Shahira F El-Menshawe1, Amal K Hussein. 1. Department of Pharmaceutics and Industrial Pharmacy, Beni Suef University, Beni Suef, Egypt. shahira.fawzy@gmail.com
Abstract
CONTEXT: Skin delivery of Meloxicam (MX) offers several advantages over the oral route which is associated with potential side effects. OBJECTIVES: The aim of this study was to develop transdermal MX in niosomes. MATERIALS AND METHODS: Vesicles prepared by thin film hydration method were characterized and the acute anti-inflammatory activity of 0.5% MX niosomal hydrogel was evaluated using carrageenan induced rat paw edema method. RESULTS: The results revealed that niosomes prepared from span 60 and cholesterol at 6:4 molar ratio using 20 mg of MX were of the highest entrapment efficiency (> 55%) and with particle size (187.3 nm). There was a marked increase in the percentage inhibition of edema in animals treated with MX vesicular gel compared to those treated with free MX and piroxicam gels. DISCUSSION: There was an inverse proportionality between vesicle size and cholesterol content. With increased cholesterol molar ratio the bilayer stability increased and permeability decreased leading to efficiently trapping the MX. In contrast, higher amounts of cholesterol may compete with the drug for packing space within the bilayer. The inhibitory effect of MX niosomal gel may be attributed to its superior skin permeation. CONCLUSIONS: The results suggest that niosomes may be promising vehicles for transdermal delivery of MX.
CONTEXT: Skin delivery of Meloxicam (MX) offers several advantages over the oral route which is associated with potential side effects. OBJECTIVES: The aim of this study was to develop transdermal MX in niosomes. MATERIALS AND METHODS: Vesicles prepared by thin film hydration method were characterized and the acute anti-inflammatory activity of 0.5% MX niosomal hydrogel was evaluated using carrageenan induced rat paw edema method. RESULTS: The results revealed that niosomes prepared from span 60 and cholesterol at 6:4 molar ratio using 20 mg of MX were of the highest entrapment efficiency (> 55%) and with particle size (187.3 nm). There was a marked increase in the percentage inhibition of edema in animals treated with MX vesicular gel compared to those treated with free MX and piroxicam gels. DISCUSSION: There was an inverse proportionality between vesicle size and cholesterol content. With increased cholesterol molar ratio the bilayer stability increased and permeability decreased leading to efficiently trapping the MX. In contrast, higher amounts of cholesterol may compete with the drug for packing space within the bilayer. The inhibitory effect of MX niosomal gel may be attributed to its superior skin permeation. CONCLUSIONS: The results suggest that niosomes may be promising vehicles for transdermal delivery of MX.
Authors: Irhan Ibrahim Abu Hashim; Noha Fawzy Abo El-Magd; Ahmed Ramadan El-Sheakh; Mohammed Fawzy Hamed; Abd El-Gawad Helmy Abd El-Gawad Journal: Int J Nanomedicine Date: 2018-02-20