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Sodium alginate microspheres of metoprolol tartrate for intranasal systemic delivery: development and evaluation.

Abstract
Bioadhesive sodium alginate microspheres of Metoprolol tartrate (MT) for intranasal systemic delivery were prepared to avoid the first-pass effect, as an alternative therapy to injection, and to obtain improved therapeutic efficacy in the treatment of hypertension and angina pectoris. The microspheres (Ms) were prepared using emulsification--cross-linking method. The formulation variables were drug loading, polymer concentration, cross-linking agent concentration, and cross-linking time. The Ms were evaluated for characteristics, like particle size, incorporation efficiency, swelling ability, in vitro bioadhesion, in vitro drug release, and in vivo pharmacodynamic performance in rabbits against isoprenaline-induced tachycardia. Treatment of in vitro data to different kinetic equations indicated matrix-diffusion controlled drug delivery from sodium alginate Ms. Polymer concentration, cross-linking agent concentration, and cross-linking time influenced the drug release profiles significantly. In vivo studies indicated significantly improved therapeutic efficacy of MT from Ms with sustained and controlled inhibition of isoprenaline-induced tachycardia as compared with oral and nasal administration of drug solution.
AuthorsP S Rajinikanth, C Sankar, B Mishra
JournalDrug delivery (Drug Deliv) 2003 Jan-Mar Vol. 10 Issue 1 Pg. 21-8 ISSN: 1071-7544 [Print] England
PMID12554360 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Alginates
  • Hexuronic Acids
  • Glucuronic Acid
  • Metoprolol
Topics
  • Administration, Intranasal
  • Alginates (administration & dosage, pharmacokinetics)
  • Animals
  • Drug Delivery Systems (methods)
  • Drug Evaluation, Preclinical (methods)
  • Female
  • Glucuronic Acid
  • Heart Rate (drug effects, physiology)
  • Hexuronic Acids
  • Male
  • Metoprolol (administration & dosage, pharmacokinetics)
  • Microspheres
  • Rabbits
  • Technology, Pharmaceutical (methods)

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