Chlorogenic acid ufasome-based hydrogel release system for increased antioxidant potential

Abstract

A hydrogel release system based on chlorogenic acid and ufasomes, consisting of a lipid encapsulation unit, a vesicle homogenization unit and a hydrogel integration chamber for the production of a stable antioxidant formulation with increased release potential.

Description

AREA OF INVENTION

[0001] The invention relates to pharmaceutical nanocarrier release systems, in particular a lipid vesicle hydrogel system loaded with bioactive substances, which integrates Ufasome technology for controlled release and improved antioxidant efficacy. The invention provides a formulation system and a structural configuration for the production, optimization, and stabilization of chlorogenic acid-loaded Ufasomes embedded in a hydrogel matrix, suitable for biomedical and cosmetic applications. BACKGROUND OF THE INVENTION

[0002] Chlorogenic acid, a naturally occurring polyphenol compound, possesses strong antioxidant and anti-inflammatory properties, but exhibits low stability, limited solubility, and insufficient bioavailability when administered via conventional dosage forms. Traditional hydrogels have insufficient permeability and retention capacity for the efficient dermal or transdermal delivery of such hydrophilic bioactives.

[0003] Ufasomes, or vesicles made of unsaturated fatty acids, represent a promising delivery system due to their ability to encapsulate both hydrophilic and lipophilic drugs while offering structural flexibility and membrane compatibility. However, ufasomes alone tend to aggregate, become instability, and leak during storage.

[0004] Therefore, there is a need for a unified delivery system that integrates ufasome nanocarriers into a hydrogel matrix, thereby ensuring superior stability, bioavailability, and sustained release of antioxidants. The present invention addresses these limitations by developing a chlorogenic acid- and ufasome-based hydrogel system optimized through design-based formulation control, providing a novel, device-like formulation framework for antioxidant therapy. SUMMARY OF THE INVENTION

[0005] The present invention provides a hydrogel delivery system based on chlorogenic acid and ufasomes, consisting of an encapsulation module, a vesicle stabilization and homogenization unit, and a hydrogel integration chamber for generating a stable antioxidant formulation.

[0006] The system utilizes a thin-film hydration mechanism to form lipid vesicles from phosphatidylcholine and oleic acid. These vesicles encapsulate chlorogenic acid and are homogenized using ultrasound to obtain uniform, nanoscale Ufasomes. The resulting vesicle suspension is then embedded in a hydrogel matrix to enhance stability, rheological properties, and controlled release.

[0007] The system also incorporates a Box-Behnken optimization interface that regulates three key parameters—lipid concentration, oleic acid content, and rotation speed—to maximize encapsulation efficiency and process yield. The optimized formulation exhibits improved antioxidant activity, delayed release, and enhanced topical applicability, representing a significant advancement in lipid-based antioxidant delivery technology. DETAILED DESCRIPTION OF THE INVENTION

[0008] The invention describes a device for administering chlorogenic acid ufasome hydrogel, consisting of several interconnected and synergistically functioning units: Encapsulation unit: A thin-film hydration chamber in which chlorogenic acid, phosphatidylcholine, and oleic acid are dissolved in methanol. The solvent is evaporated at 70 °C under vacuum using a rotary evaporator, resulting in the formation of a uniform lipid film on the flask surface. Hydration and vesicle formation unit: The lipid film is hydrated with phosphate buffer (pH 6.8) for 24 hours at room temperature to form multilamellar vesicles containing chlorogenic acid. The hydration unit maintains constant pH and temperature via an integrated control loop. Homogenization and particle size reduction unit: The hydrated vesicle dispersion is treated using an ultrasonic probe, ensuring the formation of nanoscale vesicles with uniform particle size and high encapsulation efficiency. Parameters such as amplitude, time, and pulse cycle are adjustable via a digital controller. Filtration and cleaning unit: The Ufasome dispersion passes through a 0.22 µm filtration membrane, removing impurities and unencapsulated drug particles, resulting in a stable, pure nanosuspension. Hydrogel integration chamber: The Ufasom suspension is incorporated into a pre-formulated hydrogel matrix under temperature-controlled conditions using a mechanical stirrer. The gel base, which contains suitable polymers such as Carbopol, ensures a uniform consistency and enables delayed drug release. Optimization and control interface: The device has a computing module based on the Box-Behnken design, which is programmed to modulate the lipid concentration (X1), the oleic acid ratio (X2) and the rotation speed (X3) and analyze their influence on the encapsulation efficiency (Y1) and the process yield (Y2). Quality and Performance Analysis Unit: The final hydrogel system integrates sensors for measuring pH, viscosity, particle size distribution and antioxidant activity using embedded spectroscopic and DPPH assay modules. Functional features: Improves the stability and bioavailability of chlorogenic acid. Ensures a controlled and sustained release of antioxidants. Enables the systematic optimization of formulation parameters. Offers a scalable and environmentally friendly production facility. Suitable for therapeutic and cosmetic applications with antioxidant active ingredients.

Claims

[1] A hydrogel release system based on chlorogenic acid and ufasomes, consisting of a lipid encapsulation unit, a vesicle homogenization unit and a hydrogel integration chamber for the production of a stable antioxidant formulation with increased release potential. [2] System according to claim 1, wherein the encapsulation unit Ufasome is formed by thin-layer hydration using phosphatidylcholine and oleic acid as the main components under vacuum evaporation at controlled temperature. [3] System according to claim 1, wherein the hydrogel integration chamber combines the Ufasome dispersion with a gel-forming polymer to achieve uniform viscosity, controlled release and improved topical stability. [4] System according to claim 1, wherein the device comprises a Box-Behnken optimization module that regulates the lipid concentration, oleic acid ratio and rotation speed to maximize encapsulation efficiency and process yield. [5] System according to claim 1, further comprising analytical sensors for monitoring pH value, particle size and antioxidant potential for real-time quality validation.