Ferulic acid is an organic acid isolated from Asafoetida in 1866 and is a derivative of cinnamic acid. Ferulic acid is one of the phenolic acids that are widely found in plants and can bind to polysaccharides and proteins in the cell wall to form the cell wall skeleton. Research shows that ferulic acid has very good antioxidant activity and is a potent scavenger of hydrogen peroxide, superoxide free radicals, hydroxyl free radicals and peroxynitrite, and can regulate physiological functions and inhibit the activity of free radicals related production enzymes, increases the activity of free radical scavenging enzymes. Ferulic acid is a fat-soluble antioxidant. Compared with vitamin E, ferulic acid is more effective in scavenging fat-soluble free radicals. Ferulic acid is an intercellular adhesive that can connect polysaccharides between cells in series, making the skin firm and elastic. In recent years, research on pharmacology and efficacy has found many pharmacological effects and biological activities of ferulic acid and its derivatives, and their toxicity is low. Therefore, they are widely used in medicine, health products, cosmetic raw materials and food additives. Studies have shown that ferulic acid has low toxicity and is easily metabolized by the human body, and its uses are becoming more and more extensive. Ferulic acid and its derivatives have been increasingly used in food, medicine, cosmetics and other industries.
Figure 1. Ferulic acid-loaded aspasomes.(Çiğdem Yücel, et al.; 2023)
Liposomes are microscopic vesicles formed by the encapsulation of compounds in a lipid bilayer. They were discovered by two British scientists in the 1950s. When amphiphilic molecules such as phospholipids and sphingolipids are dispersed in an aqueous phase, the hydrophobic tails of the molecules tend to cluster together and avoid the aqueous phase, while the hydrophilic heads are exposed to the aqueous phase, forming closed vesicles with a bilayer structure. Liposomes have the following properties 1. Improve the stability of encapsulated substances; After some unstable and easily oxidised compounds are made into liposomes, since the compounds are encapsulated in liposomes and protected by the lipid bilayer membrane, they can be protected from degradation by the body's enzyme system and immune system. This greatly improves the stability of the compound. 2. Reduce the toxicity of compounds; Changes to the surface properties of liposomes, such as particle size, surface charge, tissue-specific antibodies, etc., can improve the selectivity of compounds for target areas and reduce adverse reactions. 3. Long-lasting effect; Compounds are encapsulated in liposomes and can be slowly released, thereby prolonging the duration of action. 4. Good preparation properties; The liposome preparation process can encapsulate fat-soluble compounds and water-soluble compounds at the same time. The lipid materials used to prepare liposomes are less toxic, have good biocompatibility, and have no immune response. For food, liposomes, as protective carriers, can effectively protect nutrients such as vitamins, amino acids, and minerals in food, and effectively reduce the loss of nutrients during processing and storage. Since many vitamins and amino acids are easily oxidized and easily decomposed by light, they suffer great losses in food processing engineering, thus failing to achieve the purpose of nutrition. The results of the research test show that liposomes can effectively protect the activity of IgY, even in the environment of pepsin. At the same time, the sustained release effect of liposomes allows nutrients to be released slowly, which is more conducive to absorption.
Ferulic acid encapsulated by nanoliposomes integrates the advantages of ferulic acid and liposomes. a) Enhanced stability. Protected by the lipid bilayer membrane, it can be protected from degradation by the body's enzyme system and immune system, significantly improving the stability of the ingredients. It also has good heat, pH and shear stability and is easy to use. b) Improved bioavailability. Encapsulated by nano-sized liposomes, it is slowly released and easier to be absorbed, increasing bioavailability. c) It is both water-soluble and oil-soluble (amphiphilic), with a wide range of applications.
Alternate Names:
Liposome-encapsulated Ferulic Acid
Ferulic Acid Nanoliposomes
Nanoliposome-encapsulated Ferulic Acid
Nano-FA Liposomes
Nanoliposome Ferulate
References:
1. Çiğdem Yücel, et al.; Ferulic acid-loaded aspasomes: A new approach to enhance the skin permeation, anti-aging and antioxidant effects. Journal of Drug Delivery Science and Technology. 2023, Volume 86, 104748.
Preparation, characterization, and evaluation of liposomal ferulic acid in vitro and in vivo
Drug Dev Ind Pharm.
Authors: Qin J, Chen D, Lu W, Xu H, Yan C, Hu H, Chen B, Qiao M, Zhao X
Abstract
In the present study, various gradients were evaluated for efficient loading of weak acid into liposomes. Several salt gradients showed efficient loading of ferulic acid (FA) into liposomes and the optimized conditions were established in calcium acetate gradient method to obtain 80.2 +/- 5.2% entrapment efficiency (EE). Unilamellar vesicles were observed in micrographs and liposomal FA showed good stability. 80% of FA was released from liposomes within 5 h in vitro. There is a novel finding in this study: that drugs could be entrapped with a high solubility in the intraliposomal buffer in contrast to the low solubility in the extraliposomal buffer. The results of body distribution in rats indicated that liposomes could improve the body distribution of FA. For FA liposome, the concentration of FA in brain was two-fold higher than that of free FA. Liposomal FA was a promising approach to improve the body distribution of FA.
Skin delivery of ferulic acid from different vesicular systems
J Biomed Nanotechnol
Authors: Chen M, Liu X, Fahr A
Abstract
The aim of the present research is to evaluate the skin delivery capabilities of different vesicular systems, including conventional liposomes (CL), Tween 80-based deformable liposomes (DL), invasomes (INS) and ethosomes bearing ferulic acid (FA) being an antioxidant exhibiting a wide range of therapeutic effects against various diseases. All of the test formulations were characterized for particle size distribution, zeta-potential, vesicular shape and surface morphology, in vitro human skin permeation and skin deposition. Dynamic Light Scattering (DLS) and Transmission Electron Microscopy (TEM) defined that all of liposomal vesicles were almost spherical, displaying unilamellar structures with low polydispersity (PDI < 0.2) and nanometric size range (z-average no more than 150 nm). In addition, all the vesicular systems except conventional liposomes were negatively charged to a certain extent. In vitro skin permeation and skin deposition experiments demonstrated that the permeation profile of ferulic acid through human stratum corneum epidermis membrane (SCE) and the drug deposition in skin were both improved significantly using these vesicular liposomal systems. Permeation and skin deposition enhancing effect was highlighted by the ethosomal system containing 18.0 mg/ml of ferulic acid with an significantly (P < 0.01) enhanced skin flux (267.8 +/- 16.77 microg/cm2/h) and skin drug deposition (51.67 +/- 1.94 microg/cm2), which was 75 times and 7.3 times higher than those of ferulic acid from saturated PBS (pH 7.4) solution, respectively. This study demonstrated that ethosomes are promising vesicular carriers for delivering ferulic acid into or across the skin.
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