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During the past several decades, nanostructures have played their increasing influences on the developments of novel nano drug delivery systems, among which, double-chamber Janus nanostructure is a popular one. In this study, a new tri-channel spinneret was developed, in which two parallel metal capillaries were nested into another metal capillary in a core-shell manner. A tri-fluid electrospinning was conducted with a solvent mixture as the shell working fluid for ensuring the formation of an integrated Janus nanostructure. The scanning electronic microscopic results demonstrated that the resultant nanofibers had a linear morphology and two distinct compartments within them, as indicated by the image of a cross-section. Fourier Transformation Infra-Red spectra and X-Ray Diffraction patterns verified that the loaded poorly water-soluble drug, i.e. icariin, presented in the Janus medicated nanofibers in an amorphous state, which should be attributed to the favorable secondary interactions between icariin and the two soluble polymeric matrices, i.e. hydroxypropyl methyl cellulose (HPMC) and polyvinylpyrrolidone (PVP). The in vitro dissolution tests revealed that icariin, when encapsulated within the Janus nanofibers, exhibited complete release within a duration of 5 min, which was over 11 times faster compared to the raw drug particles. Furthermore, the ex vivo permeation tests demonstrated that the permeation rate of icariin was 16.2 times higher than that of the drug powders. This improvement was attributed to both the rapid dissolution of the drug and the pre-release of the trans-membrane enhancer sodium lauryl sulfate from the PVP side of the nanofibers. Mechanisms for microformation, drug release, and permeation were proposed. Based on the methodologies outlined in this study, numerous novel Janus nanostructure-based nano drug delivery systems can be developed for poorly water-soluble drugs in the future., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2024 Elsevier B.V. All rights reserved.)

The shapes of micro- and nano-products have profound influences on their functional performances, which has not received sufficient attention during the past several decades. Electrohydrodynamic atomization (EHDA) techniques, mainly include electrospinning and electrospraying, are facile in manipulate their products' shapes. In this review, the shapes generated using EHDA for modifying drug release profiles are reviewed. These shapes include linear nanofibers, round micro-/nano-particles, and beads-on-a-string hybrids. They can be further divided into different kinds of sub-shapes, and can be explored for providing the desired pulsatile release, sustained release, biphasic release, delayed release, and pH-sensitive release. Additionally, the shapes resulted from the organizations of electrospun nanofibers are discussed for drug delivery, and the shapes and inner structures can be considered together for developing novel drug delivery systems. In future, the shapes and the related shape-performance relationships at nanoscale, besides the size, inner structure and the related structure-performance relationships, would further play their important roles in promoting the further developments of drug delivery field. This article is categorized under: Therapeutic Approaches and Drug Discovery > Emerging Technologies., (© 2024 Wiley Periodicals LLC.)

The nanoproducts prepared by electrospinning have a large specific surface area, adjustable porosity, and controllable structure. Therefore, electrospinning has attracted an increasing attention in the current drug delivery systems (CDDs). In general cognition, the morphology of electrospinning nanoproducts should be homogeneous and stable to provide reproducible functions. Thus, numerous studies have been conducted to overcome the generation of beads-on-the-string by optimizing experimental conditions. This review introduces a specific electrospun nanoproduct, which is beads-on-thestring nanofibers. The presence of beads in the beads-on-the-string nanofibers can effectively encapsulate the model drug, which reduce the initial burst release of the drug and provide sustained release. At the same time, the beads-on-the-string nanofibers with composite structures can modulate the release properties of model drugs in CDDs. This review mainly summarizes the current research on the preparation of beads-on-the-string nanofibers by electrospinning and the application of beads-on-the-string nanofibers in the field of drug delivery. The future challenges and opportunities of beads-on-the-string nanofibers are also anticipated., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Porous organic polymers have received considerable attention in recent years because of their applicability as biomaterials. In particular, their hierarchical pore structures, variable morphologies, and tunable biological properties make them suitable as drug-delivery systems. In this review, the synthetic and post forming/control methods including templated methods, template-free methods, mechanical methods, electrospun methods, and 3D printing methods for controlling the hierarchical structures and morphologies of porous organic polymers are discussed, and the different methods affecting their specific surface areas, hierarchical structures, and unique morphologies are highlighted in detail. In addition, we discuss their applications in drug encapsulation and the development of stimuli (pH, heat, light, and dual-stimuli)-responsive materials, focusing on their use for targeted drug release and as therapeutic agents. Finally, we present an outlook concerning the research directions and applications of porous polymer-based drug delivery systems.

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.

The development of oral dosage forms for poorly water-soluble active pharmaceutical ingredients (APIs) is a persistent challenge. A range of methods has been explored to address this issue, and amorphous solid dispersions (ASDs) have received increasing attention. ASDs are typically prepared by starting with a liquid precursor (a solution or melt) and applying energy for solidification. Many techniques can be used, with the emergence of electrospinning as a potent option in recent years. This method uses electrical energy to induce changes from liquid to solid. Through the direct applications of electrical energy, electrospinning can generate nanofiber-based ASDs from drug-loaded solutions, melts and melt-solutions. The technique can also be combined with other approaches using the application of mechanical, thermal or other energy sources. Electrospinning has numerous advantages over other approaches to produce ASDs. These advantages include extremely rapid drying speeds, ease of implentation, compatibility with a wide range of active ingredients (including those which are thermally labile), and the generation of products with large surface areas and high porosity. Furthermore, this technique exhibits the potential to create so-called 'fifth-generation' ASDs with nanostructured architectures, such as core/shell or Janus systems and their combinations. These advanced systems can improve dissolution behaviour and provide programmable drug release profiles. Additionally, the fiber components and their spatial distributions can be precisely controlled. Electrospun fiber-based ASDs can maintain an incorporated active ingredient in the amorphous physical form for prolonged periods of time because of their homogeneous drug distribution within the polymer matrix (typically they comprise solid solutions), and ability to inhibit molecular motion. These ASDs can be utilised to generate oral dosage forms for poorly water-soluble drugs, resulting in linear or multiple-phase release of one or more APIs. Electrospun ASDs can also be exploited as templates for manipulating molecular self-assembly, offering a bridge between ASDs and other types of dosage forms. This review addresses the development, advantages and pharmaceutical applications of electrospinning for producing polymeric ASDs. Material preparation and analysis procedures are considered. The mechanisms through which performance has been improved are also discussed., (Copyright © 2018 Elsevier B.V. All rights reserved.)

Structural nanocomposites that provide fast dissolving drug release profiles are highly in demand in pharmaceutics. In this study, a poorly water-soluble drug such as quercetin or tamoxifen citrate (TC) was selected as a model active pharmaceutical ingredient. Core-shell nanofibers with ultra-thin shells were designed and prepared using modified coaxial electrospinning. Polyvinylpyrrolidone (PVP) K90 or Polycaprolactone (PCL) was selected as core. The drugs and PVP K10 were selected as shell. All types of solutions can be used as the shell fluids in modified coaxial process regardless of their electrospinnability, which means the increasing functional ingredients and unspinnable matrix can be processed. Evaluations via SEM and TEM demonstrated that the core-shell nanofibers had linear morphology with a shell thickness smaller than 100 nm. XRD and FTIR results showed that the model drug was distributed in the polymeric matrix amorphously and that PVP K10 had good compatibility with quercetin or TC. In vitro dissolution tests suggested that the core-shell nanofibers with ultra-thin shells released the loaded cargoes in the dissolution media within 1 min. The present investigation paved a new way for implementing the modified coaxial processes, which can be utilized to fabricate structural nanocomposites with ultra-thin shells for enhancing the fast dissolution of poorly water-soluble drugs., (Copyright © 2018 Elsevier B.V. All rights reserved.)

Background: Colon-specific pulsatile drug release, as a combined drug controlled-release model, is a useful drug delivery manner for a series of diseases. New nanomedicines and related preparation methods are highly desired., Methods: With diclofenac sodium (DS) as a model drug, a new type of structural nanocomposite (SC), in which composite polyvinylpyrrolidone (PVP)-DS core was coated by shellac, was fabricated via modified coaxial electrospinning. For comparison, traditional PVP-DS monolithic hydrophilic nanocomposites (HCs) were generated using a traditional blending process. Scanning electron microscopy (SEM), transmission electron microscopy (TEM), X-ray diffraction (XRD), attenuated total reflectance-Fourier transform infrared (ATR-FTIR), water contact angle (WCA), and in vitro dissolution and ex vivo permeation tests were conducted to characterize the composites., Results: SEM images demonstrated that both composites were linear nanofibers with smooth surface morphology and cross sections. TEM disclosed that the SCs had a thin shellac sheath layer of approximately 12 nm. XRD and ATR-FTIR results demonstrated that the crystalline DS was converted into amorphous composites with PVP because of favorable secondary interactions. WCA and in vitro dissolution tests demonstrated that the sheath shellac layers in SC could resist acid conditions and provide typical colon-specific pulsatile release, rather than a pulsatile release of HC under acid conditions. Ex vivo permeation results demonstrated that the SCs were able to furnish a tenfold drug permeation rate than the DS particles on the colon membrane., Conclusion: A new SC with a shellac coating on hydrophilic amorphous nanocomposites could furnish a colon-specific pulsatile drug release profile. The modified coaxial process can be exploited as a useful tool to create nanocoatings., Competing Interests: Disclosure The authors report no conflicts of interest in this work.

New methods for creating theranostic systems with simultaneous encapsulation of therapeutic, diagnostic, and targeting agents are much sought after. This work reports for the first time the use of coaxial electrospinning to prepare such systems in the form of core-shell fibers. Eudragit S100 was used to form the shell of the fibers, while the core comprised poly(ethylene oxide) loaded with the magnetic resonance contrast agent Gd(DTPA) (Gd(III) diethylenetriaminepentaacetate hydrate) and indomethacin as a model therapeutic agent. The fibers had linear cylindrical morphologies with clear core-shell structures, as demonstrated by electron microscopy. X-ray diffraction and differential scanning calorimetry proved that both indomethacin and Gd(DTPA) were present in the fibers in the amorphous physical form. This is thought to be a result of intermolecular interactions between the different components, the presence of which was suggested by infrared spectroscopy. In vitro dissolution tests indicated that the fibers could provide targeted release of the active ingredients through a combined mechanism of erosion and diffusion. The proton relaxivities for Gd(DTPA) released from the fibers into tris buffer increased (r1 = 4.79-9.75 s(-1) mM(-1); r2 = 7.98-14.22 s(-1) mM(-1)) compared with fresh Gd(DTPA) (r1 = 4.13 s(-1) mM(-1) and r2 = 4.40 s(-1) mM(-1)), which proved that electrospinning has not diminished the contrast properties of the complex. The new systems reported herein thus offer a new platform for delivering therapeutic and imaging agents simultaneously to the colon.

A series of 5-fluorouracil (5-FU) loaded core/shell electrospun fibers is reported. The fibers have shells made of Eudragit S100 (ES-100), and drug-loaded cores comprising poly(vinylpyrrolidone), ethyl cellulose, ES-100, or drug alone. Monolithic 5-FU loaded ES-100 fibers were also prepared for comparison. Electron microscopy showed all the fibers to have smooth cylindrical shapes, and clear core-shell structures were visible for all samples except the monolithic fibers. 5-FU was present in the amorphous physical form in all the materials prepared. Dissolution studies showed that the ES-100 shell was not able to prevent drug release at pH 1.0, even though the polymer is completely insoluble at this pH: around 30-80% of the maximum drug release was reached after 2h immersion at pH 1.0. These observations are ascribed to the low molecular weight of 5-FU permitting it to diffuse through pores in the ES-100 coating, and the relatively high acid solubility of the drug providing a thermodynamic impetus for this to happen. In addition, the fibers were observed to be broken or merged following 2h at pH 1.0, giving additional escape routes for the 5-FU., (Copyright © 2015 Elsevier B.V. All rights reserved.)

This study investigates the usage of a spinneret with a Teflon nozzle for fabrication of higher quality drug sustained-release electrospun nanofibers. Ethyl cellulose (EC) and quercetin were used as a filament-forming polymer matrix and an active pharmaceutical ingredient, respectively. The electrospinning was conducted using both a traditional stainless steel spinneret and a spinneret with a Teflon nozzle. Experimental results demonstrated that a Teflon-fluid interface at the spinneret's nozzle provided a better performance for implementing electrospinning than a traditional metal-fluid interface in the following aspects: (1) keeping more electrical energy on the working fluids for an efficacious process; (2) exerting less negative effect on the fluid to draw it back to the tube; and (3) making less possibility of clogging. The resulted nanofibers from the spinneret with a Teflon nozzle exhibited higher quality than those from the traditional spinneret in those: (1) smaller diameter and narrower distribution, 520±70 nm for the former and 750±280 nm for the later, as indicated by the field emission scanning electron microscopic images; and (2) better sustained-release profiles of quercetin from the former than the latter, as demonstrated by the in vitro dissolution tests. The new protocols about usage of Teflon as a spinneret's nozzle and the related knowledge disclosed here should promote the preparation and application of electrospun functional nanofibers., (Copyright © 2013 Elsevier B.V. All rights reserved.)

The objective of this study is to develop a structural nanocomposite of multiple components in the form of core-sheath nanofibres using coaxial electrospinning for the fast dissolving of a poorly water-soluble drug quercetin. Under the selected conditions, core-sheath nanofibres with quercetin and sodium dodecyl sulphate (SDS) distributed in the core and sheath part of nanofibres, respectively, were successfully generated, and the drug content in the nanofibres was able to be controlled simply through manipulating the core fluid flow rates. Field emission scanning electron microscope (FESEM) images demonstrated that the nanofibres prepared from the single sheath fluid and double core/sheath fluids (with core-to-sheath flow rate ratios of 0.4 and 0.7) have linear morphology with a uniform structure and smooth surface. The TEM images clearly demonstrated the core-sheath structures of the produced nanocomposites. Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) results verified that quercetin and SDS were well distributed in the polyvinylpyrrolidone (PVP) matrix in an amorphous state, due to the favourite second-order interactions. In vitro dissolution studies showed that the core-sheath composite nanofibre mats could disintegrate rapidly to release quercetin within 1 min. The study reported here provides an example of the systematic design, preparation, characterization and application of a new type of structural nanocomposite as a fast-disintegrating drug delivery system.

A drug-loaded nanofiber mesh which could achieve time-engineeringed biphasic release was fabricated through sequential electrospinning. The drug to polymer ratio of each single mesh was allocated and designed before the tri-layered meshes were created. The resultant meshes had the following construction: (i) the first drug-loaded mesh (top side), (ii) the second drug-loaded mesh (second side), and (iii) the third drug-loaded mesh (bottom side). The drug release speed and duration were controlled by designing morphological features of the electrospun meshes such as the fiber diameter and mesh thickness. An in vitro release experiment revealed that the tri-layered construction with distinct morphological features of each component mesh can provide biphasic drug release. The time-engineeringed dual release system using the multilayered electrospun nanofiber meshes was proved to be a useful formulation when achieving controlled drug release at different times., (Copyright © 2012 Elsevier B.V. All rights reserved.)

In this review article, some key challenges in drug delivery are first introduced and methods that have been applied in attempts to solve them enumerated. Particularly intractable problems are highlighted: these include issues of solubility, targeting and drug degradation. The technique of electrospinning is subsequently introduced, and the influence of processing parameters on the fibers produced discussed. The potential of electrospun nanofibers in drug delivery is then explored, with examples given from the recent literature to illustrate how fibers can be used to overcome hurdles in drug solubility, degradation and targeting. Future perspectives and challenges are also considered.

Cellulose acetate (CA) fibers loaded with the ester prodrugs of naproxen, including methyl ester, ethyl ester and isopropyl ester, were prepared through electrospinning using acetone/N,N-dimethylacetamide(DMAc)/ethanol (4:1:1, v/v/v) as solvent. The chemical and morphological characterizations of the medicated fibers were investigated by means of SEM, DSC, XRD and FTIR, as well as the studies of the drug release properties. The results indicated that the morphology and diameter of the fibers were influenced by the concentration of spinning solution, applied voltage, electrospun solvent and the surfactants. The average diameters of the fibers ranged between 100 and 500 nm for three prodrugs. There was good compatibility between CA and three prodrugs in the blended fibers, respectively. In vitro release indicated that constant drug release from the fiber was observed over 6 days. The prodrugs were successfully encapsulated into the fibers, and this system was stable in terms of effectiveness in release.

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.

In this study, three kinds of electrohydrodynamic atomization (EHDA) processes (electrospraying, electrospinning, and coaxial electrospinning) are implemented to create hydroxypropyl methylcellulose (HPMC) based ultra‐thin products for providing the fast dissolution of a poorly water‐soluble drug ketoprofen (KET). An EHDA apparatus, characterized by a novel spinneret, is homemade for conducting the three processes. The three types of products are electrospun nanofibers E1, electrosprayed microparticles E2, and core‐shell nanofibers E3. SEM and TEM results indicate that they have the anticipated morphologies and inner structures. X‐ray diffraction and Fourier Transform Infrared results verify that KET is mainly amorphous in all the composites due to its fine compatibility with HPMC. In vitro dissolution tests demonstrate that the drug rapid release performances has an order of E3>E1>E2≫KET powders. The fast dissolution mechanisms are suggested and the advantages of the three products are compared. The super performance of E3 in furnishing the rapid release is attributed to a synergistic action of small size (of the shell thickness), high porosity, amorphous state of drug, and the solubility of HPMC. EHDA nanostructures can support the development of nano drug delivery systems (DDSs) through tailoring the spatial distribution of drug molecules within the nano products. [ABSTRACT FROM AUTHOR]

Polymers are the backbone of drug delivery. Electrospinning has greatly enriched the strategies that have been explored for developing novel drug delivery systems using polymers during the past two decades. In this study, four different kinds of polymers, i.e., the water-soluble polymer poly (vinyl alcohol) (PVA), the insoluble polymer poly(ε-caprolactone) (PCL), the insoluble polymer Eudragit RL100 (ERL100) and the pH-sensitive polymer Eudragit S100 (ES100) were successfully converted into types of tri-layer tri-polymer core–shell fibers through bi-fluid coaxial electrospinning. During the coaxial process, the model drug metronidazole (MTD) was loaded into the shell working fluid, which was an emulsion. The micro-formation mechanism of the tri-layer core–shell fibers from the coaxial emulsion electrospinning was proposed. Scanning electron microscope and transmission electron microscope evaluations verified the linear morphology of the resultant fibers and their obvious tri-layer multiple-chamber structures. X-ray diffraction and Fourier transform infrared spectroscopy measurements demonstrated that the drug MTD presented in the fibers in an amorphous state and was compatible with the three polymeric matrices. In vitro dissolution tests verified that the three kinds of polymer could act in a synergistic manner for a prolonged sustained-release profile of MTD in the gut. The drug controlled-release mechanisms were suggested in detail. The protocols reported here pioneer a new route for creating a tri-layer core–shell structure from both aqueous and organic solvents, and a new strategy for developing advanced drug delivery systems with sophisticated drug controlled-release profiles. [ABSTRACT FROM AUTHOR]

Smart drug delivery, through which the drug molecules are delivered according to the requests of human biological rhythms or by maximizing drug therapeutic effects, is highly desired in pharmaceutics. Many biomacromolecules have been exploited for this application in the past few decades, both in industry and laboratories. Biphasic release, with an intentional pulsatile release and a following extended release stage, represents a typical smart drug delivery approach, which aims to provide fast therapeutic action and a long time period of effective blood drug concentration to the patients. In this study, based on the use of a well-known biomacromolecule, i.e., cellulose acetate (CA), as the drug (acetaminophen, ATP)-based sustained release carrier, a modified coaxial electrospraying process was developed to fabricate a new kind of core–shell nanoparticle. The nanoparticles were able to furnish a pulsatile release of ATP due to the shell polyvinylpyrrolidone (PVP). The time cost for a release of 30% was 0.32 h, whereas the core–shell particles were able to provide a 30.84-h sustained release of the 90% loaded ATP. The scanning electron microscope and transmission electron microscope results verified in terms of their round surface morphologies and the obvious core–shell double-chamber structures. ATP presented in both the core and shell sections in an amorphous state owing to its fine compatibility with CA and PVP. The controlled release mechanisms of ATP were suggested. The disclosed biomacromolecule-based process–structure–performance relationship can shed light on how to develop new sorts of advanced nano drug delivery systems. [ABSTRACT FROM AUTHOR]

Poly(α-L-glutamic acid) (PGA) is a class of synthetic polypeptides composed of the monomeric unit α-L-glutamic acid. Owing to their biocompatibility, biodegradability, and non-immunogenicity, PGA-based nanomaterials have been elaborately designed for drug delivery systems. Relevant studies including the latest research results on PGA-based nanomaterials for drug delivery have been discussed in this work. The following related topics are summarized as: (1) a brief description of the synthetic strategies of PGAs; (2) an elaborated presentation of the evolving applications of PGA in the areas of drug delivery, including the rational design, precise fabrication, and biological evaluation; (3) a profound discussion on the further development of PGA-based nanomaterials in drug delivery. In summary, the unique structures and superior properties enables PGA-based nanomaterials to represent as an enormous potential in biomaterials-related drug delivery areas. [ABSTRACT FROM AUTHOR]

The present study reports the fabrication of medicated nanofibers for potential colon-targeted drug delivery using modified coaxial electrospinning, in which salt (NaCl) solutions were exploited as shell fluids to facilitate the preparation processes. A homemade concentric spinneret with an indented core capillary was developed to conduct the coaxial processes. Optical observations and scanning electron microscopic results demonstrated that the shell-to-core fluid flow rate ratio was a key parameter, which exerted a significant influence on the electrospinning processes and could be exploited to control the fibers’ morphology and diameters. A scaling law of D=0.173F-0.531 (R2=0.9976) was built, by which the nanofibers’ sizes can be predicted and manipulated easily. X-ray diffraction and attenuated total reflected FTIR tests verified that the medicated nanofibers were essentially a polymeric nanocomposite and the guest drug diclofenac sodium (DS) had fine compatibility with the host polymer. All the drug was encapsulated in the filament-forming carrier. In vitro dissolution experiments demonstrated that the medicated nanofibers could free the drug in a neutral condition, suggesting potential colon-targeted drug delivery applications. Ex vivo tests demonstrated that the medicated fiber mats could enhance the transmembrane of DS. Based on coaxial electrospinning, a new strategy is successfully developed for creating medicated nanomaterials. [ABSTRACT FROM AUTHOR]

Medicated shellac nanofibers providing colon-specific sustained release were fabricated using coaxial electrospinning. A solution of 7.5 g shellac and 1.5 g of ferulic acid (FA) in 10 mL ethanol was used as the core fluid, and a mixture of ethanol and N , N -dimethylformamide (8/10 v/v) as the shell. The presence of the shell fluid was required to prevent frequent clogging of the spinneret. The diameters of the fibers ( D ) can be manipulated by varying the ratio of shell to core flow rates ( F ), according to the equation D = 0.52 F −0.19 . Scanning electron microscopy images revealed that fibers prepared with F values of 0.1 and 0.25 had linear morphologies with smooth surfaces, but when the shell fluid flow rate was increased to 0.5 the fiber integrity was compromised. FA was found to be amorphously distributed in the fibers on the basis of X-ray diffraction and differential scanning calorimetry results. This can be attributed to good compatibility between the drug and carrier: IR spectra indicated the presence of hydrogen bonds between the two. In vitro dissolution tests demonstrated that there was minimal FA release at pH 2.0, and sustained release in a neutral dissolution medium. The latter occurred through an erosion mechanism. During the dissolution processes, the shellac fibers were gradually converted into nanoparticles as the FA was freed into solution, and ultimately completely dissolved. [ABSTRACT FROM AUTHOR]

The present study reports a new type of sedative nanofiber membranes that were developed to permit very rapid oral delivery of helicid with concomitant taste masking. A coaxial electrospinning process was exploited to prepare core-shell nanofibers and to control the spatial depositions of different functional components. A series of tests was undertaken to characterize the resultant nanofibers. Following optimization of the electrospinning parameters, two types of core-shell nanofibers with average diameters of 730 ± 140 and 770 ± 160 nm were successfully prepared. These had uniform linear morphologies and clear core-shell structures, as verified by scanning and transmission electron microscopy images. The fibers contained sucralose in the shell and helicid in the core; X-ray diffraction demonstrated that both functional components were present in the amorphous physical form. There is significant hydrogen bonding between the functional components and the poly(vinylpyrrolidone) used as the carrier matrix, as shown from Fourier transform infrared spectroscopy and molecular mechanics simulations. In vitro dissolution tests showed that the formulations were able to release the entire incorporated drug extremely rapidly (within 1 min) when they encountered a dissolution medium, whereas the commercially available product released only 13.4 % of its drug loading in the same time. By tailoring the distribution of functional ingredients in electrospun core-shell structures, new drug delivery systems which can both accelerate dissolution and also mask unpleasant tastes were produced. [ABSTRACT FROM AUTHOR]

Abstract: This study investigated a novel type of drug-delivery membrane prepared by a modified coaxial electrospinning process. Using 1% (w/v) unspinnable zein solution as sheath fluid, the coaxial electrospinning process can be smoothly conducted to generate ketoprofen (KET)-loaded zein nanofibers coated with a thin layer of blank zein. Scanning electron microscopy and transmission electron microscopy images demonstrated that the nanofibers had a ribbon morphology with a smooth surface, as well as average diameters of 860±210nm (coating thickness of ca. 20nm) and 680±140nm (coating thickness of ca. 30nm) at sheath-to-core flow rate ratios of 0.11 and 0.25, respectively. X-ray diffraction and differential scanning calorimetry verified that KET presented an amorphous state in all nanofibers. Attenuated total reflectance Fourier transform infrared spectroscopy demonstrated that zein had good compatibility with KET because of hydrogen bonding. In vitro dissolution tests showed that the nanofibers coated with blank zein did not exert any initial burst release effect, and can enable linear drug release over a period of 16h via a diffusion mechanism. The modified coaxial electrospinning process can provide new approaches to the development of nanofiber membranes with improved structural characteristics and performance. [Copyright &y& Elsevier]

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: Tamoxifen microcapsules and drug loaded medicated fabrics were investigated. The microcapsules were prepared using a complex coacervation procedure involving gelatin B and acacia gum. The morphology, particle size, drug loading capacity and in vitro release characteristics of the drug microcapsules were optimized for coating tamoxifen microcapsules onto the cotton fabrics. Infrared (IR) spectra and SEM were used to characterize the medicated fabrics and air permeability and laundering testing were undertaken to determine the efficiency and effectiveness of the system. Results showed that optimum condition for the microcapsules was at drug/polymer ratio 1:4, polymer concentration 3%, and rate of stirring 1000rpm. In vitro release assays demonstrated that the tamoxifen was liberated over 10h after an initial bust rate period. SEM images illustrated that the tamoxifen microcapsules were spherical in shape and were also tightly fixed on to the cotton fabrics fast. These observations demonstrate that we have designed and fabricated a medicated system that potentially could be applied within a transdermal drug delivery system and so act in a system for the treatment of breast cancer. [Copyright &y& Elsevier]

Three-dimensional printing (3DP) is a rapid prototyping (RP) technology. Prototyping involves constructing specific layers that uses powder processing and liquid binding materials. Reports in the literature have highlighted the many advantages of the 3DP system over other processes in enhancing pharmaceutical applications, these include new methods in design, development, manufacture, and commercialization of various types of solid dosage forms. For example, 3DP technology is flexible in that it can be used in applications linked to linear drug delivery systems (DDS), colon-targeted DDS, oral fast disintegrating DDS, floating DDS, time controlled, and pulse release DDS as well as dosage form with multiphase release properties and implantable DDS. In addition 3DP can also provide solutions for resolving difficulties relating to the delivery of poorly water-soluble drugs, peptides and proteins, preparation of DDS for high toxic and potent drugs and controlled-release of multidrugs in a single dosage forms. Due to its flexible and highly reproducible manufacturing process, 3DP has some advantages over conventional compressing and other RP technologies in fabricating solid DDS. This enables 3DP to be further developed for use in pharmaceutics applications. However, there are some problems that limit the further applications of the system, such as the selections of suitable excipients and the pharmacotechnical properties of 3DP products. Further developments are therefore needed to overcome these issues where 3DP systems can be successfully combined with conventional pharmaceutics. Here we present an overview and the potential 3DP in the development of new drug delivery systems. © 2008 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:3666–3690, 2008 [ABSTRACT FROM AUTHOR]

[Display omitted] • Tri-chamber nanofibers in the form of core–shell microstructure embedded on one side of the Janus main structure were designed. • Hydrophilic and pH sensitive polymers were combined skillfully in complicated structure nanocomposites. • The tri-chamber nanofibers facilitated the rapid release of quercetin and the delayed and sustained release of tamoxifen citrate. • The tri-chamber nanofibers could result in a synergistic anticancer action of quercetin and tamoxifen citrate. A tri-fluid electrospinning process was successfully developed to prepare tri-chamber complex nanofibers. The core–shell and Janus structure were combined to form a delicate and complicated architecture for solving the problem of co-administration of quercetin and tamoxifen citrate, improving the oral bioavailability, and enhancing their synergistic anti-breast cancer actions. Scanning electron microscope, transmission electron microscope and confocal fluorescent microscopy images showed the complex structure of the designed nanofibers. Fourier transform infrared and X-ray diffraction analyses verified that the model drugs and the polymeric excipients had good compatibility and were presented in an amorphous state. The in vitro release study certified that the tri-chamber nanofibers facilitated the rapid release of quercetin compared with that of the crude drug (90% versus 38%) and the delayed and sustained release of tamoxifen citrate at the same time interval (decreased by 1.88 times). The in vivo pharmacokinetic and pharmacodynamic analysis verified that the tri-chamber nanofibers could result in increased oral bioavailability and enhanced synergistic anticancer action of quercetin and tamoxifen citrate. The findings proved that a new medicated drug delivery system with advanced dual-, time-, and target-specific drug release profiles was developed using the electrospun complex nanostructure. [ABSTRACT FROM AUTHOR]

Abstract: Core–sheath nanofibers prepared using coaxial electrospinning were investigated for providing biphasic drug release profiles. With ketoprofen (KET) as the model drug, polyvinylpyrrolidone and zein as the sheath polymer and core matrix, respectively, the coaxial process could be carried out smoothly and continuously without any clogging of the spinneret. Scanning electron microscopy and transmission electron microscopy observations demonstrated that the nanofibers were linear with homogeneous structure and had a clear core–sheath structure with an average diameter of 730±190nm, in which the sheath had a thickness of ca. 90nm. Differential scanning calorimetric and X-ray diffraction analyses verified that all the components in the core–sheath nanofibers were present in an amorphous state. Attenuated total reflectance Fourier transform infrared spectra demonstrated both the sheath and core matrix had good compatibility with KET owing to hydrogen bonding. In vitro dissolution tests showed that the nanofibers could provide an immediate release of 42.3% of the contained KET, followed by a sustained release over 10h of the remaining drug. The present study exhibited a simple and useful approach to systematically design and fabricate nanostructures using coaxial electrospinning for providing biphasic drug release profiles. [Copyright &y& Elsevier]

Abstract: Fast-dissolving drug delivery membranes for poorly water-soluble drugs were prepared by electrospinning using feruloyl-oleyl-glycerol (FOG) as a model drug and polyvinylpyrrolidone (PVP) K90 as a polymer matrix in a mixed solvent of chloroform/ethanol (4:1, v/v). Results from Fourier-transform infrared spectroscopy (FT-IR) illustrated good compatibility between FOG and PVP as well as a good distribution of FOG within the fibers. The morphology and diameter of the fibers were influenced by the concentration of PVP and the applied voltage. When the PVP concentration was 5% (w/v) and the applied voltage was 14kV, uniform and smooth fibers were obtained, with diameter 700–800nm. Wetting time assays confirmed fast-dissolving properties with the average dissolution time for FOG-loaded PVP fiber membranes being 2.0±1.5s. These results demonstrate the potential of electrospinning solid dispersions to improve the dissolution profile of poorly water-soluble drugs. [Copyright &y& Elsevier]

The dissolution and controlled release of poorly water soluble drugs have been challenging during the past half century. Food ingredients are often exploited to implement some strategies to conceive new drug delivery systems as potential solutions. In this study, Janus zein–PVP medicated nanofibers were fabricated through side-by-side electrospinning and by using zein as a key filament-forming matrix and a drug carrier. Ferulic acid (FA), as a poorly water-soluble model drug, was loaded on both sides of the Janus fibers. The side-by-side electrospinning process was performed for a smooth and robust preparation. SEM and TEM revealed that the resultant Janus fibers had linear morphology without beads-on-a-string phenomena, smooth surface, and obvious side-by-side structure. The FA was present in the fibers in an amorphous state due to its fine compatibility with zein and PVP. In vitro dissolution tests verified that the Janus fibers manipulated the release of FA in a two-stage manner. The controlled release mechanism of the Janus fibers was proposed. On the basis of the application of zein, a process–structure–performance relationship, which should be useful for developing many new functional materials from biological macromolecules, was disclosed. Unlabelled Image • Zein is utilized to create medicated Janus structure • A modified side-by-side electrospinning is implemented to treat zein • The Janus fibers can provide a two-stage controlled release of ferulic acid • A clear process-nanostructure-performance relationship is exhibited [ABSTRACT FROM AUTHOR]

• Cellulose acetate-based trilayer core-shell fibers with discrete drug distribution. • A modified triaxial electrospinning for producing the complex nanostructure. • The nanofibers can provide an accurate dual-stage release of the loaded drug. • A clear process-nanostructure-performance relationship is exhibited. The combination of complex nanostructures with carbohydrate polymers can provide a strong platform for promoting the development of novel drug delivery systems. In this study, tri-layer core-shell nanofibers F2 with discrete drug distributions were prepared using cellulose acetate (CA) as a key filament-forming polymeric matrix and ketoprofen (KET) as a model drug. The discrete distribution was characterized by inserting a bank CA layer between the CA/KET core layer and the PVP/KET outer layer through a modified triaxial electrospinning. Compared with the traditional core-shell nanofibers F1, the tri-layer nanofibers F2 with drug discrete distributions provided better drug dual-stage release profiles in terms of accurate release contents at the first stage and longer time period sustained release at the second stage. Despite having the same components (drug, soluble PVP, and insoluble CA) and similar linear morphologies, core-shell nanofibers F1 and tri-layer nanofibers F2 exhibited significantly different functional performances in providing dual-stage release. The different structure-performance relationships of the two types of nanofibers have played their important roles on manipulating the accuracy of dual-stage drug controlled release profiles. The mechanism that the tri-layer core-shell nanostructure containing a blank CA middle layer adjusted the drug release behaviors was proposed. [ABSTRACT FROM AUTHOR]

In nanopharmaceutics, a robust manipulation of the preparation process and an accurate prediction of the final product size are very important for developing novel nano drug delivery systems. In the present study, for the first time, a process parameter, i.e. the length of the straight fluid jet, L , is correlated with an experimental parameter, i.e. fluid flow rate, F ; a nanofiber property, i.e. diameter, D ; and the corresponding drug-sustained release profile. Using a mixed solution consisting of 15% (w/v) polyacrylonitrile and 3% (w/v) ketoprofen in acetone and N , N -dimethylformamide (2:8, v:v) as a spinnable working fluid, a series of medicated nanofibers were prepared under variable F and were characterized. The analysis results disclosed the quantitative relationships among different types of parameters. The process parameter L exhibited a better linear relationship with the nanofibers' diameter (D) than the processing parameter F. These results give a hint that process parameters can be exploited as useful tools for accurately predicting and tailoring the resultant nanofibers' D , and in turn their functional performances. The strategy proposed here presents a new approach to investigate the electrohydrodynamic process and manipulate the functions of nanoproducts through process-property-performance relationships. [ABSTRACT FROM AUTHOR]