Abstract

Background: Delivering plant extract at high loading with intact antioxidants and efficient skin permeation always remains a challenge. To address this, we prepared a stable gel formulation containing nanoethosomes loaded with Achillea millefolium L. (AM) extract for topical drug delivery. Method: The AM extract was tested at first for phytochemical analysis, antioxidant activity, total phenolic and flavonoid content, and FTIR examination. The nanoethosomes containing AM extract were synthesized and characterized by size, surface charge, and morphology, and entrapment efficiency (EE) was determined. The optimized nanoethosomes were then incorporated to develop a topical gel formulation and subjected to skin for permeation, pH, viscosity, and organoleptic evaluation for up to three months. Results: The AM ethanolic extract demonstrated 88% free radical scavenging activity and notable phenolic and flavonoid contents of up to 123 mg GAE/g and 42 mg QE/g, respectively. The optimized nanoethosomes encapsulated with AM extract (240 nm) were spherical in shape, with −31.1 mV of surface charge, and showed considerable entrapment efficiency (90%). Furthermore, the selected topical gel remained stable during the study period. The Exvivo permeation study of ethosomal gel showed the highest release percentage of 79.8%. Conclusion: The study concludes that topical gel loaded with nanoethosomes containing AM extract is an encouraging approach for topical drug delivery.

Highlights

  • It is well known that cardiovascular diseases, cancer, and neurodegenerative diseases, especially the aging process are due to the production of free radicals

  • The free radical scavenging activity of extract of Achillea millefolium L. antenna parts was determined by using the determined by 2diphenyl-1-picryl-hydrazyl (DPPH) method

  • All other metabolites of Achillea millefolium L. (AM) extract were identified in the study conducted by using the method adopted by Souza et al, in 2006 (Souza et al, 2006)

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Summary

Introduction

It is well known that cardiovascular diseases, cancer, and neurodegenerative diseases, especially the aging process are due to the production of free radicals. Because antioxidants are capable of neutralizing these free radicals, there is a need to discover new sources of them (Ratnam et al, 2006). Various medicinal plants have been investigated for their antioxidant activity. In this case, the natural antioxidants both in extract form or chemical constituents could be employed to avoid free radical associated oxidative stress (Saeed et al, 2012). Flavonoids are recognized for their free radical. The position of the substituents affects the physiological roles of different flavonoids. Flavonols from the ortho or para hydroxyl group within the two- phenyl rings have sturdy antioxidant residences, and unfastened hydroxyl on the 5,7-positions was proven to have a seasoned-oxidant impact (Eghdami and Sadeghi, 2010). Delivering plant extract at high loading with intact antioxidants and efficient skin permeation always remains a challenge.

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