A quadruped study on chitosan microspheres containing atorvastatin calcium: preparation, characterization, quantification and in-vivo application

Chem Pharm Bull (Tokyo). 2010 Sep;58(9):1161-7. doi: 10.1248/cpb.58.1161.

Abstract

Atorvastatin is commonly used as a cholesterol lowering agent in patients. Recently, the neuroprotective effects of atorvastatin became the focus of many research studies. In this study, we have formulated chitosan microspheres containing atorvastatin calcium. In-vitro characterization of chitosan microspheres and quantification of atorvastatin calcium from formulations were also evaluated. The neuroprotective efficiency of atorvastatin calcium was investigated by an experimental spinal cord injury model. Atorvastatin calcium microspheres were implanted at the laminectomy area (1 mg/kg) immediately after trauma. Twenty-four hours after injury, motor functions of animals were scored according to modified Tarlov Scale. In spinal cord tissues tumor necrosis factor (TNF)-alpha, interleukin (IL)-1beta, IL-6 and lipid peroxidation levels were quantified and ultrastructural changes have been investigated. The results of all parameters indicate that microspheres containing atorvastatin calcium were capable of improving functional outcome, attenuating the expression of TNF-alpha, IL-1beta and IL-6; lowering lipid peroxidation levels and maintaining the preservation of the cellular uniformity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticholesteremic Agents / administration & dosage*
  • Anticholesteremic Agents / therapeutic use*
  • Atorvastatin
  • Chitosan / chemistry
  • Heptanoic Acids / administration & dosage*
  • Heptanoic Acids / therapeutic use*
  • Interleukin-1beta / metabolism
  • Interleukin-6 / metabolism
  • Lipid Peroxidation / drug effects
  • Microspheres
  • Neuroprotective Agents / administration & dosage*
  • Neuroprotective Agents / therapeutic use*
  • Pyrroles / administration & dosage*
  • Pyrroles / therapeutic use*
  • Rats
  • Rats, Sprague-Dawley
  • Spinal Cord Injuries / drug therapy*
  • Spinal Cord Injuries / pathology
  • Tumor Necrosis Factor-alpha / metabolism
  • Wounds and Injuries / drug therapy
  • Wounds and Injuries / pathology

Substances

  • Anticholesteremic Agents
  • Heptanoic Acids
  • Interleukin-1beta
  • Interleukin-6
  • Neuroprotective Agents
  • Pyrroles
  • Tumor Necrosis Factor-alpha
  • Chitosan
  • Atorvastatin