Preparation of a Novel Form of Gelatin With a Three-Dimensional Ordered Macroporous Structure to Regulate the Release of Poorly Water-Soluble Drugs

J Pharm Sci. 2016 Sep;105(9):2940-2948. doi: 10.1016/j.xphs.2015.12.026. Epub 2016 Feb 20.

Abstract

In this study, a novel three-dimensional ordered macroporous gelatin (3DOMG) was fabricated as a carrier for increasing the solubility of poorly water-soluble drugs, offering sustained release and a high oral bioavailability. Polymethyl methacrylate nanospheres (257 nm) were used as a colloidal plastic framework to synthesize 3DOMG. Fenofibrate (FNB) was selected as a model drug and loaded onto 3DOMG by the adsorption equilibrium method. Detailed characterization showed that the FNB absorbed onto 3DOMG was in a microcrystalline state. A fluorescence experiment and the prepared drug microcrystal network gave further information on the physical state of the drug. A degradation experiment proved that 3DOMG was readily biodegradable. In vitro release testing showed that 3DOMG increased the dissolution rate of FNB and produced a sustained release. An in vivo pharmacokinetic study confirmed that 3DOMG improved the oral bioavailability compared with that of commercial sustained-release capsules. These findings confirm that 3DOMG can be regarded as a promising carrier for an oral drug delivery system.

Keywords: bioavailability; biodegradability; biomaterials; fenofibrate; gelatin; materials science; nanotechnology; polymeric drug carrier; sustained release; three-dimensional ordered macroporous.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biological Availability
  • Calorimetry, Differential Scanning
  • Capsules
  • Chemistry, Pharmaceutical
  • Colloids
  • Delayed-Action Preparations
  • Excipients / administration & dosage
  • Excipients / chemistry*
  • Fenofibrate / administration & dosage
  • Fenofibrate / chemistry
  • Fenofibrate / pharmacokinetics
  • Gelatin / administration & dosage
  • Gelatin / chemistry*
  • Nanospheres
  • Particle Size
  • Polymethyl Methacrylate
  • Porosity
  • Rabbits
  • Solubility

Substances

  • Capsules
  • Colloids
  • Delayed-Action Preparations
  • Excipients
  • Gelatin
  • Polymethyl Methacrylate
  • Fenofibrate