Improving oral absorption of Salmon calcitonin by trimyristin lipid nanoparticles

J Biomed Nanotechnol. 2009 Feb;5(1):76-83. doi: 10.1166/jbn.2009.443.

Abstract

Solid lipid nanoparticles (SLN) composed of trimyristin (solid lipid) and poloxamer 407 (surfactant) were prepared by a w/o/w emulsion technique for the incorporation of Salmon calcitonin, and further explored as protein carriers for oral delivery. Trimyristin SLN showed a mean size diameter of 200 nm with an association efficiency for calcitonin of approx. 86%. The morphology of SLN was investigated by cryo-SEM and by AFM, revealing spheroid shape SLN with a smooth surface. The in vitro release of calcitonin occurred for a period of 8 h, under both gastric and intestinal simulated pH conditions, predicting suitable properties for oral administration. The pharmacological activity of the protein was evaluated following oral dosage of calcitonin-loaded SLN in rats. SLN lowered the basal blood calcium levels by up to 20% with 500 IU/kg dose sustaining hypocalcaemia over 8 h. The results indicate that incorporation of Salmon calcitonin into trimyristin SLN is a key factor for the improvement of the efficiency of such carriers for oral delivery of proteins.

MeSH terms

  • Absorption
  • Administration, Oral
  • Animals
  • Calcitonin / administration & dosage*
  • Calcitonin / chemistry
  • Calcitonin / pharmacokinetics*
  • Crystallization / methods
  • Lipids / chemistry*
  • Macromolecular Substances / chemistry
  • Male
  • Materials Testing
  • Molecular Conformation
  • Nanomedicine / methods*
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Particle Size
  • Rats
  • Rats, Wistar
  • Salmon / metabolism*
  • Surface Properties
  • Triglycerides / chemistry*

Substances

  • Lipids
  • Macromolecular Substances
  • Triglycerides
  • trimyristin
  • Calcitonin