Product Detailed Description

liposomal Aescin 70% — High Bioavailability Vasoprotective and Anti-Edema Supplement

Product Overview

Liposomal Aescin 70% is a premium-grade dietary supplement ingredient delivering β-aescin in an advanced liposomal delivery system. Aescin (CAS 6805-41-0 for the aescin mixture; 20977-05-3 for sodium aescinate) is a triterpene saponin complex extracted from the dried seeds of Aesculus hippocastanum L., commonly known as horse chestnut. The aescin complex consists of closely related triterpene saponins including escin Ia, Ib, IIa, and IIb, with the β-aescin fraction representing the most pharmacologically active component. The molecular formula of the aescin complex is C₅₅H₈₆O₂₄ with a molecular weight of approximately 1131.26 g/mol, while the monosodium salt (sodium aescinate) has the molecular formula C₅₄H₈₄NaO₂₃ and a molecular weight of 1124.2 g/mol.

Aescin has been used therapeutically for decades in Europe for the treatment of chronic venous insufficiency (CVI), hemorrhoids, and post-operative or post-traumatic edema. It exhibits a unique pharmacological profile characterized by anti-edematous, anti-inflammatory, and venotonic activities. Aescin is the active principle responsible for the therapeutic efficacy of horse chestnut seed extract, which has been shown in controlled trials to be as effective as compression therapy as an alternative to medical treatment for CVI.

Why Liposomal Technology?

Conventional aescin presents significant formulation and bioavailability challenges. Sodium aescinate is often used for intravenous injection, but its clinical application is limited by strong irritation, short half-life, and low bioavailability. Following oral administration, only 13–16% of an aescin dose is absorbed (non-volatile radioactivity), with peak plasma concentrations achieved approximately 4 hours after administration. After oral administration, aescin is rapidly absorbed with an absorption half-life of approximately 1 hour, but undergoes significant first-pass metabolism resulting in a plasma bioavailability of only 1.5%.

Liposomal encapsulation provides four critical advantages:

1. Enhanced Safety and Tolerability — The SA-Lip-I formulation did not induce hemolysis at 37°C and produced by far milder venous irritation compared to commercial sodium aescinate injection. The LD50 of SA-Lip-I was 2.12-fold higher than that of the commercial SA-I, indicating significantly improved safety margins with no obvious side effects.

2. Enhanced Stability and Sustained Release — The mean particle size of SA-Lip-I was 117.33 ± 0.95 nm, with a PDI of 0.140 ± 0.017 and a zeta potential of −30.34 ± 0.23 mV. The cumulative release of SA-Lip at 12 hours was more than 80%, which met the release requirements of nanoparticles. SA-Lip-I was well stable in the four mediators (simulated gastric fluid, simulated intestinal fluid, phosphate buffer, and physiological saline) and met the clinical medication requirements.

3. Superior Efficacy — SA-Lip-I demonstrated better efficacy than unencapsulated SA-I, with a significant difference. The liposomal formulation achieved the optimal curative effect while reducing irritation and toxic side effects, and greatly alleviating patient pain during treatment.

4. Enhanced Cellular Uptake — liposomes fuse directly with cell membranes, facilitating efficient cellular delivery via lipid-mediated pathways. The encapsulation of aescin into nanocarriers is a promising strategy to overcome its limitations, such as poor water solubility and low bioavailability, thereby enhancing its therapeutic efficacy.

Product Specifications

Key Features

• High Purity — Standardized to ≥70% aescin by HPLC, ensuring consistent active content of the principal triterpene saponin complex.

• Liposomal Enhancement — Phospholipid bilayer encapsulation achieves 117.33 ± 0.95 nm particle size with PDI of 0.140 ± 0.017 and zeta potential of −30.34 ± 0.23 mV, with cumulative release exceeding 80% at 12 hours.

• 2.12-Fold Higher Safety Margin — The LD50 of liposomal sodium aescinate was 2.12-fold higher than commercial unencapsulated sodium aescinate, with no hemolysis at 37°C and significantly milder venous irritation.

• Clinically Validated for Post-Traumatic Edema — A double-blind, parallel-group, 3-arm clinical study in 300 patients demonstrated that oral escin (20 mg three times daily) reduced edema in 82.3% of patients with post-operative or post-traumatic soft tissue swelling, compared with 72.4% for placebo (p<0.05).

• Clinically Validated for Chronic Venous Insufficiency — Standardized horse chestnut seed extract has been shown to significantly reduce symptoms of chronic venous insufficiency, with aescin demonstrating efficacy comparable to compression therapy in controlled trials.

• Anti-Edematous Mechanisms — Aescin inhibits exudation by reducing the extravasation of fluid into the tissue and accelerating the subsidence of oedema. The mode of action is based on changes in the permeability of the affected capillary walls. In addition, aescin raises capillary resistance, inhibits inflammatory processes, and improves microcirculation.

• 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 & Formulation Guidance

Recommended Dosage

Clinical studies have evaluated aescin across a range of doses. A double-blind, parallel-group, 3-arm clinical study in 300 patients with post-operative or post-traumatic soft tissue swelling used oral escin at 20 mg three times daily for 14 days, demonstrating a reduction in edema in 82.3% of patients compared with 72.4% for placebo (p<0.05). A placebo-controlled study in 100 orthopedic patients used oral escin at 2×20 mg three times daily (120 mg/day), with treatment improving post-plastering edema in 92% of patients and post-traumatic edema in 95% of patients. The usual initial dosage of standardized horse chestnut extract is 90 to 150 mg of aescin daily, while the effective oral dose is 600–900 mg of standardized extract corresponding to 100–150 mg aescin daily, divided into 2 doses. A clinical trial in chronic venous insufficiency evaluated patients receiving oral escin at 50 mg twice daily (100 mg/day), compared with placebo. For general venous health and anti-edema support, 100–150 mg aescin daily is commonly used.

Important Safety Information: Aescin should not be used by individuals with known hypersensitivity to horse chestnut or related plants. Caution is advised in patients taking anticoagulant medications (e.g., warfarin), as horse chestnut may potentiate anticoagulant activity. Aescin should not be applied to broken or ulcerated skin. Pregnant or lactating women and children should consult a healthcare professional before use. The safety of aescin has not been established in children under 12 years of age for all indications.

Shipping & Lead Time

• 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.