Investigation of the parameters affecting the release of flurbiprofen from chitosan microspheres

Abstract

Flurbiprofen (FLB), a NSAID, widely used for preventing pain generally for arthritis or dental problems. In this study, FLB loaded chitosan microspheres were prepared by ionotropic gelation method. In this method, microspheres were formed by dropping chitosan solutions containing FLB into sodium alginate solutions including sodium tripolyphosphate (TPP). A variety of formulation parameters like drug:polymer ratio, drug concentration, polymer's molecular weight, polymer concentration, pH and the concentration of TPP solutions, drying method and stirring time were analyzed. The dissolution studies were performed in a shaking water bath in pH 7.4 phosphate buffer saline (PBS) at 37 °C. Laser diffractometer was used for particle size analysis, and scanning electron microscope (SEM) was used for morphological properties. Drug loading and loading efficiency were calculated by using UV spectrophotometer. The particles obtained were spherical with 0.7-1.3 mm size range, and the loading efficiency was approximately 21-79%. The dissolution studies conducted revealed that drug:polimer ratio and the polymer type and concentration affected the drug release from microspheres. It was observed that increasing the polymer concentration, polymer's molecular weight and TPP concentration decreased the FLB release from microspheres, which was according to Higuchi kinetics.

Optimization of the colloidal properties of chitosan nanoparticles encapsulating alpha-arbutin

“…Accordingly, formulations (P1, P6, and P11) prepared to utilize the lowest concentration of TPP (0.02%, w/v) exhibited a micrometer size range compared to those prepared with higher concentrations. On the other hand, by increasing chitosan concentration from 0.10 to 0.30% at constant TPP concentration, an insignificant increase (P> 0.05) in P.S was observed similar to what was reported by Tilkan and Özdemir, [24], showing the insignificance of the increase in chitosan concentration on the obtained particle size during the encapsulation of flurbiprofen into chitosan microspheres.…”

Chitosan-based oral colon-specific delivery systems for polyphenols: recent advances and emerging trends

“…133 It has been reported that the polymer ratio, the DDA of chitosan, the molecular weight of the polymers, and the concentration of counterions significantly affect drug release from microspheres. 134,135 The emulsion cross-linking method is different from the above three methods. Using this method, chitosan solution at a slightly acidic pH is added to liquid paraffin containing a surfactant, generating a water/oil emulsion before adding a cross-linking agent, after which the microspheres can be obtained by filtration, washing with a suitable solvent, and drying.…”

“…133 It has been reported that the polymer ratio, the DDA of chitosan, the molecular weight of the polymers, and the concentration of counterions significantly affect drug release from microspheres. 134,135…”

Application of zein and chitosan in the development of a colon-specific delivery system

“…In a study performed with microspheres formed of chitosan, Eudragit ® , and diclofenac sodium and coated with Eudragit ® , a continuous release was obtained during a period of 8-12 hours for colon-specific delivery (Deshmukh and Naik, 2013). Tilkan and Özdemir (2017) investigated the parameters affecting the release of flurbiprofen from chitosan microspheres and obtained between 8 and 12 hours for delivery.…”