Production of hybrid lipid-based particles loaded with inorganic nanoparticles and active compounds for prolonged topical release

Int J Pharm. 2009 Dec 1;382(1-2):296-304. doi: 10.1016/j.ijpharm.2009.08.033. Epub 2009 Aug 29.

Abstract

The production of particulate hybrid carriers containing a glyceryl monostearate (Lumulse GMS-K), a waxy triglyceride (Cutina HR), silanized TiO(2) and caffeine were investigated with the aim of producing sunscreens with UV-radiation protection properties. Particles were obtained using the supercritical PGSS (Particles from Gas Saturated Solutions) technique. This method takes advantages of the lower melting temperatures of the lipids obtained from the dissolution of CO(2) in the bulk mixture. Experiments were performed at 13 MPa and 345 K, according to previous melting point measurements. Blends containing Lumulse GMS-K and Cutina HR lipids (50 wt%) were loaded with silanized TiO(2) and caffeine in percentile proportions of 6 and 4 wt%, respectively. The particles produced were characterized using several analytical techniques as follows: system crystallinity was checked by X-ray diffraction and differential scanning calorimetry, thermal stability by thermogravimetric analysis, and morphology by scanning and transmission electron microscopy. Further, the UV-shielding ability of TiO(2) after its dispersion in the lipidic matrix was assessed by solid UV-vis spectroscopy. Preliminary results indicated that caffeine-loaded solid lipid particles presented a two-step dissolution profile, with an initial burst of 60 wt% of the loaded active agent. Lipid blends loaded with TiO(2) and caffeine encompassed the UV-filter behavior of TiO(2) and the photoaging prevention properties of caffeine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Caffeine / administration & dosage
  • Caffeine / chemistry*
  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Chromatography, Supercritical Fluid
  • Crystallization
  • Crystallography, X-Ray
  • Delayed-Action Preparations
  • Drug Carriers*
  • Drug Compounding
  • Glycerides / chemistry*
  • Kinetics
  • Microscopy, Electron, Scanning
  • Microscopy, Electron, Transmission
  • Nanoparticles*
  • Pressure
  • Solubility
  • Spectrophotometry, Ultraviolet
  • Sunscreening Agents / administration & dosage
  • Sunscreening Agents / chemistry*
  • Surface Properties
  • Technology, Pharmaceutical
  • Thermogravimetry
  • Titanium / administration & dosage
  • Titanium / chemistry*
  • Transition Temperature
  • Triglycerides / chemistry*
  • Waxes

Substances

  • Delayed-Action Preparations
  • Drug Carriers
  • Glycerides
  • Sunscreening Agents
  • Triglycerides
  • Waxes
  • titanium dioxide
  • glyceryl monostearate
  • Caffeine
  • Titanium