Chlorogenic acid (CGA) is a polyphenolic compound found in various plant-based foods, particularly in coffee, fruits, and vegetables. It has gained attention due to its potential health benefits, including antioxidant and anti-inflammatory properties [1-3]. Despite the potential health benefits associated with chlorogenic acid, its bioavailability is relatively low. Several factors contribute to this limited utilization. Firstly, chlorogenic acid exhibits low water solubility, impeding its dissolution in the gastrointestinal tract. Consequently, its bioavailability is restricted, as the absorption of hydrophobic compounds such as chlorogenic acid often relies on their solubility in aqueous environments [3]. Furthermore, it should be noted that Chlorogenic acid exhibits sensitivity towards various factors including heat, light, and enzymatic activity. The exposure to these aforementioned elements has the potential to induce the degradation of chlorogenic acid, thereby diminishing its stability and bioavailability [4]. This susceptibility to degradation can manifest during the stages of food processing, storage, or even within the digestive environment. Moreover, even in cases where chlorogenic acid is successfully absorbed, its distribution to targeted tissues may be hindered. The compound must effectively reach specific sites within the body in order to exert its therapeutic effects, and the challenges associated with tissue distribution may contribute to its relatively low utilization rate.
To address the challenges associated with the low bioavailability of chlorogenic acid, researchers have developed various of nanocarriers, such as micelles, liposomes, or nanoparticles, to promote its dissolution in aqueous environments and facilitate its absorption in the gastrointestinal tract, finally improving its application in biomedical field [5,6]. These nanocarriers also act as protective shields, preventing the direct exposure of chlorogenic acid to environmental factors, which could maintain the stability of chlorogenic acid during storage and transportation, ensuring its bioavailability upon administration [7,8]. The nanocarriers can be designed to provide controlled and sustained release of chlorogenic acid [9]. This controlled release profile can extend the time that chlorogenic acid is available for absorption in the gastrointestinal tract. A controlled release also contributes to a prolonged therapeutic effect, reducing the need for frequent dosing. By enhancing the targeted delivery and controlled release of chlorogenic acid, nanocarriers may help reduce side effects associated with systemic exposure. This is particularly relevant when aiming to concentrate the therapeutic effects of chlorogenic acid at specific sites while minimizing its impact on healthy tissues.
In summary, nanocarriers provide a versatile and effective platform for improving the bioavailability of chlorogenic acid, addressing challenges associated with its natural properties. These advantages make nanocarrier-mediated delivery an attractive strategy for enhancing the therapeutic potential of chlorogenic acid in various applications, from pharmaceuticals to functional foods. However, how to fine-tune the formulation of nanocarriers to achieve optimal properties such as particle size, surface charge, and stability, ultimately improving the overall effectiveness of chlorogenic acid delivery, remains an urgent issue. Additionally, understanding the biodistribution and clearance of nanocarriers in vivo is critical for predicting their efficacy and potential long-term effects. The fate of nanocarriers after administration, including whether they accumulate in specific organs or are efficiently cleared from the body, remains an area of active research. Addressing these disadvantages and unresolved issues will be crucial for harnessing the full potential of nanocarriers in grafting chlorogenic acid and ensuring the development of safe and effective therapeutic strategies.
References
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- Li H, Xu J, Hu JF, et al. (2022). Sustained release of chlorogenic acid-loaded nanomicelles alleviates bone loss in mouse periodontitis. Biomaterials science 10: 5583-5595.
- Roy T, Dey SK, Pradhan A, et al. (2022). Facile and Green Fabrication of Highly Competent Surface-Modified Chlorogenic Acid Silver Nanoparticles: Characterization and Antioxidant and Cancer Chemopreventive Potential. ACS omega 7: 48018-48033.
- Wang T, Yin L, Ma Z, et al. (2022). Chlorogenic Acid-Loaded Mesoporous Silica Nanoparticles Modified with Hexa-Histidine Peptides Reduce Skin Allergies by Capturing Nickel. Molecules (Basel, Switzerland) 27(4). [crossref]
- Yao M, McClements DJ, Zhao F, et al. (2017). Controlling the gastrointestinal fate of nutraceutical and pharmaceutical-enriched lipid nanoparticles: From mixed micelles to chylomicrons. NanoImpact 5: 13-21.