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Updated: Aug 10, 2026

Generation and Recovery of β-cell Spheroids From Step-growth PEG-peptide Hydrogels
Published on: December 6, 2012
Controlled and complete release of a model poorly water-soluble drug, prednisolone, from hydroxypropyl
V M Rao1, J L Haslam, V J Stella
1The Department of Pharmaceutical Chemistry, 2095 Constant Avenue, The University of Kansas, Lawrence, Kansas 66047, USA.
Abstract:
Sustained-release formulations such as hydroxypropyl methylcellulose (HPMC)-based hydrophilic matrix tablets of poorly water-soluble drugs often result in incomplete release because of the poor solubility and dissolution rate of the drug in the hydrophilic matrix. Sulfobutylether-beta-cyclodextrins ((SBE)(7M)-beta-CDs) have been known to improve the solubility of such drugs by forming inclusion complexes. The present paper deals with the modification of drug release from an HPMC-based matrix tablet of a sparingly water-soluble drug, prednisolone (PDL), using (SBE)(7M)-beta-CD as a solubilizing agent. Tablets were prepared by direct compression of a physically mixed PDL, (SBE)(7M)-beta-CD, and polymer. On exposure to water, an in situ PDL:(SBE)(7M)-beta-CD complex was formed in the gel layer, and enhanced drug release relative to a control formulation was observed (lactose used as the excipient instead of (SBE)(7M)-beta-CD ). Other possible changes due to the incorporation of (SBE)(7M)-beta-CD in the formulation were also probed. Incorporation of (SBE)(7M)-beta-CD lead to a higher water uptake relative to the control (lactose) formulation. For a fixed total tablet weight, polymer type, and loading, the drug release rate appeared to depend on the molar ratio of (SBE)(7M)-beta-CD to PDL and not the absolute amount of (SBE)(7M)-beta-CD present in the matrix tablet. This work shows that incorporation of (SBE)(7M)-beta-CD into the matrix tablets could be considered in designing a sustained-release tablet of poorly water-soluble drugs.
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