Preparation and characterization of ethylcellulose microspheres for sustained-release of pregabalin

Abstract

Background and purpose: Pregabalin is used in the treatment of epilepsy, chronic pain, and other psychological disorders. Preparation of pregabalin in the sustained-release formulation will enhance patient compliance and reduce the incidence of side effects. The aim of this study was to prepare sustained-release microspheres for pregabalin utilizing ethylcellulose and evaluate the processing factors that influence the fabrication and the performance of the prepared microspheres. Experimental approach: The microspheres were prepared using the water-oil-oil double emulsion solvent evaporation method. Microspheres were characterized for particle size, encapsulation efficiency, and in vitro drug release. The influence of the processing variables on the characteristics of the prepared microspheres was studied. Microspheres solid-state characterization performed using differential scanning calorimetry, Fourier transform infrared spectroscopy and scanning electron microscopy. Findings/Results: The results described in the context of the current work illustrated the suitability of the water-oil-oil system in the preparation of sustained-release microspheres for pregabalin. The optimum formulation was prepared at a drug to polymer ratio of 1:3 w/w, stirring speed of 600 rpm, surfactant concentration of 1.5%, and external phase volume of 150 mL. This formula produced microspheres particle size in the range 600-1000 μm, with 87.6% yield, and 80.14 ± 0.53% encapsulation efficiency. Drug release from the microspheres was found to be diffusion controlled, with a pH-independent behavior. Conclusion and implication The current work presented a successful attempt to fabricate a sustained-release microsphere comprising pregabalin. This will help overcome the frequent dosing problems with conventional pregabalin dosage forms and improve product performance.

Design and Fabrication of Anticancer Drug‐Loaded Poly(ϵ‐caprolactone)‐Poly(ethylene glycol)‐Poly(ϵ‐caprolactone) Micelles as Controlled Release System

“…Correlating these results indicated that the bigger the microparticles, the larger EE. The reason is that higher agitating speed which provided stronger shear force leading to the formation of smaller droplets and consequently smaller microspheres [19] . For this reason as shown in Table 1, optimized production factors can be obtained at a shaking speed of 600 rpm.…”

“…The reason is that higher agitating speed which provided stronger shear force leading to the formation of smaller droplets and consequently smaller microspheres. [19] For this reason as shown in Table 1, optimized production factors can be obtained at a shaking speed of 600 rpm. The data obtained as a result of the equation showed that X 4 (drug:polymer ratio) was more important than X 1 (shaking speed).…”

Development and evaluation of polycaprolactone-based electrospun nanofibers containing timolol maleate as a sustained-release device for treatment of glaucoma: in vivo evaluation in equine eye

“…To ensure that no major interaction took place between the polymers and pharmacologically active parts of the drug, the Fourier-transform infrared spectroscopy (FTIR) evaluation was utilized. The drug, polymers, and all prepared nanofibers were observed after being pressed with potassium bromide to obtain disks for examination ( 19 ). The spectrophotometer (Prestige-21, Shimadzu, Japan) was used to record the FTIR spectra of the samples between the 4000-400 cm -1 range, and the recorded data were analyzed for any significant shift, change, and elimination of characteristic peaks of the drug in the nanofibers.…”

Evaluation of PLGA nanoparticles containing outer membrane proteins of Acinetobacter baumannii bacterium in stimulating the immune system in mice

“…The direct method was used to determine the encapsulation efficiency percentage (EE%) ( 23 24 ). To describe briefly, 10 mg of PLGA nanoparticles containing OMPs was dissolved in 1 mL of dichloromethane and shaken at 37 °C for 30 min to evaporate the solvent.…”