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

Abstract

The aim of this study was to fabricate propranolol hydrochloride (Prop. HCl) (as a water-soluble drug):Eudragit RS100 (Eud) nanobeads and nanofibres applying the electrospraying method as an economical and one-step technique. Different ratios of Prop. HCl:Eud (i.e. 1:5 and 1:10) at total solution concentrations of 10-20% W/V were investigated. The FE-SEM studies revealed that morphology and size of the samples were highly affected by the solution concentration; so that, the nanobeads (a mean diameter of 82.9 nm) were formed in low concentration and at the highest concentration of the solution, nanofibres (a mean diameter of 232.3 nm) were resulted. Besides the morphological changes, the size of processed nanoformulations was increased with an increment of the solution concentrations. X-ray diffraction results as well as DSC thermograms clearly indicated that the drug crystallinity decreased in the electrosprayed samples. Furthermore, in vitro dissolution test showed that the electrosprayed samples had relatively slower release patterns toward the pure drug and physical mixtures, where the samples with the drug:polymer ratio of 1:10 indicated a faster release rate toward 1:5 ratio; nevertheless, the concentration of the injected formulations did not remarkably impressed the release behaviours. The current study established the suitability of electrospraying method in the fabrication of the water-soluble drugs nanobeads/nanofibres; however, in vivo effectiveness of the prepared nanoformulations should be meticulously considered.

Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

“…As literature review revealed the ESSs morphological features as well as their size distribution are crucial characteristics impress drug delivery mechanisms and its effectiveness, where these parameters depend on the ambient, solution, and operation variables. 24,25,40 The operation variables, including the feeding rate, applied voltage, and the distance between syringe/ nozzle tip and grounded screen along with ambient factors were fixed in regard to our preliminary analyzes. In the current study, the solution characteristics such as polymer and solution concentrations were selected as variable parameters.…”

“…19,20,23 Electrospraying or electrospinning is an emerging alternative method for SDs preparation. 24 The efficacy of the electrospraying technique for dissolution enhancement of different drugs with low water solubility including atorvastatin calcium, ezetimibe, 24 propranolol hydrochloride (HCl), 25 raloxifene HCl, 26 anticancer drugs, 27 and azithromycin 28 have been demonstrated by many authors.…”

“…In another word by imposing a high voltage electrical force, the polymer-drug solution droplets from a syringe will jet-out (atomize) and form micro/nano sized particles/fibers on a grounded screen placed under the tip of the syringe. 25,31 The applied voltage, flow rate of the polymer-drug solution, and deposition distance as the system variables, surface tension, electrical conductivity, viscosity, and density as the polymer physical features, polymer to drug ratios and jetting behavior of the system (polymer-drug solution) are the affecting and controlling parameters that lead to nanofibers or nanoparticles (nanobeads) formation. 32,33…”

“…19,34,35 Eudragit ® RS100 (Eudr) is a hydrophilic water-insoluble copolymer of poly (ethylacrylate, methyl-methacrylate and chlorotrimethyl-ammonioethyl methacrylate) containing quaternary ammonium groups (4.5- 6.8 %) with particular attributes such as non-toxicity, high permeability, good stability and aqueous media swelling ability. 25,36 Polyethylene glycol (PEG) as the mostly used polymer for SDs preparation has special advantages including good solubility in water and numerous organic solvents, quite low melting point, solubilizing ability of some combinations, 37 and wettability augmentation. 13 Considering aforementioned parameters it seems that preparing nano-solid dispersions (NSDs) of GLC with Eudr and PEG may be beneficial to solve solubility, stability, dissolution, and bioavailability issues.…”

Made-on-demand, complex and personalized 3D-printed drug products

“…Recent attempts in the drug delivery field included the development of targeted/smart DDSs, 1 , 2 and formulations of DDSs with sustained-/controlled-release behavior(s). 3 - 5 Different materials have been used in DDSs and the material inventory is continuously expanding especially in the targeted/ controlled delivery areas. In parallel with the advancement of new materials for DDSs, new procedures and techniques of material fabrication have been developed.…”