The release behavior of doxorubicin hydrochloride from medicated fibers prepared by emulsion-electrospinning

State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Changchun, China.
European Journal of Pharmaceutics and Biopharmaceutics (Impact Factor: 3.38). 04/2008; 70(1):165-70. DOI: 10.1016/j.ejpb.2008.03.010
Source: PubMed


The release behavior of a water-soluble small molecule drug from the drug-loaded nanofibers prepared by emulsion-electrospinning was investigated. Doxorubicin hydrochloride (Dox), a water-soluble anticancer agent, was used as the model drug. The laser scanning confocal microscopic images indicated that the drug was well incorporated into amphiphilic poly(ethylene glycol)-poly(L-lactic acid) (PEG-PLA) diblock copolymer nanofibers, forming "core-sheath" structured drug-loaded nanofibers. The drug release behavior of this drug-loaded system showed a three-stage diffusion-controlled mechanism, in which the release rate of the first stage was slower than that of the second stage, but both obeyed Fick's second law. Based on these results, it is concluded that the Dox-loaded fibers prepared by emulsion-electrospinning represent a reservoir-type delivery system in which the Dox release rate decreases with the increasing Dox content in the fibers.

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    • "Controlled release drug therapy is a process in which a predetermined concentration of a drug is delivered to a particular target over a specified duration, in a predicted behavior [1]. The main goal of this process is to increase the effectiveness of the drug by means of localizing the delivery, decreasing the side effects, decreasing the number of the administrations and even elimination of specialized administration methods [1] [2]. Numerous studies have been carried out in order to design, characterize and develop controlled drug delivery systems; the focus has been aimed in particular towards drug delivery systems that utilize biodegradable polymers such as different grades of poly(lactic acid) [3e6]. "
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    ABSTRACT: In vitro drug release mechanism of core/shell nanofibers of poly(methyl methacrylate)(PMMA)–nylon6 fabricated through coaxial electrospinning containing different concentrations of ampicillin was investigated. Scanning electron microscopy (SEM), transmission electron microscopy (TEM), Korsmeyer–Peppas equation and Fickian diffusion model were utilized to characterize the system. Antibacterial activity of the designed drug delivery system was investigated against Gram-positive Listeria innocua through optical density (OD) measurement. The system showed sustained drug release through three stages; although the release in stage I followed non-Fickian diffusion, Fickian diffusion was proven to be the release mechanism of stages II and III. A significant decrease in the diffusion coefficient from stage II to stage III was observed, which is believed to be the consequence of crystallization of fibers as a result of long-term incubation in an aqueous solution. Finally, the antibacterial activity of the system was verified by means of optical density (OD) measurements against Gram-positive L. innocua.
    Polymer 05/2013; 54(11):2699–2705. DOI:10.1016/j.polymer.2013.03.046 · 3.56 Impact Factor
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    • "Electrospinning is a versatile polymer processing technique to fabricate engineered scaffolds with micro to nanoscale topography and high porosity mimic to the natural extracellular matrix (ECM) [1] [2]. It offers great flexibility in terms of material selection for drug delivery applications, and a rich variety of drugs have been physically or chemically formulated within electrospun nanofibers or on their surfaces, such as antibiotics [3] [4] [5] [6] [7], anticancer drugs [8] [9], proteins [10] [11], and DNA [12] [13] [14]. Meanwhile, the drug release mechanism is associated with polymer degradation and diffusion pathway, and the release profile of drug from electrospun nanofibers may be tuned by the polymer composition and fiber morphology [15]. "
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    ABSTRACT: Fabrication of nanofiber-based drug delivery system with controlled release property is of general interest in biomedical sciences. In this study, we prepared an antibiotic drug tetracycline hydrochloride (TCH)-loaded halloysite nanotubes/poly(lactic-co-glycolic acid) composite nanofibers (TCH/HNTs/PLGA), and evaluated the drug release and antibacterial activity of this drug delivery system. The structure, morphology, and mechanical properties of the formed electrospun TCH/HNTs/PLGA composite nanofibrous mats were characterized using scanning electron microscopy (SEM), Fourier transform infrared spectroscopy, and tensile testing. We show that the incorporation of TCH-loaded HNTs within the PLGA nanofibers is able to improve the tensile strength and maintain the three-dimensional structure of the nanofibrous mats. In vitro viability assay and SEM morphology observation of mouse fibroblast cells cultured onto the fibrous scaffolds demonstrate that the developed TCH/HNTs/PLGA composite nanofibers are cytocompatible. More importantly, the TCH/HNTs/PLGA composite nanofibers are able to release the antibacterial drug TCH in a sustained manner for 42 days and display antimicrobial activity solely associated with the encapsulated TCH drug. With the improved mechanical durability, sustained drug release profile, good cytocompatibility, and non-compromised therapeutic efficacy, the developed composite electrospun nanofibrous drug delivery system may be used as therapeutic scaffold materials for tissue engineering and drug delivery applications.
    Colloids and surfaces B: Biointerfaces 04/2013; 110C:148-155. DOI:10.1016/j.colsurfb.2013.04.036 · 4.15 Impact Factor
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    • "[28] [29] Therefore, a site-specific and targeted DDS is essential to overcome these problems in the effective treatment of cancers using Dox as an anticancer agent. Application of liposomes,[30] [31] hydrogels,[32] microspheres,[33] polymeric micelles,[34] drug-polymer conjugates,[35] magnetic nanoparticles [36] [37] and nanofibrous scaffolds [38] [39] have been reported in literature. "
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    ABSTRACT: In this study, stimuli-responsive nanofibers (NFs) were successfully prepared via electrospinning method. Poly(N-isopropylacrylamide-co-acrylamide-co-vinylpyrrolidone) P(NIPAAM-AAm-VP) was used as the material for preparing the electrospinning NFs. Doxorubicin (Dox)-loaded NFs were prepared and characterized by XRD, Scanning electron microscopy and FTIR. A response surface methodology was used to evaluate the effect of key parameters on the fiber diameter. The cytotoxicity of Dox-loaded NFs was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide, a tetrazole assay on lung cancer A549 cell lines. In vitro cytotoxicity assay showed that the P(NIPAAM-AAm-VP) fibers themselves did not affect the growth of A549 cells. Antitumor activity of the Dox-loaded fibers against the cells was kept over the whole experimental process, while that of pristine Dox disappeared within 48 h. Drug release pattern from these systems is in zero order and drug release rate is not dependent on drug/polymer ratio in different implant formulations. These novel NFs were stable and preserved their morphology even after incubation in release medium (pH 7.4, 37 °C), while collapsed and dispersed quickly in aqueous solution of acidic medium at room. The reported incorporation of stimuli-responsive properties into NFs takes advantage of their extremely large surface area and porosity and is expected to provide a simple platform for smart drug delivery.
    Designed Monomers & Polymers 02/2013; 16(6). DOI:10.1080/15685551.2013.771303 · 2.78 Impact Factor
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