The AAPS Journal

, Volume 12, Issue 2, pp 158–170 | Cite as

Formulation and Evaluation of a Protein-loaded Solid Dispersions by Non-destructive Methods

Research Article

Abstract

The purpose of this investigation was to develop solid dispersion (SD) formulation of cyclosporine (CyA) using polyethylene glycol (PEG-6000) to enhance its dissolution rate followed by nondestructive method for the prediction of both drug and carrier. SD formulations were prepared by varying the ratio of CyA and PEG-6000 by solvent evaporation technique and characterized by dissolution, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transform infrared (FTIR), powder X-ray diffraction (PXRD), near infrared (NIR) and near infrared chemical imaging (NIR-CI). Dissolution data revealed enhanced dissolution of CyA when compared with pure CyA. DSC results showed that the crystallinity of PEG-6000 has decreased as indicated by decrease in the enthalpy of fusion and melting peak in the formulations. FTIR data demonstrated no chemical interaction between drug and carrier. The surface morphology of SD formulations was similar to PEG-6000 particle. NIR-CI disclosed homogeneity of SD matrix as indicated by symmetrical histograms with smaller values of skewness. Similar to NIR, a multivariate peak evaluation with principal component analysis and partial least square (PLS) were carried out with PXRD spectral data. PLS models with both techniques showed good correlation coefficient and smaller value of root mean square of errors. The accuracy of model for predicting CyA and PEG-6000 in NIR and PXRD data were 5.22%, 5.35%, 5.27%, and 2.10%, respectively. In summary, chemometric applications of non-destructive method sensors provided a valuable means of characterization and estimation of drug and carrier in the novel formulations.

Key words

cyclosporin NIR PEG-6000 PXRD solid dispersion 

Notes

Acknowledgments

The authors would like to thank the Oak Ridge Institute for Science and Education (ORISE) for supporting post doctoral research program. The views presented in this article do not necessarily reflect those of the US Food and Drug Administration.

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Copyright information

© American Association of Pharmaceutical Scientists 2010

Authors and Affiliations

  • Ziyaur Rahman
    • 1
  • Ahmed S. Zidan
    • 1
    • 2
  • Mansoor A. Khan
    • 1
    • 3
  1. 1.Division of Product Quality and ResearchCenter of Drug Evaluation and Research, Food and Drug AdministrationSilver SpringUSA
  2. 2.Faculty of PharmacyZagazig UniversityZagazigEgypt
  3. 3.FDA/CDER/DPQRSilver SpringUSA

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