Multicomponent amorphous nanofibers electrospun from hot aqueous solutions of a poorly soluble drug.
OBJECTIVE
To design and fabricate multicomponent amorphous electrospun nanofibers for synergistically improving the dissolution rate and permeation profiles of poorly water-soluble drugs.


METHODS
Nanofibers were designed to be composed of a poorly water soluble drug, helicid, a hydrophilic polymer polyvinylpyrrolidone as filament-forming matrix, sodium dodecyl sulfate as transmembrane enhancer and mannitol as taste masking agent, and were prepared from hot aqueous co-dissolving solutions of them. An elevated temperature electrospinning process was developed to fabricate the composite nanofibers, which were characterized using FESEM, DSC, XRD, ATR-FTIR, in vitro dissolution and permeation tests.


RESULTS
The composite nanofibers were homogeneous with smooth surfaces and uniform structure, and the components were combined together in an amorphous state because of the favorable interactions such as hydrogen bonding, electrostatic interaction and hydrophobic interactions among them. In vitro dissolution and permeation tests demonstrated that the composite nanofibers had a dissolution rate over 26-fold faster than that of crude helicid particles and a 10-fold higher permeation rate across sublingual mucosa.


CONCLUSIONS
A new type of amorphous material in the form of nanofibers was prepared from hot aqueous solutions of multiple ingredients using an electrospinning process. The amorphous nanofibers were able to improve the dissolution rate and permeation rate of helicid.
Yu
Deng-Guang
DG
College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, Shanghai, 201620, China. ydg017@dhu.edu.cn
Gao
Li-Dong
LD
White
Kenneth
K
Branford-White
Christopher
C
Lu
Wei-Yue
WY
Zhu
Li-Min
LM
D002152:Calorimetry, Differential Scanning; D008855:Microscopy, Electron, Scanning; D057139:Nanofibers; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D012995:Solubility; D012996:Solutions; D017550:Spectroscopy, Fourier Transform Infrared; D014867:Water; D014961:X-Ray Diffraction
D004364:Pharmaceutical Preparations; D012996:Solutions; D014867:Water