Improving the topical delivery of zinc phthalocyanine using oleic acid as a penetration enhancer: in vitro permeation and retention

Drug Dev Ind Pharm. 2011 May;37(5):569-75. doi: 10.3109/03639045.2010.529144. Epub 2010 Dec 3.

Abstract

Topical photodynamic therapy with zinc phthalocyanine (ZnPc), second-generation photosensitizer, can be an alternative method for the treatment of skin cancer. However, ZnPc has poor penetration in the skin. This study was aimed at investigating whether the presence of oleic acid (chemical enhancer) in propylene glycol can improve the topical delivery of ZnPc. The topical (to the skin) and transdermal (across the skin) delivery of ZnPc were evaluated in vitro using suine ear skin mounted in Franz diffusion cell. Photosensitizer was quantified by fluorescence emission, which is a sensitive and selective method. At 5 and 10%, oleic acid increased the topical and transdermal delivery significantly. When the concentration of oleic acid was further increased (20-60% w/w), the topical delivery of ZnPc was still elevated, but its transdermal delivery was substantially reduced. It was concluded that oleic acid (in propylene glycol formulations) can promote the topical delivery of ZnPc, with reduced transdermal delivery. This approach can be effective for the treatment of skin cancer by topical photodynamic therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Administration, Topical
  • Animals
  • Chemistry, Pharmaceutical / methods
  • Drug Delivery Systems / methods*
  • Drug Stability
  • Ear, External / metabolism
  • Indoles / administration & dosage*
  • Indoles / chemistry*
  • Indoles / pharmacokinetics
  • Isoindoles
  • Oleic Acid / administration & dosage*
  • Oleic Acid / chemistry*
  • Oleic Acid / pharmacokinetics
  • Organometallic Compounds / administration & dosage*
  • Organometallic Compounds / chemistry*
  • Organometallic Compounds / pharmacokinetics
  • Permeability
  • Photochemotherapy / methods
  • Photosensitizing Agents / administration & dosage*
  • Photosensitizing Agents / chemistry*
  • Photosensitizing Agents / pharmacokinetics
  • Propylene Glycol / chemistry
  • Skin / drug effects
  • Skin / metabolism
  • Skin Neoplasms / drug therapy
  • Skin Neoplasms / metabolism
  • Swine
  • Zinc Compounds

Substances

  • Indoles
  • Isoindoles
  • Organometallic Compounds
  • Photosensitizing Agents
  • Zinc Compounds
  • Zn(II)-phthalocyanine
  • Oleic Acid
  • Propylene Glycol