Salbutamol is a relatively selective beta-2-adrenoreceptor stimulant. After
parenteral administration, stimulation of the beta receptors in the body, both beta-1
and beta-2, occurs because (a) beta-2 selectivity is not absolute, and (b) higher
concentrations of salbutamol occur in the regions of these receptors with parentral
mode of administration. This results in the beta-1 effect of cardiac stimulation, and
beta-2 effects of peripheral vasodilatation and hypotension, skeletal muscle tremor
and uterine muscle relaxation.
In order to reduce the uptake of salbutamol by beta-1 receptor and to increase the
drug concentration in lungs with minimum dose through niosomes was tried in this
study to formulate and optimize Salbutamol Sulphate niosomes for targeting lungs to reduce the dose level and dosing frequency of Salbutamol Sulphate by
sustained release niosome formulation. To determine the stability of Salbutamol Sulphate niosome formulation with
and without stabilizing agent on storage. To determine the stability of salbutamol sulphate niosomes as per ICH
guidelines. To compare the bio-distribution nature of niosomal formulation and drug in
solution to different organs in mice when administered via intravenous route. To evaluate the altered pharmacokinetics and metabolism of Salbutamol
Sulphate niosomal formulation in rabbits.
Stable noisome formulation were prepared by thin film hydration technique
using Tween 20, 40, 60, 80 and Span 20, 40, 60, 80 in the ratio of 20:90
(cholesterol:surfactant). Drug entrapment was found to be high in Span 60 and Tween
60 formulations. Good in vitro release was found to be in Tween 80+CHOL and Span
60+DCP+CHOL formulations. Tween 80 formulation shows three fold increased drug
concentration in lungs and found to have higher plasma concentration as well as mean
residence time