Design and evaluation of polysaccharide-based transdermal films for the controlled delivery of nifedipine

Chem Pharm Bull (Tokyo). 2014;62(2):144-52. doi: 10.1248/cpb.c13-00579.

Abstract

It was aimed to develop the matrix type polysaccharide-based transdermal films of nifedipine (NFD) to provide its long term plasma concentration. The mechanical tests were carried out on gel formulations which were utilised in the fabrication of transdermal films to determine the type of polymer (pectin, sodium alginate) and plasticizer (propylene glycol, glycerine) as well as their concentrations. The mechanical strength, elasticity, bioadhesiveness and the drug release characteristics of optimised films containing NFD were evaluated. Permeation of NFD from the films with/without adding an enhancer (nerolidol) was followed through excised rat skin using Franz diffusion cells. Results showed that the gels composed of either pectin or sodium alginate were appropriate for the fabrication of transdermal films of NFD, and the addition of propylene glycol improved mechanical strength, flexibility, and bioadhesiveness of the films. Permeation data showed that nerolidol was an effective permeation enhancer for the polysaccharide-based transdermal films of NFD.

MeSH terms

  • Adhesiveness
  • Administration, Cutaneous
  • Alginates / chemistry*
  • Animals
  • Calcium Channel Blockers / administration & dosage*
  • Calcium Channel Blockers / pharmacokinetics
  • Delayed-Action Preparations / chemistry*
  • Elasticity
  • Female
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Nifedipine / administration & dosage*
  • Nifedipine / pharmacokinetics
  • Pectins / chemistry*
  • Rats
  • Rats, Wistar
  • Sesquiterpenes / chemistry
  • Skin / metabolism
  • Skin Absorption*
  • Transdermal Patch*
  • Vasodilator Agents / administration & dosage
  • Vasodilator Agents / pharmacokinetics

Substances

  • Alginates
  • Calcium Channel Blockers
  • Delayed-Action Preparations
  • Hexuronic Acids
  • Sesquiterpenes
  • Vasodilator Agents
  • Pectins
  • Glucuronic Acid
  • Nifedipine
  • nerolidol