Release profile and characteristics of electrosprayed particles for oral delivery of a practically insoluble drug

Abstract

acid) (PLGA) microspheres containing celecoxib were prepared via electrospraying, and the influence of three processing parameters namely flow rate, solute concentration and drug loading, on the physico-chemical properties of the particles and the drug-release profile was studied. Microspheres with diameters between 2 and 8 mm were produced and a near-monodisperse size distribution was achieved ( polydispersivity indices of 6-12%). Further, the inner structure of the particles showed that the internal porosity of the particles increased with increasing solvent concentration. X-ray powder diffraction (XRPD) analysis indicated that the drug was amorphous and remained stable after eight months of storage. Drug release was studied in USP 2 (United States Pharmacopeia Dissolution Apparatus 2) dissolution chambers, and differences in release profiles were observed depending on the parametric values. Changes in release rate were found to be directly related to the influence of the studied parameters on particle size and porosity. The results indicate that electrospraying is an attractive technique for producing drug-loaded microspheres that can be tailored towards an intended drug-delivery application. Compared with the more conventional spray-drying process, it provides better control of particle characteristics and less aggregation during particle formation. In particular, this study demonstrated its suitability for preparing capsules in which the drug is molecularly dispersed and released in a sustained manner to facilitate improved bioavailability.

Size and morphology controlling of PLGA microparticles produced by electro hydrodynamic atomization

“…The effect of flow rate on particle size by several polymers has been reported in a number of other studies. [35][36][37] Testing was done on six formulations (A to F) sprayed at three flow rates (2, 3 and 5 ml/hr) to determine the effect of flow rate on size of the microparticles.…”

Electrohydrodynamic atomization: A two-decade effort to produce and process micro-/nanoparticulate materials

“…In a different study, Valo et al (2009) encapsulated beclomethasone-dipropionate a hydrophobic drug in PLA nanoparticles via electrospray in the stable cone-jet mode. Bohr et al (2012) also fabricated celecoxib-loaded PLGA microparticles with diameters ranging from 2 to 8 μm for improving oral delivery where celecoxib is a hydrophobic, non-steroidal anti-inflammatory drug with a low aqueous solubility (≈ 5 μg/ml) and solubility-limited bioavailability. Ketoprofen (KET) a hydrophobic drug extensively used for treatment of inflammation, pain, or rheumatism was encapsulated in ethyl cellulose microparticles by electrospray (Huang et al, 2012).…”

Poly(ethylene carbonate)-containing polylactic acid microparticles with rifampicin improve drug delivery to macrophages

“…The ratio among PLA, PEC and RF at 4% solid concentration as well as the liquid flow rate, voltage and solvent used was adjusted to obtain a stable cone jet and particles in the preferred size range for pulmonary delivery. Please refer to the following articles for an overview of the parameters influencing electrospraying jet formation and particle properties . After the screening process, solutions of 3% (w/v) polymer, either PLA or PEC : PLA mixtures at 5:95 and 10:90 (w/w) ratios and 1% (w/w) RF in DCM were found to form microparticles of a size suitable for inhalation after electrospraying.…”