Liposomal fisetin is an innovative drug delivery system, mainly used to address the limitations of fisetin in application, so as to better exert its pharmacological activity. Fisetin is a natural tetrahydroxyflavone compound, widely present in traditional Chinese medicinal plants such as Cotinus coggygria and Toxicodendron vernicifluum, as well as fruits and vegetables like strawberries, apples, onions, and cucumbers. It has a wide range of sources, high safety, and various pharmacological activities.
However, fisetin has many problems in practical application. Its solubility in water is extremely low, only about 80-90 μg/mL, and its dissolution rate is also low. At the same time, it is easily affected by digestive enzymes such as salivary amylase and pepsin, as well as factors like pH value, leading to severe degradation in the digestive tract. Moreover, as a P-glycoprotein substrate, it is difficult to be absorbed orally, with an absolute bioavailability of only 7.8% in rats. All these have greatly restricted its efficacy and clinical application.
FAQs
Q:How long is the supply cycle?
A: Regular orders will be shipped within 3 working days, while large orders (over 2 tons) require confirmation 10 days in advance. We have a regular safety stock and cooperate with multiple logistics companies to ensure timely transportation. Special needs can be negotiated for expedited processing.
Q:Can you provide technical support?
A: We have a professional R&D team that can provide descriptions of raw material characteristics, formula recommendations, and application cases (such as tablets, powders, soft capsules, etc.). If you need assistance with product filing, we can also provide compliance guidance.
Q:What is the minimum order quantity (MOQ)?
A:The standard MOQ is 100kg, while the MOQ for some high-value raw materials is 10kg. New customers can apply for a trial order (1-5kg) first, and the sample fee can be deducted from subsequent orders.
Q:What are the payment methods?
A:Support international trade common payment methods such as T/T and letter of credit (L/C).
Liposome technology provides an effective solution to these problems. Liposomes usually use lipids such as phospholipids and cholesterol as carriers, which have good safety. They have a hydrophilic core and a hydrophobic phospholipid bilayer, and can effectively encapsulate both hydrophilic and lipophilic drugs, making them a promising nano-drug delivery system. Encapsulating fisetin in liposomes can significantly improve its water solubility and protect the drug from degradation in the body.
To further enhance the performance of liposomal fisetin, researchers modify its surface. For example, polyethylene glycol (PEG) is introduced. When this hydrophilic polymer is modified on the surface of liposomes, it can form a hydration membrane and a "conformational cloud", improving the stability of ordinary liposomes, reducing clearance by the immune system, and increasing the circulation time in the body. However, PEG-modified liposomes have a slow penetration rate through the gastrointestinal mucus layer and epithelial barrier, prolonging their retention time in the digestive tract and still posing a risk of being damaged. Therefore, octaarginine (R8) is introduced, which is a cell-penetrating peptide composed of 8 arginines. It can quickly pass through biological membranes, reduce the residence time of drug-loaded liposomes in the digestive tract, and also has the effect of inhibiting drug efflux. By preparing PEG and R8 dual-modified fisetin liposomes, the complementary advantages of the two are realized. Experiments show that the retention rate of this dual-modified liposome in simulated saliva, gastric juice, and intestinal juice is much higher than that of unmodified liposomes. It has higher structural stability in simulated digestive juice, and its 18-hour cumulative release rate is also much higher than that of fisetin raw material drugs and unmodified liposomes, greatly improving the bioavailability of fisetin.
In general, as a new type of drug delivery system, liposomal fisetin has effectively improved the solubility, stability, and bioavailability of fisetin, expanded its application range in the medical field, and has broad clinical application prospects. With the deepening of research, it is expected to bring more new breakthroughs.
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