Comparison of solid self-microemulsifying drug delivery system (solid SMEDDS) prepared with hydrophilic and hydrophobic solid carrier

• Published in: International journal of pharmaceutics 2011-11, Vol.420 (2), p.412-418
• Main Authors: Oh, Dong Hoon, Kang, Jun Hyeok, Kim, Dong Wuk, Lee, Beom-Jin, Kim, Jong Oh, Yong, Chul Soon, Choi, Han-Gon
• Format: Article
• Language: English
• Subjects: Animals; Bioavailability; Calorimetry, Differential Scanning; Colloidal silica; Crystalline property; Dextran; Dextrans - chemistry; Dextrans - pharmacokinetics; Dissolution; droplet size; Drug Carriers - chemistry; Drug Carriers - pharmacokinetics; Drug delivery; drugs; Emulsions; Ethylene Glycols - chemistry; Ethylene Glycols - pharmacokinetics; Flurbiprofen; Flurbiprofen - blood; Flurbiprofen - chemistry; Flurbiprofen - pharmacokinetics; Glycerides - chemistry; Glycerides - pharmacokinetics; hydrophilicity; Hydrophobic and Hydrophilic Interactions; Hydrophobicity; Male; microcapsules; Microscopy, Electron, Scanning; Oral bioavailability; Organic Chemicals - chemistry; Organic Chemicals - pharmacokinetics; Particle Size; Polyethylene Glycols - chemistry; Polyethylene Glycols - pharmacokinetics; Rats; Rats, Sprague-Dawley; Silica; Silicon Dioxide - chemistry; Silicon Dioxide - pharmacokinetics; Solid self-emulsifying drug delivery system; Solubility; spray drying; Surface Properties; Surface-Active Agents - chemistry; Surface-Active Agents - pharmacokinetics; X-Ray Diffraction
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2011.09.007

In order to compare the effects of hydrophilic and hydrophobic solid carrier on the formation of solid self-microemulsifying drug delivery system (SMEDDS), two solid SMEDDS formulations were prepared by spray-drying the solutions containing liquid SMEDDS and solid carriers. Colloidal silica and dextran were used as a hydrophobic and a hydrophilic carrier, respectively. The liquid SMEDDS, composed of Labrafil M 1944 CS/Labrasol/Trasncutol HP (12.5/80/7.5%) with 2% w/v flurbiprofen, gave a z-average diameter of about 100 nm. Colloidal silica produced an excellent conventional solid SMEDDS in which the liquid SMEDDS was absorbed onto its surfaces. It gave a microemulsion droplet size similar to that of the liquid SMEDDS (about 100 nm) which was smaller than the other solid SMEDDS formulation. In the solid SMEDDS prepared with dextran, liquid SMEDDS was not absorbed onto the surfaces of carrier but formed a kind of nano-sized microcapsule with carrier. However, the drug was in an amorphous state in two solid SMEDDS formulations. Similarly, they greatly improved the dissolution rate and oral bioavailability of flurbiprofen in rats due to the fast spontaneous emulsion formation and the decreased droplet size. Thus, except appearance, hydrophilic carrier (dextran) and hydrophobic carrier (colloidal silica) hardly affected the formation of solid SMEDDS such as crystalline properties, dissolution and oral bioavailability.