Controlled poorly soluble drug release from solid self-microemulsifying formulations with high viscosity hydroxypropylmethylcellulose

Tao Yi, Jiangling Wan, Huibi Xu, Xiangliang Yang

Research output: Contribution to journalArticlepeer-review

43 Citations (Scopus)

Abstract

The objective of this work was the development of a controlled release system based on self-microemulsifying mixture aimed for oral delivery of poorly water-soluble drugs. HPMC-based particle formulations were prepared by spray drying containing a model drug (nimodipine) of low water solubility and hydroxypropylmethylcellulose (HPMC) of high viscosity. One type of formulations contained nimodipine mixed with HPMC and the other type of formulations contained HPMC and nimodipine dissolved in a self-microemulsifying system (SMES) consisting of ethyl oleate, Cremophor® RH 40 and Labrasol®. Based on investigation by transmission electron microscopy (TEM), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray powder diffraction, differences were found in the particle structure between both types of formulations. In vitro release was performed and characterized by the power law. Nimodipine release from both types of formulations showed a controlled release profile and the two power law parameters, n and K, correlated to the viscosity of HPMC. The parameters were also influenced by the presence of SMES. For the controlled release solid SMES, oil droplets containing dissolved nimodipine diffused out of HPMC matrices following exposure to aqueous media. Thus, it is possible to control the in vitro release of poorly soluble drugs from solid oral dosage forms containing SMES.

Original languageEnglish
Pages (from-to)274-280
Number of pages7
JournalEuropean Journal of Pharmaceutical Sciences
Volume34
Issue number4-5
DOIs
Publication statusPublished - 7 Aug 2008
Externally publishedYes

Keywords

  • Controlled release
  • Hydroxypropylmethylcellulose
  • Poorly soluble drugs
  • Self-microemulsifying
  • Spray drying

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