Title:A Novel Surfactant-free Lipid-based Formulation for Improving Oral Bioavailability of Loratadine Using Colloidal Silicon Dioxide as Emulsifier and Solid Carrier
Volume: 19
Issue: 3
Author(s): Ri Huang, Yonggang Tan, Lao Shen, Tao Wang and Dongqin Quan*
Affiliation:
- Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing,China
Keywords:
Lipid-based formulation, Loratadine, colloidal silicon dioxide, CSD, bioavailability, morphology.
Abstract: Background: The purpose of this study was to develop an innovative surfactant-free lipidbased
formulation (LF) for improving oral bioavailability of loratadine based on using solid particles
colloidal silicon dioxide (CSD) as emulsifier and solid carrier.
Methods: Loratadine was dissolved in oil solution with the aid of co-solvent and LF formulations were
prepared by a simple adsorption and milling technique. The LF Powder was evaluated in terms of angle
of repose and X-ray powder diffraction. After dispersing and emulsifying in water, the particle size
and morphology were also characterized. In vitro dissolution and pharmacokinetic behavior in vivo
were also studied.
Results: Orthogonal design indicated that the amount of CSD in formulations had a major and
significant influence on emulsification. The optimal formulation showed LF with good flowability and
without crystallization or deposition of loratadine in it.
Conclusion: After dispersing in water, an emulsion with the mean droplet size of 1.2μm was obtained.
Although the dissolution of drug from LF was slower in vitro in acidic aqueous solution, pharmacokinetic
studies in vivo showed that the bioavailability of loratadine increased 2.49-fold by CF compared
to a commercial tablet.