title: Electrospinning of artemisinin-loaded core-shell fibers for inhibiting drug re-crystallization.
abstract: The main aim of this study was to inhibit the re-crystallization of a potent antimalarial drug, artemisinin (ART), by encapsulating it in core-shell fibers via a coaxially electrospun method. The ART-infiltrated cellulose acetate (CA) solution as the core material and poly(vinyl pyrrolidone) (PVP) solution as the shell material were used to prepared ART-loaded core-shell fibers ([ART/CA]/PVP). Transmission electron microscopy images confirmed the core-shell structures of the coaxially electrospun fibers. The scanning electron microscope (SEM), X-ray diffraction, and differential scanning calorimetry were performed to characterize the physical states of ART in the fibers. It was observed that ART crystals were formed in the ART-loaded CA/PVP composite fibers (ART/CA/PVP) during the electrospinning process and increased during storage duration. While ART crystals hardly were observed in the fresh core-shell [ART/CA]/PVP fibers with high ART entrapped amount (20 wt.%) and a little was detected after 6-month storage. Fourier transform infrared spectroscopy (FTIR) results illustrated the hydrogen bonding interaction between ART and CA in the core-shell [ART/CA]/PVP fibers mainly contributed to the amorphous state of ART. Importantly, combination of the hydrophilic PVP shell and the amorphous ART in CA core, the core-shell [ART/CA]/PVP fibers provided a continued and stable ART release manner. Ex vivo permeation studies suggested the amorphous ART in the medicated core-shell fibers could permeate through the stratum corneum smoothly. Hence, the core-shell [ART/CA]/PVP fiber matrix could provide a potential application in transdermal patches.
authors.affiliation: School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China.
authors.forename: Yongli
authors.initials: Y
authors.lastname: Shi
authors.forename: Jianhua
authors.initials: J
authors.lastname: Zhang
authors.forename: Shuxin
authors.initials: S
authors.lastname: Xu
authors.forename: Anjie
authors.initials: A
authors.lastname: Dong
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D037621:Artemisinins / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D003460:Crystallization; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000295:instrumentation; D004356:Drug Storage; D055664:Electrochemical Techniques / Q000295:instrumentation; D004867:Equipment Design; D006801:Humans; D057139:Nanofibers / Q000737:chemistry* / Q000648:ultrastructure; D011205:Povidone / Q000737:chemistry*; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D017550:Spectroscopy, Fourier Transform Infrared; D013552:Swine; D014961:X-Ray Diffraction
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D004337:Drug Carriers; C005062:acetylcellulose; D002482:Cellulose; C031327:artemisinin; D011205:Povidone