Formulasi Etosom Ekstrak Etanol Daun Tekelan (Chromolaena odorata L.) dan Karakterisasi Fisik, Uji Stabilitas Fisik, Penetrasi serta Aktivitas Antipenuaan Kulit secara In Vivo

Abstract

Ethanol extract of tekelan leaves (Chromolaena ododrata L.) has secondary metabolites in the form of tannins, phenols, flavonoids, saponins, alkaloids, steroids and essential oils such as α-pinene, cadinene, champora, limonene, β-caryophyllene and cadinol isomers. Specific flavonoid compounds found in tekelan leaf extract are quercetin compounds. Quercetin compounds are antioxidants that can prevent aging of the skin. One of the extrinsic factors causing aging is excessive ultraviolet irradiation. Quercetin compounds have low solubility in water, so the penetration properties are low if formulated in topical dosage forms. Therefore, a formula in small particle size, namely ethosome preparation, was developed that can improve the problem of its penetration properties. The purpose of this study is the formulation of ethosomal preparations from ethanol extract of tekelan leaves along with characterization and evaluation of preparations and the effectiveness of skin anti-aging in vivo. The methods carried out in this study were identification of quercetin compounds by Clt-preparative, antioxidant test of DPPH free radical scavenging method, determination of IC50 value and total flavonoids, formulation and characterisation of four ethosomal preparation formulas (F1-without extract, F2-extract 0.5 g in 10 mL ethanol, F3-extract 1 g in 20 mL ethanol, F4-extract 1.5 g in 30 mL ethanol) compared with their liposomal preparations (100 mg extract in 10 mL PBS saline). Further characterisation of the preparation (organoleptic, particle size, zeta potential and TEM) was carried out. Physical stability test was conducted for 12 weeks storage, viscosity, absorption efficiency, penetration on rabbit skin by Franz diffusion method, in vivo irritation test on rabbit skin, anti-aging activity on rat skin irradiated with UV-B light and compared with liposome preparation and histopathological profile. The results obtained are quercetin compounds in the ethanol extract of tekelan leaves with an Rf value of 0.46 (orange color), IC50 value of 31.145 mcg/mL, the highest total flavonoids are found in F4 (228.971 mgEQ/g). All formulas are still in nanometer size and F4 has the smallest particle size (102,87±0,59 nm). The result of sorption efficiency was 68.44%, cumulative amount at 480th minute (1120.20±815.05 mcg/cm2), %cumulative (38.82±0.45%), flux value (23.01±1.732 μg.cm-2h-1). The ethosome preparation did not show any irritation on rabbit skin. The macroscopic anti-aging test results from each irradiated group showed that the skin pigment was irregular, the skin became pale, telangiectasis of small and dilated blood vessels), solar elastosis (thickened skin due to abnormal elastin accumulation). While microscopically showed that the epidermal layer was thinned and collagen density was less. Meanwhile, the group treated with tekelan leaf extract ethosomes experienced improvements in macroscopic structure. While the microscopic structure of the epidermis began to appear clearly and collagen density increased. The conclusion of this study is that all ethosome preparations meet the requirements of the physical characteristics of ethosomes and F4 (1.5 g extract in 30 mL ethanol) is the formula that has the best anti-aging effectiveness.