Document Detail

Amorphous formulations of indomethacin and griseofulvin prepared by electrospinning.
MedLine Citation:
PMID:  25317777     Owner:  NLM     Status:  Publisher    
Following a series of optimisation experiments, two series of electrospun polyvinylpyrrolidone (PVP) fibres were prepared. One set of fibres contained various loadings of indomethacin, known to form stable glasses, and the other griseofulvin (a poor glass former). Drug loadings of up to 33 % w/w were achieved. Electron microscopy data showed the fibres largely to comprise smooth and uniform cylinders, with evidence for solvent droplets in some samples. In all cases, the drug was found to exist in the amorphous physical state in the fibre on the basis of X-ray diffraction and differential scanning calorimetry (DSC) measurements. Modulated temperature DSC showed that the relationship between a formulation's glass transition temperature (Tg) and the drug loading follows the Gordon-Taylor equation, but not the Fox equation. The results of Gordon-Taylor analysis indicated that the drug/polymer interactions were stronger with indomethacin. The interactions between drug and polymer were explored using molecular modelling simulations, and found to be stronger with indomethacin; the presence of such intermolecular interactions was further confirmed using IR spectroscopy. The amorphous form of both drugs was found to be stable after storage for 8 months in a desiccator (relative humidity < 25 %). Finally, the functional performance of the fibres was studied; in all cases, the drug-loaded fibres released their drug cargo very rapidly, offering accelerated dissolution over the pure drug.
Felipe L Lopez; Gemma C Shearman; Simon Gaisford; Gareth R Williams
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-10-15
Journal Detail:
Title:  Molecular pharmaceutics     Volume:  -     ISSN:  1543-8392     ISO Abbreviation:  Mol. Pharm.     Publication Date:  2014 Oct 
Date Detail:
Created Date:  2014-10-15     Completed Date:  -     Revised Date:  2014-10-16    
Medline Journal Info:
Nlm Unique ID:  101197791     Medline TA:  Mol Pharm     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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