Formulation and in vitro characterization of a novel solid lipid-based drug delivery system

Chem Pharm Bull (Tokyo). 2014;62(12):1173-9. doi: 10.1248/cpb.c14-00339.

Abstract

The liquid self-emulsifying drug delivery system (L-SEDDS), commonly used to deliver effective but poorly water-soluble oleanolic acid (OA), has many limitations such as high manufacturing costs, few choices of dosage forms, risk of leakage from hard gelatin capsules, low stability, limited portability, incompatibility with capsule materials, and relatively restricted storage conditions. Thus the main purpose of our study was to develop a promising solid lipid-based drug delivery system (S-SEDDS) for OA. The S-SEDDS, prepared from wet granulation with an optimized L-SEDDS formulation and mannitol, was characterized by particle size analysis, scanning electron microscopy, differential scanning calorimetry, and X-ray powder diffraction. Finally, the solubility of the OA-loaded S-SEDDS was compared with that of OA powder in the dissolution assay. Our new S-SEDDS for OA was developed from the optimum L-SEDDS with ethyl oleate (oil phase), Labrasol (surfactant), and Transcutol P (cosurfactant) at a volume ratio of 15:71:14 with 1.5% w/v OA and mannitol. The dissolution of OA was improved by 60% compared with that of the pure OA powder. All the problems associated with the L-SEDDS were resolved. The methodologies we developed for OA delivery could also be utilized for the delivery of other drugs with the S-SEDDS.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemistry, Pharmaceutical*
  • Dosage Forms
  • Drug Compounding
  • Drug Delivery Systems*
  • Ethylene Glycols / chemistry
  • Excipients
  • Glycerides
  • In Vitro Techniques
  • Lipids / chemistry*
  • Mannitol
  • Oleanolic Acid / chemistry
  • Organic Chemicals / chemistry
  • Particle Size
  • Powders
  • Solubility
  • Surface-Active Agents

Substances

  • Dosage Forms
  • Ethylene Glycols
  • Excipients
  • Glycerides
  • Lipids
  • Organic Chemicals
  • Powders
  • Surface-Active Agents
  • Labrasol
  • Mannitol
  • Oleanolic Acid
  • carbitol