599$/KG
499$/KG
Product Detailed Description
liposomal Gastrodin 70% is a premium-grade dietary supplement ingredient delivering gastrodin in an advanced liposomal delivery system. Gastrodin (CAS 62499-27-8), also known as 4-(hydroxymethyl)phenyl-beta-D-glucopyranoside or gastrodine, is the major active constituent of Gastrodia elata Blume (Orchidaceae), a medicinal plant commonly known as Tianma in China. It is a phenolic glycoside that is chemically characterized by a glucose unit conjugated to a 4-hydroxybenzyl alcohol moiety via a β-glycosidic linkage. Gastrodin occurs as white to almost white powder or crystals and is soluble in water and methanol.
Gastrodia elata has been used for centuries in traditional Chinese medicine for the treatment of infantile convulsion, epilepsy, spasm, tetanus, and vertigo. Gastrodin has been reported to possess a wide range of pharmacological effects, including antioxidation, anti-inflammation, hypoglycemic, hypolipidemic, antitumor, immunomodulation, and antiallergy activities, as well as good sedative and sleep-inducing effects that can alleviate symptoms of neurasthenia, insomnia, and headache. It is clinically used for brain-related diseases in China and has shown promise as a therapeutic agent for demyelinating diseases.
Conventional gastrodin presents significant formulation and bioavailability challenges. Gastrodin is a water-soluble drug with limited passive permeability across biological membranes, and its ability to cross the blood-brain barrier is restricted. This limits its therapeutic potential for central nervous system (CNS) disorders despite its established neuroprotective properties.
Liposomal encapsulation provides four critical advantages:
1. Dramatically Enhanced Brain Delivery — A multivesicular liposome formulation of gastrodin (GAS-MVLs), prepared by microfluidic technology, achieved an average particle size of 2.09 ± 0.17 μm with a dense, spherical structure and relatively narrow size distribution. In vivo pharmacokinetic studies in mice demonstrated that the intracerebral AUC of GAS-MVLs was 5.68 times higher than that of the GAS solution, with a Cmax 2.036 times higher. The brain-targeting efficiency (BTE) was 1.945, and the relative uptake rate (Re) was 5.688, indicating significant enrichment of gastrodin in the brain.
2. Enhanced Blood-Brain Barrier Permeability — In an in vitro BBB model established by coculturing mouse brain endothelial cells (bEnd.3) and astrocytes (C8-D1A), the apparent transmittance of GAS-MVLs was 67.71% at 6 hours after administration, which was 1.92 times higher than that of the GAS solution.
3. Protection from Degradation and Premature Metabolism — The phospholipid bilayer shields gastrodin from enzymatic degradation and premature metabolism during digestive transit, preserving its intact molecular structure until reaching optimal absorption sites.
4. Sustained Release for Prolonged Neuroprotective Activity — Liposomal delivery provides a controlled-release profile that maintains steady plasma levels of gastrodin, supporting prolonged neuroprotective and neuromodulatory activity rather than a sharp peak followed by rapid clearance.
High Purity — Standardized to ≥70% gastrodin by HPLC, with ≥98.0% (HPLC) assay available for premium applications.
Liposomal Enhancement — Multivesicular liposome encapsulation achieves 5.68-fold higher intracerebral AUC and 2.036-fold higher Cmax compared to free gastrodin solution, with 1.92-fold higher BBB permeability.
Clinically Established for Neurological Disorders — Gastrodia elata has been used to treat infantile convulsion, epilepsy, spasm, tetanus, and vertigo. Gastrodin is clinically used for brain-related diseases in China.
Neuroprotective Mechanisms — Gastrodin demonstrates significant neuroprotective effects across various neurodegenerative disease models, including Alzheimer's disease and Parkinson's disease. Its mechanisms involve multi-target actions such as inhibiting pathological protein aggregation (Aβ) and modulating oxidative stress, ferroptosis, and cellular senescence.
Demyelinating Disease Support — Gastrodin promotes CNS myelinogenesis and alleviates demyelinating injury by activating the PI3K/AKT/mTOR signaling pathway, identifying it as a promising therapeutic agent for demyelinating diseases.
Sedative and Sleep Support — Gastrodin exhibits good sedative and sleep-inducing effects and can alleviate symptoms of neurasthenia, insomnia, and headache.
Brain-Targeting Ligand — Gastrodin has been explored as a brain-targeting ligand for the construction of novel glucose transporter (GLUT1)-targeted lipid drug delivery systems, demonstrating favorable targeting to bEnd.3 brain microvascular endothelial cells and GL glioma cells.
Water-Dispersible — Liposomal powder offers excellent dispersibility in aqueous systems; suitable for capsules, tablets, powder drink mixes, and functional beverages.
Batch Traceability — Complete COA, HPLC chromatogram, and identity data provided for each batch.
| Application | Recommended Usage | Notes |
|---|---|---|
| Capsules / Tablets | 100–200 mg per serving | 1–3 capsules daily with meals; clinical studies used 300 mg twice daily |
| Functional Beverages | 50–100 mg per 250 mL | Water-dispersible; suitable for RTD formats |
| Powdered Drink Mixes | 300–600 mg per sachet | Best absorbed when taken with food |
| Neuroprotection Formulas | 300–600 mg per serving | Often combined with NAD+ precursors, RESVERATROL, or curcumin |
| Cognitive Support Formulas | 300–600 mg per serving | Often combined with phosphatidylserine or DHA |
| Sleep Support Formulas | 100–300 mg per serving | Take 30–60 minutes before bedtime |
Clinical studies and commercial products commonly recommend varying doses of gastrodin depending on the application. For oral tablets, the typical dosage is 50–100 mg per administration, taken three times daily (150–300 mg/day). For maximum neuroprotective benefit, a suggested regimen of 600 mg gastrodin in divided doses (300 mg twice daily) for thirty days has been reported, followed by a maintenance dose of 300 mg daily based on the experience of gastrodin as an over-the-counter pharmaceutical agent. For injection, 0.6 g once daily for 14 days has been used in clinical studies for cerebral infarction. For sustained-release tablets, 150 mg twice daily for 4 weeks has been evaluated. For general neuroprotective and cognitive support, 300–600 mg daily in divided doses is commonly used. Liposomal formulations may allow for more efficient utilization of lower doses due to enhanced bioavailability and brain targeting.
Stock Orders: 3–5 business days after payment confirmation.
Bulk / Custom Orders: 2–3 weeks, depending on quantity and customization requirements.
Shipping Methods: International Express (FedEx, DHL, UPS), air freight, and sea freight.
Coverage: Worldwide shipping, including remote areas.
Gastrodin Encyclopedia — Scientific Background
Gastrodin (CAS 62499-27-8), also known as 4-(hydroxymethyl)phenyl-beta-D-glucopyranoside or gastrodine, is a naturally occurring phenolic glycoside and the principal bioactive constituent of Gastrodia elata Blume (Orchidaceae), commonly known as Tianma. It is chemically characterized by the molecular formula C₁₃H₁₈O₇ and a molecular weight of 286.28 g/mol. Gastrodin consists of a glucose unit conjugated to a 4-hydroxybenzyl alcohol moiety via a β-glycosidic linkage. It occurs as a white to almost white crystalline powder with a bitter taste and little hygroscopicity, and is soluble in water and methanol.
| Property | Value |
|---|---|
| CAS No. | 62499-27-8 |
| Molecular Formula | C₁₃H₁₈O₇ |
| Molecular Weight | 286.28 g/mol |
| IUPAC Name | 4-(Hydroxymethyl)phenyl β-D-glucopyranoside |
| Synonyms | Gastrodine, 4-Hydroxybenzyl Alcohol 4-O-β-D-Glucopyranoside |
| Appearance | White to almost white powder to crystal |
| Melting Point | 154.0–160.0°C |
| Specific Rotation | −66.0 to −70.0 deg (C=1, H₂O) |
| λmax | 272 nm (MeOH) |
| PubChem CID | 96023450 |
| KEGG Compound | C16964 |
Gastrodin is extracted from the dried rhizome of Gastrodia elata Blume, a perennial saprophytic orchid native to East Asia and widely cultivated in China. The plant is a well-known traditional Chinese medicine with medicinal and food-based homology. The crude gastrodin is obtained by extraction with ethanol from the dried roots of G. elata under sonication, followed by preparative isolation and purification using high-speed counter-current chromatography. The content of gastrodin in the rhizome varies depending on the source, cultivation conditions, and extraction method, with optimized extraction conditions using freeze-dried tissues at 50°C with deionized water yielding superior results compared to methanol extraction.
Gastrodin demonstrates significant neuroprotective effects across various neurodegenerative disease models, including Alzheimer's disease (AD) and Parkinson's disease (PD). Its mechanisms involve multi-target actions such as inhibiting pathological protein aggregation (Aβ), modulating oxidative stress, suppressing ferroptosis, and regulating cellular senescence. These complementary mechanisms make gastrodin a promising therapeutic agent for the prevention and treatment of neurodegenerative disorders.
Gastrodin promotes CNS myelinogenesis and alleviates demyelinating injury by activating the PI3K/AKT/mTOR signaling pathway. These results identify gastrodin as a promising therapeutic agent for demyelinating diseases and highlight the potential of zebrafish models for screening pro-myelinogenic pharmacotherapy.
Gastrodin exhibits significant anti-inflammatory and antioxidant properties, contributing to its broad pharmacological profile. It has been reported to possess antioxidation, anti-inflammation, hypoglycemic, hypolipidemic, antitumor, immunomodulation, and antiallergy activities. These effects are mediated through modulation of multiple signaling pathways, including Nrf2 activation and inhibition of NF-κB signaling.
Gastrodin has a good sedative and sleep-inducing effect and can alleviate symptoms of neurasthenia, insomnia, and headache. This clinical profile supports its traditional use for neurological and psychological conditions.
Gastrodin has been explored as a brain-targeting ligand for the construction of novel glucose transporter (GLUT1)-targeted lipid drug delivery systems. The gastrodin-modified liposomes exhibited favorable targeting to bEnd.3 brain microvascular endothelial cells and GL glioma cells, demonstrating the potential of gastrodin as a ligand for brain-targeted drug delivery.
Despite its established neuroprotective properties, native gastrodin presents significant bioavailability challenges. As a water-soluble drug, gastrodin has limited passive permeability across biological membranes, and its ability to cross the blood-brain barrier is restricted. This limits its therapeutic potential for CNS disorders despite its established neuroprotective properties.
These limitations have driven the development of advanced delivery systems, including multivesicular liposomes (MVLs) prepared by microfluidic technology. GAS-MVLs significantly delivered gastrodin across the BBB and enriched gastrodin in the brain, providing a possibility for brain-targeting delivery of gastrodin in the prevention and treatment of central nervous system diseases by oral administration.
liposomal encapsulation of gastrodin provides a fundamentally different delivery mechanism from conventional forms. The phospholipid bilayer surrounds the gastrodin molecule, forming a nanoscale vesicle that enhances stability, BBB permeability, and brain delivery. This delivery system:
Achieves 5.68-fold higher intracerebral AUC compared to free gastrodin solution
Achieves 2.036-fold higher Cmax in the brain compared to free gastrodin solution
Demonstrates 1.92-fold higher BBB permeability (67.71% vs. 35.27% apparent transmittance at 6 h)
Achieves brain-targeting efficiency (BTE) of 1.945 and relative uptake rate (Re) of 5.688
Provides a spherical, dense multivesicular structure with average particle size of 2.09 ± 0.17 μm
The GAS-MVLs prepared by microfluidic technology showed an obvious multivesicular structure and a relatively narrow distribution of particle sizes. The prepared GAS-MVLs were spherical with a dense structure. Both in vitro and in vivo experiment results showed that GAS-MVLs significantly delivered GAS across the BBB and enriched GAS in the brain. This provides a possibility for brain-targeting delivery of GAS in the prevention and treatment of central nervous system diseases by oral administration and lays the foundation for further development of oral brain-targeted preparations of GAS.
Clinical studies have evaluated gastrodin for cerebrovascular and neurological conditions. In patients with cerebral infarction, gastrodin injection at 0.6 g once daily for 14 days achieved a total effective rate of 94.74%. For migraine, gastrodin injection at 0.6 g (i.v.gtt) once daily for 10 days or sustained-release tablets at 150 mg twice daily for 4 weeks have been evaluated, with a total effective rate of 73.33% and reductions in IGF-1 and IL-6 levels.
Gastrodin and gastrodigenin (HBA) demonstrate significant neuroprotective effects across various neurodegenerative disease models, including Alzheimer's disease and Parkinson's disease. Their mechanisms involve multi-target actions such as inhibiting pathological protein aggregation (Aβ) and modulating oxidative stress, ferroptosis, and cellular senescence. These preclinical findings support the clinical investigation of gastrodin for neurodegenerative disease prevention and treatment.
Gastrodin alleviates glucocorticoid-induced osteoporosis in rats via activating the Nrf2 signaling pathways, demonstrating additional therapeutic potential beyond its well-established neurological applications.
Gastrodin is generally well tolerated. In clinical studies, a small number of patients experienced dry mouth and nose, but no serious adverse effects were reported. Gastrodia elata has been used as a traditional Chinese medicine with medicinal and food-based homology for centuries, supporting its safety profile.
Regulatory status varies by region:
China — Gastrodin is approved as a pharmaceutical ingredient and is clinically used for brain-related diseases. It is available in injection, tablet, and sustained-release tablet formulations.
United States — Gastrodin is commercialized as a dietary supplement ingredient. USP has established a reference standard for Gastrodin (Catalog No. 1288394) to support quality control and standardization.
Global Standards — Gastrodin is monographed in the USP and is available as a research chemical with ≥98% purity (HPLC) from major suppliers. Testing protocols must adhere to international standards including USP, European Pharmacopoeia, and FAO/WHO Codex Alimentarius. Formulators should verify local regulatory requirements prior to market entry.
This product is intended for research, nutraceutical, and functional food applications. Not intended to diagnose, treat, cure, or prevent any disease.
599$/KG
499$/KG
RELATED
RELATED
This website uses cookies to ensure you get the best experience on our website.
Español
Français
Deutsch
日本語
한국어
Phone
Comment
（0）