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Sustained release is highly desired for "efficacious, safe and convenient" drug delivery, particularly for those anticancer drug molecules with toxicity. In this study, a modified coaxial electrospraying process was developed to coat a hydrophobic lipid, i.e., stearic acid (SA), on composites composed of the anticancer drug tamoxifen citrate (TC) and insoluble polymeric matrix ethylcellulose (EC). Compared with the electrosprayed TC-EC composite microparticles M1, the electrosprayed SA-coated hybrid microparticles M2 were able to provide an improved TC sustained-release profile. The 30% and 90% loaded drug sustained-release time periods were extended to 3.21 h and 19.43 h for M2, respectively, which were significantly longer than those provided by M1 (0.88 h and 9.98 h, respectively). The morphology, inner structure, physical state, and compatibility of the components of the particles M1 and M2 were disclosed through SEM, TEM, XRD, and FTIR. Based on the analyses, the drug sustained-release mechanism of multiple factors co-acting for microparticles M2 is suggested, which include the reasonable selections and organizations of lipid and polymeric excipient, the blank SA shell drug loading, the regularly round shape, and also the high density. The reported protocols pioneered a brand-new manner for developing sustained drug delivery hybrids through a combination of insoluble cellulose gels and lipid using modified coaxial electrospraying. [ABSTRACT FROM AUTHOR]

One of the most important trends in developments in electrospinning is to combine itself with traditional materials production and transformation methods to take advantage of the unique properties of nanofibers. In this research, the single-fluid blending electrospinning process was combined with the casting film method to fabricate a medicated double-layer hybrid to provide a dual-phase drug controlled release profile, with ibuprofen (IBU) as a common model of a poorly water-soluble drug and ethyl cellulose (EC) and polyvinylpyrrolidone (PVP) K60 as the polymeric excipients. Electrospun medicated IBU-PVP nanofibers (F7), casting IBU-EC films (F8) and the double-layer hybrid films (DHFs, F9) with one layer of electrospun nanofibers containing IBU and PVP and the other layer of casting films containing IBU, EC and PVP, were prepared successfully. The SEM assessments demonstrated that F7 were in linear morphologies without beads or spindles, F8 were solid films, and F9 were composed of one porous fibrous layer and one solid layer. XRD and FTIR results verified that both EC and PVP were compatible with IBU. In vitro dissolution tests indicated that F7 were able to provide a pulsatile IBU release, F8 offered a typical drug sustained release, whereas F9 were able to exhibit a dual-phase controlled release with 40.3 ± 5.1% in the first phase for a pulsatile manner and the residues were released in an extended manner in the second phase. The DHFs from a combination of electrospinning and the casting method pave a new way for developing novel functional materials. [ABSTRACT FROM AUTHOR]

Different from traditional solid dispersion (SD) for improving the dissolution rates of poorly water-soluble drugs, the upgraded 4th SD was developed to furnish a drug sustained-release profile. In this work, two different kinds of 4th SDs were fabricated using two electrospinning processes. One is a ternary SD (nanofibers F2) that consisted of ethyl cellulose (EC), polyethylene glycol 1000 (PEG), and tamoxifen citrate (TAM) from a modified coaxial process, and the other is a binary SD (nanofibers F1) which is comprised of EC and TAM from a single-fluid blending process. Scanning electronic microscopic observations demonstrated that F2 (330±50 nm) showed a better quality than F1 (870±230 nm) in terms of size and size distribution although both of them had a smooth surface morphology and a cross section. X-ray diffraction patterns verified that both SDs were amorphous nanocomposites owing to the favorable secondary interactions among these components, as suggested from the results of FTIR. In vitro dissolution experiments indicated that F2 could furnish an improved drug sustained-release characteristics compared to F1, exhausting all the contained TAM and having weaker leveling-off late release. The molecular behaviors of drug sustained-release from the binary 4th SD were suggested. The protocols reported here paved an alternative way for developing novel functional nanomaterials for effective delivery of poorly water-soluble drugs. [ABSTRACT FROM AUTHOR]

A family of medicated Janus fibers that provides highly tunable biphasic drug release was fabricated using a side-by-side electrospinning process employing a Teflon-coated parallel spinneret. The coated spinneret facilitated the formation of a Janus Taylor cone and in turn high quality integrated Janus structures, which could not be reliably obtained without the Teflon coating. The fibers prepared had one side consisting of polyvinylpyrrolidone (PVP) K60 and ketoprofen, and the other of ethyl cellulose (EC) and ketoprofen. To modulate and tune drug release, PVP K10 was doped into the EC side in some cases. The fibers were linear and had flat morphologies with an indent in the center. They provide biphasic drug release, with the PVP K60 side dissolving very rapidly to deliver a loading dose of the active ingredient, and the EC side resulting in sustained release of the remaining ketoprofen. The addition of PVP K10 to the EC side was able to accelerate the second stage of release; variation in the dopant amount permitted the release rate and extent this phase to be precisely tuned. These results offer the potential to rationally design systems with highly controllable drug release profiles, which can complement natural biological rhythms and deliver maximum therapeutic effects. [ABSTRACT FROM AUTHOR]

This manuscript reports a new type of drug-loaded core-shell nanofibers that provide tunable biphasic release of quercetin. The nanofibers were fabricated using a modified coaxial electrospinning process, in which a polyvinyl chloride (PVC)-coated concentric spinneret was employed. Poly (vinyl pyrrolidone) (PVP) and ethyl cellulose (EC) were used as the polymer matrices to form the shell and core parts of the nanofibers, respectively. Scanning and transmission electron microscopy demonstrated that the nanofibers had linear morphologies and core-shell structures. The quercetin was found to be present in the nanofibers in the amorphous physical status, on the basis of X-ray diffraction results. In vitro release profiles showed that the PVP shell very rapidly freed its drug cargo into the solution, while the EC core provided the succedent sustained release. Variation of the drug loading permitted the release profiles to be tuned. [ABSTRACT FROM AUTHOR]

The influence of different types of solvents as sheath fluids on the quality of electrospun ethyl cellulose (EC) nanofibers is investigated in this paper by a modified coaxial process. With 24 w/v % EC in ethanol as electrospinning core fluid and pure solvents including methanol, ethanol and N,N-dimethyl formamide (DMF) as sheath fluids, EC nanofibers were generated by the modified processes. Field emission scanning electron microscope observations demonstrate that the modified process is effective in improving the nanofibers' quality in terms of nanofibers' diameters, distributions and structural uniformity. The key of the modified coaxial process is the reasonable selection of the sheath solvents that is suitable for the drawing process of core EC fluid during the electrpospinning. The EC nanofibers' diameters (D, nm) could be manipulated through the reasonable selection of the type of the sheath solvents based on their boiling point (T, °C) D = 841-3.71T (R=0.9753). This paper provides useful methods for the implementation of the modified coaxial process controllably to obtain polymer nanofibers with high quality. [ABSTRACT FROM AUTHOR]

The influence of different types of solvents as sheath fluids on the quality of electrospun ethyl cellulose (EC) nanofibers is investigated in this paper by a modified coaxial process. With 24 w/v % EC in ethanol as electrospinning core fluid and pure solvents including methanol, ethanol and N,N-dimethyl formamide (DMF) as sheath fluids, EC nanofibers were generated by the modified processes. Field emission scanning electron microscope observations demonstrate that the modified process is effective in improving the nanofibers' quality in terms of nanofibers' diameters, distributions and structural uniformity. The key of the modified coaxial process is the reasonable selection of the sheath solvents that is suitable for the drawing process of core EC fluid during the electrpospinning. The EC nanofibers' diameters (D, nm) could be manipulated through the reasonable selection of the type of the sheath solvents based on their boiling point (T, °C) D = 841-3.71T (R=0.9753). This paper provides useful methods for the implementation of the modified coaxial process controllably to obtain polymer nanofibers with high quality. [ABSTRACT FROM AUTHOR]

Sustained-release ethyl cellulose (EC) micro-particles were prepared by electrospraying. Ketoprofen (KET) was taken as a model drug and various concentrations of EC functioned as a rate-controlling polymer. The morphology of the micro-particles was assessed using SEM. Images showed that as EC content increased, the granules shared similar surface characteristics containing pure EC. Micro-particle structures were analyzed by DSC, XRD, and FTIR. It was noted that the crystalline drug was converted into an amorphous form in all the granulations and that there was chemical interaction between KET and EC observed from FTIR. Dissolution studies revealed that as the amount of EC increased, the drug release rate decreased. This investigation suggests that electrospraying can be exploited as a useful tool for developing novel particulate drug delivery systems. [ABSTRACT FROM AUTHOR]

Abstract: Novel doughnut-shaped multi-layered drug delivery devices (DDDs) were developed with local variations of the drug and release-retardant material for providing linear release profiles. Based on computer-aided design models, different DDDs containing acetaminophen as a model drug, hydroxypropyl methylcellulose as matrix and ethyl cellulose (EC) as a release-retardant material were prepared automatically using a three-dimensional printing (3DP) system. In vitro dissolution assays demonstrated that all the 3DP DDDs had with different diameters, heights, concentrations of EC and central hole diameters were able to give linear release profiles. Morphological and erosion studies showed that acetaminophen was released through a simultaneous surface erosion process involving the outer peripheries and inner apertures. The barrier layers on both bases of DDDs had good adhesion strength with the drug-contained regions and offered consistent release retardation for the whole duration of the dissolution process. The release time periods of the DDDs were dependent on the annular thicknesses or the passes of binder solution containing a release-retardant material. The dosage of the DDD can be adjusted independently by changing the heights of the DDDs. Thus, 3DP is capable of offering novel strategies for developing DDDs with complex design features for desired drug release profiles. [Copyright &y& Elsevier]

A side-by-side electrospinning process characterized by a home-made eccentric spinneret was established to produce the Janus beads-on-a-string products. In this study, ketoprofen (KET) and methylene blue (MB) were used as model drugs, which loaded in Janus beads-on-a-string products, in which polyvinylpyrrolidone K90 (PVP K90) and ethyl cellulose (EC) were exploited as the polymer matrices. From SEM images, distinct nanofibers and microparticles in the Janus beads-on-a-string structures could be observed clearly. X-ray diffraction demonstrated that all crystalline drugs loaded in Janus beads-on-a-string products were transferred into the amorphous state. ATR-FTIR revealed that the components of prepared Janus nanostructures were compatibility. In vitro dissolution tests showed that Janus beads-on-a-string products could provide typical double drugs controlled-release profiles, which provided a faster immediate release of MB and a slower sustained release of KET than the electrospun Janus nanofibers. Drug releases from the Janus beads-on-a-string products were controlled through a combination of erosion mechanism (linear MB-PVP sides) and a typical Fickian diffusion mechanism (bead KET-EC sides). This work developed a brand-new approach for the preparation of the Janus beads-on-a-string nanostructures using side-by-side electrospinning, and also provided a fresh idea for double drugs controlled release and the potential combined therapy. [ABSTRACT FROM AUTHOR]

In nanopharmaceutics, polymeric coating is a popular strategy for modifying the drug release kinetics and, thus, new methods for implementing the nanocoating processes are highly desired. In the present study, a modified coaxial electrospraying process was developed to formulate an ultra-thin layer of ethyl cellulose (EC) on a medicated composite core consisting of tamoxifen citrate (TAM) and EC. A traditional single-fluid blending electrospraying and its monolithic EC-TAM nanoparticles (NPs) were exploited to compare. The modified coaxial processes were demonstrated to be more continuous and robust. The created NPs with EC coating had a higher quality than the monolithic ones in terms of the shape, surface smoothness, and the uniform size distribution, as verified by the SEM and TEM results. XRD patterns suggested that TAM presented in all the NPs in an amorphous state thanks to the fine compatibility between EC and TAM, as indicated by the attenuated total reflection (ATR)-FTIR spectra. In vitro dissolution tests demonstrated that the NPs with EC coating required a time period of 7.58 h, 12.79 h, and 28.74 h for an accumulative release of 30%, 50%, and 90% of the loaded drug, respectively. The protocols reported here open a new way for developing novel medicated nanoparticles with functional coating. [ABSTRACT FROM AUTHOR]

Highlights: [•] A new spinneret with Teflon nozzle for implementing electrospinning. [•] The Teflon nozzle facilitates energy transfer to the working fluid. [•] New knowledge about the interfacial interactions between Teflon/metal and fluids. [•] Producing quercetin-loaded composite fibers with higher quality. [•] Nanofibers from the new protocols provide better sustained drug release profile. [Copyright &y& Elsevier]

The most important property of a wound dressing is its anti-bacteria performance. Although electrospun nanofibers are frequently demonstrated to be potent candidates as wound dressings, no Janus fibers have been explored for this popular application. In this study, a Janus wound dressing composed of polyvinylpyrrolidone (PVP) and ethyl cellulose (EC) polymer matrices was prepared via a side-by-side electrospinning process, in which ciprofloxacin (CIP) and silver nanoparticles (AgNPs) were loaded in the two sides. A homemade acentric spinneret was exploited to maintain a continuous preparation process. Scanning and transmission electron microscope results demonstrated that the Janus fibers had a uniform and cylindrical morphology with a clear Janus structure, and AgNPs distributed in one side. X-ray diffraction patterns suggested that drug was present in the fibers in an amorphous state owing to rapid drying and its good compatibility with PVP, which was verified by infrared spectroscopy. In vitro tests showed that over 90% of CIP was released within the first 30 min, ensuring a strong antibacterial effect at the initial stages of wound healing. The Janus fibers were demonstrated to have good bactericidal activity against the growth of both Gram-positive S. aureus and Gram-negative E. coli. The PVP-CIP/EC-AgNPs Janus fibers could thus be a promising candidate for effective wound dressings. This work paves a new way for creating Janus structure-based advanced functional nanomaterials. Unlabelled Image • A side-by-side electrospinning process was conducted using a nanosuspension as a working fluid. • Hydrophilic polyvinylpyrrolidone and hydrophobic ethyl cellulose are combined into Janus fibers. • Ciprofloxacin and Ag nanoparticles are encapsulated into the Janus nanofibers. • The Janus nanofibers showed an improved performance against bacteria. [ABSTRACT FROM AUTHOR]

New strategies based on advanced technologies are highly desired for expanding the applications of biological macromolecules in the applied scientific fields. In the present study, a new kind of core-shell nano depots were designed, in which the shell section was a drug-polymer composite and the core section was a drug reservoir. With ethyl cellulose and ketoprofen as a filament-forming polymeric matrix and a model drug, respectively, a triaxial electrospinning apparatus was developed to conduct both coaxial and triaxial processes, by which monolithic nanofibers F1 and core-shell nano depots F2 were successfully prepared. Although both of them had the same double components, their different nanostructures generated considerable differences in providing drug sustained release profiles. The core-shell nanofiber depots F2 were able to provide a better zero-order drug release profile: no initial burst release, smooth sustained release effect, and smaller tailing-off release for a nice zero-order drug release kinetics. The release percentage (Q) can be linearly manipulated through the release time (t) according to the equation Q 2 = 9.40 + 4.74 t (R = 0.9936), providing opportunity for precise administration. The developed strategy and advanced electrospinning technique exhibit a new way for constructing process-structure-performance relationships at nano scale and for expanding the potential applications of biological macromolecules in the applied fields. Unlabelled Image • An ethyl cellulose based core-shell structural drug nanodepot • A modified triaxial electrospinning for preparing the depots • The depots have a drug distribution with a drug reservoir in a medicated shell. • The depots provided a zero-order drug sustained release profile. • An obvious process-nanostructure-performance relationship is exhibited. [ABSTRACT FROM AUTHOR]

• A side-by-side electrospinning exploiting a round charged surface. • Janus fibers containing hydrophilic and insoluble polymers for biphasic drug release. • Crescent surface for better fast release and round surface for better sustained release. • Combination of structure- and shape-performance based on Janus nanostructure. In nature, the combination of composition, structure, and shape determines the matter's functional performance to a large extent. Inspired by which, two electrospun Janus nanofiber formulations were created using side-by-side electrospinning in this work. Tamoxifen citrate (TAM) was used as a model drug and ethyl cellulose (EC) and polyvinylpyrrolidone K60 (PVP) as the polymer carrier matrices. The fibers have linear cylindrical morphologies and distinct Janus structures by scanning electron microscopy. One side of the fibers took a round shape, while the other was crescent-shaped. The drug was present in both polymer matrices in the form of amorphous solid dispersions, owing to strong intermolecular interactions between drug and polymer. In vitro dissolution tests demonstrated that both sets of fibers could provide biphasic drug release due to the difference in solubility of PVP and EC. The different shape of TAM-EC and TAM-PVP side of the Janus structure resulted in a considerable variation in the drug release profiles. The Janus structure with crescent TAM-PVP side and round TAM-EC side gave a more rapid burst release in the first phase of release, and slower sustained release in the second phase. This work thus reports a new strategy for systematically developing advanced functional nanomaterials based on both shape- and structure-performance relationships. [ABSTRACT FROM AUTHOR]