Application of Electrospun Drug-Loaded Nanofibers in Cancer Therapy.

In the 21st century, chemotherapy stands as a primary treatment method for prevalent diseases, yet drug resistance remains a pressing challenge. Utilizing electrospinning to support chemotherapy drugs offers sustained and controlled release methods in contrast to oral and implantable drug delivery modes, which enable localized treatment of distinct tumor types. Moreover, the core-sheath structure in electrospinning bears advantages in dual-drug loading: the core and sheath layers can carry different drugs, facilitating collaborative treatment to counter chemotherapy drug resistance. This approach minimizes patient discomfort associated with multiple-drug administration. Electrospun fibers not only transport drugs but can also integrate metal particles and targeted compounds, enabling combinations of chemotherapy with magnetic and heat therapies for comprehensive cancer treatment. This review delves into electrospinning preparation techniques and drug delivery methods tailored to various cancers, foreseeing their promising roles in cancer treatment.

A combined electrohydrodynamic atomization method for preparing nanofiber/microparticle hybrid medicines.

Bacterial prostatitis is a challenging condition to treat with traditional dosage forms. Physicians often prescribe a variety of dosage forms with different administration methods, which fail to provide an efficient and convenient mode of drug delivery. The aim of this work was to develop a new type of hybrid material incorporating both electrosprayed core-shell microparticles and electrospun nanofibers. A traditional Chinese medicine (Ningmitai, NMT) and a Western medicine (ciprofloxacin, CIP) were co-encapsulated within this material and were designed to be released in a separately controlled manner. Utilizing polyvinylpyrrolidone (PVP) as a hydrophilic filament-forming polymer and pH-sensitive Eudragit® S100 (ES100) as the particulate polymeric matrix, a combined electrohydrodynamic atomization (EHDA) method comprising coaxial electrospraying and blending electrospinning, was used to create the hybrids in a single-step and straightforward manner. A series of characterization methods were conducted to analyze both the working process and its final products. Scanning electron microscopy and transmission electron microscopy revealed that the EHDA hybrids comprised of both CIP-PVP nanofibers and NMT-ES100 core-shell microparticles. Multiple methods confirmed the rapid release of CIP and the sustained release of NMT. The antibacterial experiments indicated that the hybrids exhibited a more potent antibacterial effect against Escherichia coli dh5α and Bacillus subtilis Wb800 than either the separate nanofibers or microparticles. The amalgamation of fibrous nanomedicine and particulate micromedicine can expand the horizon of new types of medicines. The integration of electrospinning and coaxial electrospraying provides a straightforward approach to fabrication. By combining hydrophilic soluble polymers and pH-sensitive polymers in the hybrids, we can ensure the separate sequential controlled release of CIP and NMT for a potential synergistic and convenient therapy for bacterial prostatitis.

Integrating Chinese Herbs and Western Medicine for New Wound Dressings through Handheld Electrospinning.

In this nanotechnology era, nanostructures play a crucial role in the investigation of novel functional nanomaterials. Complex nanostructures and their corresponding fabrication techniques provide powerful tools for the development of high-performance functional materials. In this study, advanced micro-nanomanufacturing technologies and composite micro-nanostructures were applied to the development of a new type of pharmaceutical formulation, aiming to achieve rapid hemostasis, pain relief, and antimicrobial properties. Briefly, an approach combining a electrohydrodynamic atomization (EHDA) technique and reversed-phase solvent was employed to fabricate a novel beaded nanofiber structure (BNS), consisting of micrometer-sized particles distributed on a nanoscale fiber matrix. Firstly, Zein-loaded Yunnan Baiyao (YB) particles were prepared using the solution electrospraying process. Subsequently, these particles were suspended in a co-solvent solution containing ciprofloxacin (CIP) and hydrophilic polymer polyvinylpyrrolidone (PVP) and electrospun into hybrid structural microfibers using a handheld electrospinning device, forming the EHDA product E3. The fiber-beaded composite morphology of E3 was confirmed through scanning electron microscopy (SEM) images. Fourier-transform infrared (FTIR) spectroscopy and X-ray diffraction (XRD) analysis revealed the amorphous state of CIP in the BNS membrane due to the good compatibility between CIP and PVP. The rapid dissolution experiment revealed that E3 exhibits fast disintegration properties and promotes the dissolution of CIP. Moreover, in vitro drug release study demonstrated the complete release of CIP within 1 min. Antibacterial assays showed a significant reduction in the number of adhered bacteria on the BNS, indicating excellent antibacterial performance. Compared with the traditional YB powders consisting of Chinese herbs, the BNS showed a series of advantages for potential wound dressing. These advantages include an improved antibacterial effect, a sustained release of active ingredients from YB, and a convenient wound covering application, which were resulted from the integration of Chinese herbs and Western medicine. This study provides valuable insights for the development of novel multiscale functional micro-/nano-composite materials and pioneers the developments of new types of medicines from the combination of herbal medicines and Western medicines.

Recent Progress of Electrospun Herbal Medicine Nanofibers.

Herbal medicine has a long history of medical efficacy with low toxicity, side effects and good biocompatibility. However, the bioavailability of the extract of raw herbs and bioactive compounds is poor because of their low water solubility. In order to overcome the solubility issues, electrospinning technology can offer a delivery alternative to resolve them. The electrospun fibers have the advantages of high specific surface area, high porosity, excellent mechanical strength and flexible structures. At the same time, various natural and synthetic polymer-bound fibers can mimic extracellular matrix applications in different medical fields. In this paper, the development of electrospinning technology and polymers used for incorporating herbal medicine into electrospun nanofibers are reviewed. Finally, the recent progress of the applications of these herbal medicine nanofibers in biomedical (drug delivery, wound dressing, tissue engineering) and food fields along with their future prospects is discussed.

Electrospun Core-Sheath Nanofibers with Variable Shell Thickness for Modifying Curcumin Release to Achieve a Better Antibacterial Performance.

The inefficient use of water-insoluble drugs is a major challenge in drug delivery systems. Core-sheath fibers with various shell thicknesses based on cellulose acetate (CA) were prepared by the modified triaxial electrospinning for the controlled and sustained release of the water-insoluble Chinese herbal active ingredient curcumin. The superficial morphology and internal structure of core-sheath fibers were optimized by increasing the flow rate of the middle working fluid. Although the prepared fibers were hydrophobic initially, the core-sheath structure endowed fibers with better water retention property than monolithic fibers. Core-sheath fibers had flatter sustained-release profiles than monolithic fibers, especially for thick shell layers, which had almost zero-order release for almost 60 h. The shell thickness and sustained release of drugs brought about a good antibacterial effect to materials. The control of flow rate during fiber preparation is directly related to the shell thickness of core-sheath fibers, and the shell thickness directly affects the controlled release of drugs. The fiber preparation strategy for the precise control of core-sheath structure in this work has remarkable potential for modifying water-insoluble drug release and improving its antibacterial performance.

Electrospun Hydrophilic Janus Nanocomposites for the Rapid Onset of Therapeutic Action of Helicid.

The oral delivery of active ingredients for the fast onset of therapeutic effects is a well-known method in patients. In this study, a new kind of hydrophilic Janus structural nanocomposite was designed for the rapid dissolution and transmembrane permeation of helicid, an herbal medicine with poor water solubility. A side-by-side electrospinning process characterized by an eccentric spinneret was developed to fabricate the Janus nanocomposites. The morphology, inner structure, incorporated components and their physical states, hydrophilicity, and functional performances of the Janus nanocomposites were investigated. The experimental results demonstrated that an unspinnable fluid (polyvinylpyrrolidone K10-sodium dodecyl sulfate) could be simultaneously treated with an electrospinnable fluid (polyvinylpyrrolidone K90-helicid) to create Janus structural nanocomposites. The prepared Janus nanofibers exhibited linear morphology and notable side-by-side inner structure with all the incorporated components present in an amorphous state. Both the control of monolithic nanocomposites and the Janus composites can provide more than 10-fold the transmembrane rates of crude helicid particles. Compared with monolithic nanocomposites, the Janus nanocomposites exhibited improved hydrophilicity and can further promote the dissolution and transmembrane permeation of helicid for a potentially faster onset of therapeutic actions. The generation mechanisms and functional performance of Janus nanocomposites were suggested. The preparation protocols reported here can provide a useful approach for designing and developing new functional nanocomposites in the form of Janus structures. Meanwhile, the medicated hydrophilic Janus nanocomposites represent a newly developed kind of nano drug delivery system for the fast onset of therapeutic action of orally administered water-insoluble drugs.

Electrospun pH-sensitive core-shell polymer nanocomposites fabricated using a tri-axial process.

A modified tri-axial electrospinning process was developed for the generation of a new type of pH-sensitive polymer/lipid nanocomposite. The systems produced are able to promote both dissolution and permeation of a model poorly water-soluble drug. First, we show that it is possible to run a tri-axial process with only one of the three fluids being electrospinnable. Using an electrospinnable middle fluid of Eudragit S100 (ES100) with pure ethanol as the outer solvent and an unspinnable lecithin-diclofenac sodium (PL-DS) core solution, nanofibers with linear morphology and clear core/shell structures can be fabricated continuously and smoothly. X-ray diffraction proved that these nanofibers are structural nanocomposites with the drug present in an amorphous state. In vitro dissolution tests demonstrated that the formulations could preclude release in acidic conditions, and that the drug was released from the fibers in two successive steps at neutral pH. The first step is the dissolution of the shell ES100 and the conversion of the core PL-DS into sub-micron sized particles. This frees some DS into solution, and later the remaining DS is gradually released from the PL-DS particles through diffusion. Ex vivo permeation results showed that the composite nanofibers give a more than twofold uplift in the amount of DS passing through the colonic membrane as compared to pure DS; 74% of the transmitted drug was in the form of PL-DS particles. The new tri-axial electrospinning process developed in this work provides a platform to fabricate structural nanomaterials, and the core-shell polymer-PL nanocomposites we have produced have significant potential applications for oral colon-targeted drug delivery. STATEMENT OF SIGNIFICANCE: A modified tri-axial electrospinning is demonstrated to create a new type of core-shell pH-sensitive polymer/lipid nanocomposites, in which an electrospinnable middle fluid is exploited to support the un-spinnable outer and inner fluids. The structural nanocomposites are able to provide a colon-targeted sustained release and an enhanced permeation performance of diclofenac sodium. The developed tri-axial process can provide a platform for fabricating new structural nanomaterials with high quality. The strategy of a combined usage of polymeric excipients and phospholipid in a core-shell format should provide new possibilities of developing novel drug delivery systems for efficacious oral administration of poorly-water soluble drugs.

Liposomes self-assembled from electrosprayed composite microparticles.

Composite microparticles, consisting of polyvinylpyrrolidone (PVP), naproxen (NAP) and lecithin (PC), have been successfully prepared using an electrospraying process and exploited as templates to manipulate molecular self-assembly for the synthesis of liposomes in situ. Field emission scanning electron microscope (FESEM) and transmission electron microscope (TEM) observations demonstrate that the microparticles have an average diameter of 960 ± 140 nm and a homogeneous structure. X-ray diffraction (XRD) patterns, differential scanning calorimetry (DSC) and attenuated total reflectance-Fourier transform infrared (ATR-FTIR) results verify that the building blocks NAP and PC are scattered in the polymer matrix in a molecular way owing to the very fast drying of the electrospraying process and the favorable secondary interactions among the components. FESEM, scanning probe microscope (SPM) and TEM observations demonstrate that the liposomes can be achieved through molecular self-assembly in situ when the microparticles contact water thanks to 'like prefers like' and by means of the confinement effect of the microparticles. The liposomes have an encapsulation rate of 91.3%, and 80.7% of the drug in the liposomes can be freed into the dissolution medium in a sustained way and by a diffusion mechanism over a period of 24 h. The developed strategy not only provides a new, facile, and effective method to assemble and organize molecules of multiple components into liposomes with electrosprayed microparticles as templates, but also opens a new avenue for nanofabrication in a step-by-step and controllable way.