Formulation and <i>in Vitro</i> Characterization of a Novel Solid Lipid-Based Drug Delivery System

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.

Self-Emulsifying Granules and Pellets: Composition and Formation Mechanisms for Instant or Controlled Release

“…Consequently, S-SEDDS combine the benefits of liquid SEDDS, e.g., enhanced solubility and bioavailability, with those of solid dosage forms, e.g., easy handling and administration, better patient compliance, high stability and reproducibility, faster and easier production and hence lower production cost). More specifically, they offer the following advantages: They reduce the risk of interaction of the ingredients of SEDDS with the capsule shell, thus offering stability improvement due to reduced risk of chemical degradation and microbial growth implying increased product shelf life [ 26 , 27 ]. They can be administered as immediate or controlled release formulations depending on the choice of the powder excipient, with which the SEDDS liquid is formulated.…”

“…They reduce the risk of interaction of the ingredients of SEDDS with the capsule shell, thus offering stability improvement due to reduced risk of chemical degradation and microbial growth implying increased product shelf life [ 26 , 27 ].…”

Preparation and Characterization of Ticagrelor Solid Self nano-emulsion

“…1-Liquid component in SNEDDS may interact with capsule shell , thus by solidifying the dosage form, the stability will increase and also the shelf life (8,9).…”