Inorganic-polymer nanohybrid carrier for delivery of a poorly-soluble drug, ursodeoxycholic acid

Int J Pharm. 2010 Dec 15;402(1-2):117-22. doi: 10.1016/j.ijpharm.2010.09.039. Epub 2010 Oct 7.

Abstract

Delivery of poorly soluble drugs has been problematic due to its low absorption profile and bioavailability. In this work, ursodeoxycholic acid (UDCA), a poorly-soluble drug, was intercalated into inorganic nanovehicle, layered double hydroxides (LDHs), with a molecular level to enhance its solubility in biological fluid. The UDCA-loaded nanovehicle (i.e., UDCA-LDHs) was also coated with an anionic polymer, Eudragit(®) S100, to increase the dissolution rate of UDCA. According to the powder X-ray diffraction (PXRD) patterns of UDCA-LDHs, the gallery height of LDHs was expanded from 3.6Å to 28.3Å, indicating that the UDCA molecules were successfully intercalated into the interlayer space of LDHs. Fourier transform infrared (FT-IR) spectra also revealed that the UDCA molecules were well stabilized in the LDHs through electrostatic interaction. The in vitro dissolution test in a simulated biological fluid (pH=6.8) showed that the total dissolved fraction of UDCA for the first 2h was about 60.2% for the Eudragit(®) S100 coated UDCA-LDHs, which was a dramatic increase as compared with 19.0% dissolution from intact UDCA. It is, therefore, concluded that LDHs nanovehicle coated with an anionic polymer is a promising delivery system for improving aqueous solubility of poorly soluble drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cholagogues and Choleretics / administration & dosage*
  • Cholagogues and Choleretics / chemistry
  • Drug Carriers / chemistry*
  • Drug Stability
  • Excipients / chemistry
  • Hydroxides / chemistry*
  • Polymethacrylic Acids / chemistry*
  • Powder Diffraction / methods
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • Static Electricity
  • Time Factors
  • Ursodeoxycholic Acid / administration & dosage*
  • Ursodeoxycholic Acid / chemistry
  • X-Ray Diffraction / methods

Substances

  • Cholagogues and Choleretics
  • Drug Carriers
  • Excipients
  • Hydroxides
  • Polymethacrylic Acids
  • methylmethacrylate-methacrylic acid copolymer
  • Ursodeoxycholic Acid