Myricetin-loaded, phytosome-based emulgel system with enhanced antioxidant activity

Abstract

A myricetin-loaded, phytosome-based emulgel drug delivery system consisting of an encapsulation unit, an emulgel matrix integration unit, and a process control module for the production of a stable, antioxidant topical formulation.

Description

AREA OF INVENTION

[0001] The invention relates to pharmaceutical and cosmetic delivery systems, in particular a system for delivering bioactive compounds and a formulation system for encapsulating and controlling the release of flavonoids such as myricetin. It relates in particular to a phytosome-based emulgel system that improves the antioxidant efficacy, bioavailability, and dermal absorption of myricetin for therapeutic or skincare applications. BACKGROUND OF THE INVENTION

[0002] Myricetin is a naturally occurring flavonoid with strong antioxidant, anti-inflammatory, and anti-aging properties. However, its therapeutic efficacy is limited in conventional formulations due to its low water solubility, low permeability, and instability.

[0003] Existing formulations such as simple gels, emulsions, or liposomes do not guarantee sufficient dermal penetration or sustained release of myricetin. Phytosome technology, which complexes bioactive substances with phospholipids, improves lipophilicity and membrane compatibility. However, pure phytosome dispersions do not exhibit suitable rheological properties for topical application.

[0004] Therefore, there is a need for an integrated formulation system or device that combines the advantages of phytosomes and emulgels, thus offering superior encapsulation efficiency, stability, and prolonged antioxidant activity in topical applications. The present invention addresses these limitations by developing a myricetin-loaded, phytosome-based emulgel system that effectively releases myricetin through the skin while preserving its bioactivity. SUMMARY OF THE INVENTION

[0005] The invention relates to a myricetin-loaded, phytosome-based emulgel system, consisting of a lipid-based encapsulation unit, an emulgel matrix formation unit and an integrated control module for optimizing encapsulation efficiency, process yield and delayed drug release (24 hours).

[0006] The system utilizes a phosphatidylcholine-based phytosome complexation mechanism to encapsulate myricetin molecules. These are then embedded in a gel-emulsion hybrid matrix, which stabilizes the encapsulated phytosomes and enables topical application.

[0007] The invention further comprises a process control and optimization unit for regulating important parameters - including the ratio of active ingredient to lipid, the stirring speed and the duration of sonication - in order to ensure a consistent particle size, dispersion stability and release kinetics.

[0008] The resulting myricetin-loaded emulgel exhibits increased antioxidant activity, delayed release, and improved dermal permeation. This makes it ideally suited for therapeutic or cosmetic antioxidant formulations. DETAILED DESCRIPTION OF THE INVENTION

[0009] The invention describes a device and a system for the production of phytosome emulgel formulations, consisting of the following integrated components: Phytosome formation unit: This unit includes a thin-layer hydration module in which myricetin is complexed with phosphatidylcholine to form stable phytosomes.

[0010] The unit is equipped with controlled heating, vacuum rotation and nitrogen purging to prevent oxidative degradation.

[0011] Parameters such as temperature (40-60 °C), active ingredient-lipid ratio (1:1 to 1:3) and hydration time are automatically optimized.

[0012] Module for particle size and stability control: This unit integrates a stirring and ultrasound unit for size reduction and homogenization of the phytosome vesicles.

[0013] Ultrasonic frequency and stirring speed (500-2000 rpm) are monitored by sensors to ensure a uniform particle size distribution (100-200 nm).

[0014] Emulgel integration unit: This unit integrates the phytosome dispersion into a gel-emulsion hybrid matrix using a mechanical stirrer and a temperature-controlled vessel.

[0015] The matrix consists of an oil phase, an aqueous phase, an emulsifier and a gelling agent (e.g., Carbopol or hydroxypropyl methylcellulose).

[0016] The system ensures a homogeneous dispersion and a viscosity suitable for dermal application.

[0017] Formulation optimization: The device features a controller based on a central composite design of experiments (CCD) that allows for the systematic variation of formulation parameters to optimize process yield, encapsulation efficiency, and drug release profile.

[0018] Interface for analysis and quality assessment: The device integrates sensors for pH value, viscosity, particle size and zeta potential.

[0019] Integrated UV-Vis and DPPH antioxidant assay modules determine the antioxidant activity and release kinetics of myricetin.

[0020] Storage and dosing module: The finished phytosome-based emulgel is stored under controlled environmental conditions to maintain stability and antioxidant efficacy before packaging. Functional properties:

[0021] Improves the antioxidant effect of myricetin through phospholipid complexation.

[0022] Ensures a controlled release over 24 hours (Q24h).

[0023] Improves stability, bioavailability, and dermal absorption.

[0024] Suitable for pharmaceutical and cosmetic applications.

Claims

[1] A myricetin-loaded, phytosome-based emulgel drug release system comprising an encapsulation unit, an emulgel matrix integration unit and a process control module for the production of a stable, antioxidant topical formulation. [2] System according to claim 1, wherein the encapsulation unit comprises a thin-layer hydration chamber for the formation of myricetin-phosphatidylcholine phytosomes under controlled temperature and vacuum. [3] System according to claim 1, wherein the emulgel matrix integration unit combines a gel-forming polymer and an emulsifier to create a hybrid emulsion-gel matrix which ensures uniform dispersion and rheological stability. [4] System according to claim 1, further comprising an optimization control module implementing a central composite experimental design to adjust the drug-lipid ratio, stirring speed and ultrasonic treatment time to maximize encapsulation efficiency and drug release. [5] System according to claim 1, wherein the analytical interface evaluates viscosity, pH value, particle size and antioxidant activity, thus enabling real-time quality control of the formulation.