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.

journal_name

Drug Deliv

journal_title

Drug delivery

authors

Rajinikanth PS,Sankar C,Mishra B

doi

10.1080/713840323

keywords:

subject

Has Abstract

pub_date

2003-01-01 00:00:00

pages

21-8

issue

1

eissn

1071-7544

issn

1521-0464

pii

7WL7827GE2FT7XLC

journal_volume

10

pub_type

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