Development of Lecithin Nanoemulsion Based Organogels for Permeation Enhancement of Metoprolol through Rat Skin

The human skin is a readily accessible area for drug delivery

J. Varshosaz

2013

Scholarcy highlights

  • The human skin is a readily accessible area for drug delivery
  • Transdermal drug delivery has some benefits: skipping first pass metabolism in liver, steady infusion of a drug over an extended period of time, better compliance of the patient due to ease of usage and reduced frequency of use, a choice for drugs with low therapeutic index and short half life, and so easy elimination of drug when toxicity occurs during the application
  • Lecithin 200, 100p were from Locus Meyer industry, Germany, lecithin 170 was from Degussa, Germany, n-butanol, isopropyl alcohol, n-propanol, potassium monohydrogen phosphate, NaOH, and sodium lauryl sulphate were from Merck Chemical Company, Germany, cellulose membrane from Biocin industry, Belgium, isopropyl myristate from Aldrich company, Germany, and metoprolol was from Alborz Darou, Iran, as a gift sample
  • Metoprolol is an antihypertensive drug with short half life which needs to be used, frequently; it goes under a high first pass metabolism so that its oral bioavailability is just 50%
  • This drug is a good candidate for transdermal delivery
  • The formulations containing more than 50% of lecithin and less than 30% could not be prepared, since more than 50% of lecithin could not be dissolved in isopropyl myristate, and when its concentration was less than 30% too much alcohol was needed to prepare the nanoemulsion
  • Phase diagrams seen in Figures 1–4 show the effect of lecithin type, alcohol type, drug content, and lecithin/isopropyl myristate ratio on the transparent region of nanoemulsions, respectively
  • Formulations containing 10% aqueous solution of metoprolol had higher drug release rate, and those containing lecithin 200 were preferred because of using less alcohol for elucidating the systems

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