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Research Article

Development of a novel vesicular system using a binary mixture of sorbitan monostearate and polyethylene glycol fatty acid esters for rectal delivery of rutin

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Pages 28-36 | Received 07 May 2012, Accepted 30 Aug 2012, Published online: 19 Oct 2012
 

Abstract

Anorectal diseases, such as hemorrhoids, are bothersome benign conditions that warrant special attention. The design of an optimized vesicular system for localized rectal delivery can be a suitable conservative treatment. The feasibility of preparing proniosomes using different types of Gelucires®, in combination with Span® 60 as binary mixtures of nonionic surfactants, was checked, then the prepared proniosomes using Span 60 or Span 60/Gelucire were compared to conventional niosomes through investigations comprising the following: encapsulation efficiency (EE%); particle-size analysis; transmission electron microscopy; zeta potential (Z), and in vitro release study and ex vivo permeation study using excised rat rectum. All preparations showed satisfactory stability (Z >30 mV), particle size <300 nm with niosomes showing the lowest EE%, and the largest particle size, together with the least amount of drug released or accumulated in the rectal walls. Span 60/Gelucire proniosomes exhibited lower particle size as well as better release and permeation results, compared to Span 60 proniosomes. Span 60/Gelucire 44/14 (2:1) proniosomes attained the highest percentage of drug released (98.39%) and drug deposition in the rectal walls (86.26%) after 8 hours, which therefore seems to be the most suitable formula able to achieve targeted therapeutic efficacy, aiming to improve the patient’s quality of life.

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