International Journal of Applied Pharmaceutics ISSN - 0975 - 7058 Vol 12, Special Issue 1, 2020 EFFECT OF TRANSFERSOME FORMULATION ON THE STABILITY AND ANTIOXIDANT ACTIVITY OF N-ACETYLCYSTEINE IN ANTI-AGING CREAM HARMITA HARMITA*, ISKANDARSYAH ISKANDARSYAH, SHOFIYAH FATIN AFIFAH Department of Pharmacy, Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia. Email: igakadeharmita@gmail.com Received: 26 September 2019, Revised and Accepted: 17 December 2019 ABSTRACT Objective: N-acetylcysteine is an antioxidant with thiol/sulfhydryl groups and is currently being developed as an active ingredient in anti-aging creams. The study’s aim was to compare the stability and antioxidant activity of N-acetylcysteine in anti-aging creams formulated with and without a transfersome carrier system. Methods: Stability was assessed by performing cycling, centrifugal, and accelerated stability tests. In addition, antioxidant activity was measured by the DPPH method, and in vitro penetration was measured using Franz diffusion cells. The analysis of N-acetylcysteine was performed using high- performance liquid chromatography with ultraviolet–visible detection at a wavelength of 214 nm and a flow rate of 1.0 mL/min, injection volume of 5 µL, and a mobile phase of phosphate buffer pH 3.0. Results: The N-acetylcysteine transfersome and non-transfersome cream preparations did not change color or show phase separation during the cycling and centrifugal tests. The N-acetylcysteine in the transfersome and non-transfersome cream preparations had strong antioxidant activity, with half-maximal inhibitory concentrations of 26.90 µg/mL and 38.63 µg/mL, respectively. The in vitro penetration test using Franz diffusion cells showed that the cumulative amount of penetrated N-acetylcysteine was 7355.13 µg/cm 2 (flux of 845.67 µg/cm 2 ∙h) in the transfersome cream and 4677.61 µg/cm 2 (flux of 533.33 µg/cm 2 ∙h) in the non-transfersome cream. Conclusion: The in vitro penetration test results showed that the transfersome formulations in creams were able to increase the cumulative amount and flux of penetrated N-acetylcysteine in anti-aging cream preparations relative to those not formulated with transfersome. Keywords: N-acetylcysteine, Transfersome, Anti-aging, Stability, Antioxidant, High-performance liquid chromatography. INTRODUCTION Signs of aging can be partly prevented and slowed using various methods, one of which is the application of cosmetics. Cosmetics that are currently widely used to mask or slow signs of aging of the skin are called anti-aging cosmetics. Anti-aging products on the market are available in various dosage forms, one of which is a cream. Creams are generally preferred as topical dosage forms because cream is easily applied and easily removed from the skin [1]. Anti-aging cream products available on the market generally use an antioxidant as the active ingredient. Antioxidants are simple molecules that can prevent cell damage caused by oxidation stimulated by other molecules [2]. An antioxidant that has recently been developed as an active ingredient in anti-aging creams is N-acetylcysteine. N-acetylcysteine is an antioxidant derived from the amino acid L-cysteine. N-acetylcysteine contains thiol/sulfhydryl (R-SH/-SH) groups, which are antioxidants [3]. N-acetylcysteine can prevent and/ or inhibit the oxidative process as measured by different biomarkers of oxidative stress [4]. N-acetylcysteine can act as a direct antioxidant and indirect antioxidant. The mechanism of direct antioxidation involves a free thiol group that can interact directly with electrons from reactive oxygen species. In addition, N-acetylcysteine also can act as an indirect antioxidant because it can undergo deacetylation to cysteine, which is an intracellular reduced glutathione precursor that can increase glutathione levels in the body [3,4]. N-acetylcysteine is not stable under oxidative conditions because it is easily oxidized when formulated. Stabilization strategies are needed to maintain the stability of N-acetylcysteine formulations for use as antioxidative anti-aging creams. One strategy to maintain the stability of N-acetylcysteine is to formulate it with a transfersome carrying system [5]. The study’s aim was to test the effects of transfersome systems on the stability and antioxidant activity of N-acetylcysteine in anti-aging formulations. MATERIALS AND METHODS Instrumentation The following instrumentation was used: High-performance liquid chromatography (HPLC) (Model LC-20AT; Shimadzu, Japan); rotary vacuum evaporator (Buchi, Switzerland); ultraviolet (UV)–visible spectrophotometer (Shimadzu UV-1601 and Jasco Climate Chamber; Nuve Sanayi Malzemeleri Imalat ve Tic. A.S., Turki); vortex mixer (Thermo Scientific, America); centrifuge (Hettich Centrifugen EBA 200); microcentrifuge (Thermo Fisher Scientific); sonicator (Branson 3200); particle size analyzer (Malvern Zetasizer, Inggris); oven (Memmert); refrigerator (GEA, Germany); and Franz diffusion cell. Materials N-acetylcysteine standard (Daebong LS Co. LTD., Korea Selatan); phosphatidylcholine (Merck, Germany); Tween 80 (Merck); potassium dihydrogen phosphate (Merck, Germany); phosphoric acid (Merck); sodium hydroxide (Merck); sodium metabisulfite (Merck); dichloromethane p.a (Merck); distilled water (Ikapharmindo Putramas); and methanol (Merck) were used. Preparation of mobile phase potassium dihydrogen phosphate pH 3.0 A 6.8 g amount of potassium dihydrogen phosphate was dissolved in 1000 mL of distilled water, adjusted with phosphoric acid to a pH 3.0, filtered, and degassed. © 2020 The Authors. Published by Innovare Academic Sciences Pvt Ltd. This is an open access article under the CC BY license (http://creativecommons. org/licenses/by/4. 0/) DOI: http://dx.doi.org/10.22159/ijap.2020.v12s1.FF034 The 4 th International Conference on Global Health 2019 Research Article