Methylprednisolone acetate–Eudragit^® RS100 electrospuns: Preparation and physicochemical characterization

Abstract

The aim of the present study was to formulate methylprednisolone acetate -Eudragit(®) RS100 nanofibers and nanobeads by the electrospinning method. The physicochemical characteristics of the prepared electrospuns were assessed as well. The particle size and morphology were evaluated using scanning electron microscopy. The crystallinity of the drug in the nanofibers and nanobeads obtained was also studied by X-ray crystallography and differential scanning calorimetry (DSC) thermograms. In addition, FT-IR spectroscopy was applied to investigate any possible chemical interaction between the drug and carrier during the preparation process. The drug release kinetics were considered, to predict the release mechanism. Increasing the concentration of the injected solution resulted in the production of more nanofibers and less nanobeads, with the particle size ranging from 100 to 500 nm. The drug crystallinity was decreased during the electrospinning process; however, no interaction between drug and polymer was observed. The electrospuns showed faster drug release pattern compared to the pure drug. The release data were best fitted to the Weibull model, in which the corresponding shape factor values of the model were less than 0.75 indicating the diffusion mechanism of drug release. In conclusion, electrospinning could be considered as a simple and cost effective method for fabricating the drug: polymer nanofibers and nanobeads.

Morphological and physicochemical evaluation of the propranolol HCl–Eudragit® RS100 electrosprayed nanoformulations

“…HCl during the electrospraying procedure. These findings were in good agreement with DSC thermograms and similar previously reported results for the TA-PLGA, AZI-PLGA and MPA-Eud electrosprayed nanobeads [22][23][24].…”

“…It can be concluded that the beads formation occurs in the low concentration of solutions (1:5 and 1:10 drug:polymer ratios). The solution at the low polymer concentrations has high surface tension which leads to the dispersion of liquid jet into the divided droplets; on the contrary, the fibre formation could be dominated at the high polymer concentrations because of the increasing in the viscoelastic forces [12,[22][23][24][37][38][39]. So, therefore, the formation of fibres or beads was highly affected by polymer solution concentrations; where the size of the prepared beads is increased by increasing the solution concentration and the fibres were produced at the highest solution concentration.…”

“…Consequently, the absence of any probable chemical interaction between Prop. HCl and Eud could not be absolutely realized from the FT-IR spectroscopy results [22][23][24]44].…”

“…The technique has various applications in microelectronics [17], optical electronics, biotechnology, environmental engineering [18], modern material and medical technologies, new DDSs and ingredients dosage fabrication in the food, cosmetic and medicine production industries [19]. Some drugs such as insulin [20], paclitaxel [21], azithromycin [22], triamcinolone acetonide [23], methylprednisolone acetate [24], ibuprofen [25], naproxen [26], etc. [27][28][29][30][31][32][33][34] have been prepared by this method.…”

“…Besides, it can adhere to the negatively charged cells, so this polymer sounds to be an opportune carrier for localized and extended delivery of the proper drugs to the various physiologic fluids [22][23][24]. There are some reports that show the application of Eud as a suitable carrier at delivery of triamcinolone acetonide [23], methylprednisolone acetate [24], azithromycine [22] and some anti-inflammatory drugs to the eye [12]. To the best of our knowledge, there is no report regarding the preparation of the water-soluble drug-Eud electrosprayed nanoformulations.…”