posted on 2016-06-09, 00:00authored byMiao Jin, Deng-Guang Yu, Carlos F. G. C. Geraldes, Gareth R. Williams, S. W. Annie Bligh
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.