TY - JOUR

T1 - Development of phytocosmeceutical microemulgel containing flaxseed extract and its in vitro and in vivo characterization

AU - Tasneem, Rabia

AU - Khan, Haji Muhammad Shoaib

AU - Rasool, Fatima

AU - Khan, Kashif-ur-Rehman

AU - Umair, Muhammad

AU - Esatbeyoglu, Tuba

AU - Korma, Sameh A.

N1 - Funding Information: The publication of this article was funded by the Open Access Fund of Leibniz Universität Hannover.

PY - 2022/8/9

Y1 - 2022/8/9

N2 - Antioxidants from natural sources are extensively attaining consideration to avert the skin from damage and aging caused by free radicals. Flaxseed (Linum usitatissimum L.), a natural therapeutic agent, was meant to be explored cosmeceutical by quantifying its potential phytoconstituents and to be incorporated into a microemulgel for topical use. Hydroalcoholic fractions (both methanolic and ethanolic; 80%) flaxseed extracts were subjected to phytochemical screening by quantifying total phenolic content (TPC), total flavonoid content (TFC), and high-performance liquid chromatography-ultraviolet (HPLC-UV), and for biological activities through 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, tyrosinase inhibition assay, and sun protection factor (SPF). Ethanolic fraction was selected for further study by TPC (18.75 mg gallic acid equivalent/g) and TFC (1.34 mg quercetin equivalent/g). HPLC-UV analysis showed the existence of benzoic, quercetin, caffeic, vanillic, p-coumaric, gallic, cinnamic, syringic, and sinapic acids. Biological activities showed 87.00%, 72.00%, and 21.75 values for DPPH assay, tyrosinase inhibition, and SPF assays, respectively. An oil-in-water (OW) microemulsion containing the flaxseed extract, with 99.20 nm Zeta size, −19.3 Zeta potential and 0.434 polydispersity index was developed and incorporated in Carbopol-940 gel matrix to formulate an active microemulgel with 59.15% release in in vitro studies. The successfully formulated stable active microemulgel produced statistically significant effects (p < 0.05), in comparison to a placebo, on skin erythema, melanin, sebum, moisture, and elasticity, in a noninvasive in vivo study performed on 13 healthy human female volunteers. Other cosmeceutical products can also be formulated from flaxseed, making it a considerable candidate for further utilization in the pharmaceutical industry.

AB - Antioxidants from natural sources are extensively attaining consideration to avert the skin from damage and aging caused by free radicals. Flaxseed (Linum usitatissimum L.), a natural therapeutic agent, was meant to be explored cosmeceutical by quantifying its potential phytoconstituents and to be incorporated into a microemulgel for topical use. Hydroalcoholic fractions (both methanolic and ethanolic; 80%) flaxseed extracts were subjected to phytochemical screening by quantifying total phenolic content (TPC), total flavonoid content (TFC), and high-performance liquid chromatography-ultraviolet (HPLC-UV), and for biological activities through 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, tyrosinase inhibition assay, and sun protection factor (SPF). Ethanolic fraction was selected for further study by TPC (18.75 mg gallic acid equivalent/g) and TFC (1.34 mg quercetin equivalent/g). HPLC-UV analysis showed the existence of benzoic, quercetin, caffeic, vanillic, p-coumaric, gallic, cinnamic, syringic, and sinapic acids. Biological activities showed 87.00%, 72.00%, and 21.75 values for DPPH assay, tyrosinase inhibition, and SPF assays, respectively. An oil-in-water (OW) microemulsion containing the flaxseed extract, with 99.20 nm Zeta size, −19.3 Zeta potential and 0.434 polydispersity index was developed and incorporated in Carbopol-940 gel matrix to formulate an active microemulgel with 59.15% release in in vitro studies. The successfully formulated stable active microemulgel produced statistically significant effects (p < 0.05), in comparison to a placebo, on skin erythema, melanin, sebum, moisture, and elasticity, in a noninvasive in vivo study performed on 13 healthy human female volunteers. Other cosmeceutical products can also be formulated from flaxseed, making it a considerable candidate for further utilization in the pharmaceutical industry.

KW - antioxidant

KW - cosmetic

KW - formulation development

KW - HPLC-UV

KW - in vivo study

KW - Linum usitatissimum

KW - pharmaceutic

KW - phytocosmetics

KW - radical scavenging activity

KW - topical

UR - http://www.scopus.com/inward/record.url?scp=85137580371&partnerID=8YFLogxK

U2 - 10.3390/pharmaceutics14081656

DO - 10.3390/pharmaceutics14081656

M3 - Article

VL - 14

JO - Pharmaceutics

JF - Pharmaceutics

IS - 8

M1 - 1656

ER -