| Purpose: The objective of this study was to improve the permeability and water solubility rate of
a poor water soluble drug, cyclosporine A (CsA).
Methods: In order to improve the drug dissolution rate and oral bioavailability, electrospinning
method was used as an approach to prepare. The fibers were evaluated for surface morphology,
thermal characterizations, drug crystallinity, in vitro drug release and in vivo bioavailability
studies.
Results: Scanning electron microscope (SEM) results confirmed that the fibers were in microsize range and the size of the fibers was in the rang of 0.2 to 2 micron. Differential scanning
calorimetry (DSC) and powder X-ray diffractometry (XRPD) analysis ensured that the crystalline
lattice of drug were weakened or destroyed in the fibers. The drug release was 15.28%, 20.67%,
and 32.84% from pure drug, fibers of formulation B, and formulation A, respectively. In vivo
study results indicated that the bioavailability parameters of the optimized fiber formulation
were improved and the maximum concentration (Cmax) were significantly higher for fibers (3001
ng/mL) than for pure drug (2550 ng/mL). The dissolution rate of the formulations was dependent
on the nature and ratio of drug to carriers.
Conclusion: The physicochemical properties showed that the optimized mixture of polyethylene
glycol (PEG) and povidone (PVP) fibers could be an effective carrier for CsA delivery. PEG and
PVP fibers improved the absolute bioavailability and drug dissolution rate with appropriate
physicochemical properties. |