Drug Discov Ther. 2011;5(2):96-106. (DOI: 10.5582/ddt.2011.v5.2.96)

Development and characterization of local anti-inflammatory implantation for the controlled release of the hexane extract of the flower-heads of Euryops pectinatus L. (Cass.).

Nesseem DI, Michel CG


A hexane extract of the flower-heads of Euryops pectinatus L. (Cass.) was formulated into local anti-inflammatory implantation patches with controlled release. Cross-linked sodium hyaluronate patches (F1-F3) and chitosan patches (F4-F6) were prepared by a casting/solvent evaporation technique. Morphological and mechanical characterizations including the components ratio, surfactant and the loaded amount of the hexane extract (50, 100, and 200 mg/kg b.wt.) were investigated. Release studies were performed during 24 h using a diffusion cell. Films with optimum in vitro release rate have been investigated for testing the anti-inflammatory activity and the sustaining effect of the formulations. The sustained anti-inflammatory effect of the hexane extract of E. pectinatus flower-heads from the selected films was studied by inducing paw edema in rats with 1% (w/v) carrageenan solution. The results indicated the compatibility of hexane extract with both sodium hyaluronate and chitosan patches forming yellowish transparent films. Based on variations in drug release profiles throughout the 24-h among the formulations (F1-F6) studies, F3 and F6 were selected for further investigation. When the films were applied 1 h before the subplantar injection of carrageenan in the hind paw of male Albino rats, formulation (F3) provided its maximum inhibition of paw edema in rats (91.3%) 4 h after edema induction whereas, formulation (F6) showed less inhibition after 4 h (70.6%). The previous two formulations (F3 and F6) produced potent results (95.3 and 89.5%, respectively) after 24 h when compared with a local market preparation containing 25% β-sitosterol used as positive control. Histophathological investigation was conducted for 1, 4, and 12 weeks to study the tissue response for the two formulations (F3 and F6) at the implantation site. Chemical investigation of the hexane extract was achieved for both unsaponifiable matter (USM) and fatty acid methyl esters (FAME) using gas liquid chromatography (GLC). The USM was dominated by n-pentacosane (14.40%), phytosterols (Cholesterol, Campesterol, Stigmasterol, β-sitosterol, α-amyrin) reached 33.44% and the FAME was dominated by Linoleinic (49.97%). Quality control of the local implantation was evaluated by GLC using cholesterol as an analytical marker and phytosterols as an active marker compared to the plain extract.

KEYWORDS: Euryops pectinatus hexane extract, chemical investigation, local anti-inflammatory implantation, sodium hyaluronate, chitosan patches, in vitro release-in vivo study

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