Drug loading into beta-cyclodextrin granules using a supercritical fluid process for improved drug dissolution

Eur J Pharm Sci. 2008 Mar 3;33(3):306-12. doi: 10.1016/j.ejps.2008.01.003. Epub 2008 Jan 11.

Abstract

To improve dissolution properties of drugs, a supercritical fluid (SCF) technique was used to load these drugs into a solid carrier. In this study, granules based on beta-cyclodextrin (betaCD) were applied as a carrier for poor water-soluble drug and loaded with a model drug (ibuprofen) using two different procedures: controlled particle deposition (CPD), SCF process and solution immersion (SI) as a conventional method for comparison. Using the CPD technique, 17.42+/-2.06wt.% (n=3) ibuprofen was loaded into betaCD-granules, in contrast to only 3.8+/-0.15wt.% (n=3) in the SI-product. The drug loading was confirmed as well by reduction of the BET surface area for the CPD-product (1.134+/-0.07m(2)/g) compared to the unloaded-granules (1.533+/-0.031m(2)/g). Such a reduction was not seen in the SI-product (1.407+/-0.048m(2)/g). The appearance of an endothermic melting peak at 77 degrees C and X-ray patterns representing ibuprofen in drug-loaded granules can be attributed to the amount of ibuprofen loaded in its crystalline form. A significant increase in drug dissolution was achieved by either drug-loading procedures compared to the unprocessed ibuprofen. In this study, the CPD technique, a supercritical fluid process avoiding the use of toxic or organic solvents was successfully applied to load drug into solid carriers, thereby improving the water-solubility of the drug.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calorimetry, Differential Scanning
  • Cellulose / chemistry
  • Crystallization
  • Drug Compounding / methods*
  • Ibuprofen / chemistry
  • Microscopy, Electron, Scanning
  • Povidone / chemistry
  • Solubility
  • Surface Properties
  • X-Ray Diffraction
  • beta-Cyclodextrins / chemistry*

Substances

  • beta-Cyclodextrins
  • Cellulose
  • Povidone
  • betadex
  • microcrystalline cellulose
  • Ibuprofen