Abstract
Objective: To design topical Quercetin (Qc)-loaded transfersomes (TFs) for wound treatment. Methods: Qc-loaded TFs were prepared by thin-film hydration technique using 2241full factorial design and the optimum formula was selected. In vivo skin, deposition and cutaneous wound induction studies were performed for four groups of male wistar rats. At the end of the experiment, biochemical parameters were measured in the healed tissues (total proteins (TP), total antioxidant capacity (TAC), glutathione reductase (GSH), nitric oxide (NO), and malonaldehyde (MDA). Two in vivo histopathological experiments using male wistar rats were performed; the first study was done for the healed tissues of the above experiment and the second was to confirm the safety of formulations. Results: Qc optimum TFs (F6) showed EE% of 91.1%, PS of 695.35 nm, PDI of 0.592, and ZP of-11.1 mV, and spherical shape. In vivo skin deposition study showed that drug percentage retained in the skin from Qc optimum TFs was significantly higher than that from Qc suspension and Qc liposomes (p<0.05). There was no significant difference in the values of TP, TAC and MDA between the treated groups (p>0.05). GSH in TFs treated groups was significantly higher than the other groups (p<0.05) while NO in TFs treated groups was significantly lower than the other treated groups (p<0.05). Histopathological experiments showed that wounds treated by TFs healed better than those treated by both liposomes and Qc suspension. Conclusion: Qc-loaded TFs can be used as successful drug-delivery system for wound healing.
Highlights
Herbal drugs have been used in many diseases [1]
Transfersomes (TFs) are elastic nano-vesicles composed of lecithin and surface-active agent and they differ from the conventional liposomes by their ability to squeeze themselves into the intercellular region of the stratum corneum [16, 17]
ANOVA results showed that only type of surface-active agent and hydration volume had a significant effect on EE% (P
Summary
Herbal drugs have been used in many diseases [1]. Plant pigments which are found in herbal drugs as flavonoids which are found in fruits and vegetables, have many physiological activities [2]. Quercetin (Qc) has high antioxidant activity which reduces the expression of matrix metalloproteinase that causes wrinkling and decreasing of the elasticity of healthy and photoaged skin [6]. The topical application of Qc in various formulation approaches includes permeation enhancers [11] such as lecithin and chitosan nanoparticles [12] which increase the penetration of Qc through the skin to make its topical and transdermal delivery easier, targeting the drug towards the desired tissue and concentrating the drug in it while reducing its concentration in the non-target tissues. Surface-active agent vesicles are an alternative drug delivery system to conventional liposomes. Transfersomes (TFs) are elastic nano-vesicles composed of lecithin and surface-active agent and they differ from the conventional liposomes by their ability to squeeze themselves into the intercellular region of the stratum corneum [16, 17]
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