride delivery systems. Methods: Ethylcellulose microparticles containing fluoride (EM) were prepared by emulsification of ethyl acetate dispersion containing polymer and FS (ethylcellulose:FS ratio of 1:0.25 wt/wt) with aqueous external phase containing polysorbate 80 (0.8% vol/vol) using the volume ratio (organic:aqueous) of 1:5. The organic solvent was evaporated; microparticles were collected by centrifuging, washed with deionized water and freeze-dried. Gelatin microparticles containing FS (GM) was obtained by dispersion of the natural polymer in water, adding FS (6:1 wt/wt) and 20% (wt/wt) of mannitol. The final dispersions were spray-dried. Particle morphology and size were investigated using optical microscopy. The content of fluoride ions in the microparticles was quantified using a potentiometric method. The encapsulation efficiency and in vitro release profile of fluoride was also determined. Results: Microparticles exhibited polydispersity and mean diameters