Nanoemulsion for transdermal delivery and method of making the same
Inventors
HUEN, Ngar Yee • KWOK, Sau Kuen Connie • XU, Jinjie • WONG, Chun Him • Xiao, Min
Assignees
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Publication Number
US-10137085-B2
Publication Date
2018-11-27
Expiration Date
Abstract
The present invention relates to a nanoemulsion for transdermal delivery. The presently claimed invention provides chemical formulations for preparing a nanoemulsion, and the methods for preparing the nanoemulsion. The nanoemulsion has desirable particle size for efficient transdermal delivery, and doesn't involve any organic solvent which is harmful to human skin. The corresponding fabrication method is simple.
Core Innovation
The invention provides a chemical formulation for preparing an oil in water nanoemulsion. The formulation includes an oil phase and surfactant with ethanol and water, together with an active ingredient selected from Schisandrin B and epidermal growth factor. A defined weight ratio constraint is set for water relative to ethanol plus isopropyl myristate and polysorbate 80, and the nanoemulsion is specified as an oil in water nanoemulsion.
The invention further includes transdermal relevant active ingredients by formulating nanoemulsions with epidermal growth factor and palmitoyl-pentapeptide-3. In these formulations, the oil phase and surfactant are defined as propylene glycol monocaprylate and polysorbate 20, respectively, and a penetration enhancer is included. A weight ratio constraint is imposed on oil to surfactant, and the nanoemulsion is again specified as an oil in water nanoemulsion.
In addition, specific chemical component combinations and ratios are provided, including isopropyl myristate, polysorbate 80, ethanol, water, and Schisandrin B with fixed weight percentages and a defined water-to-(ethanol plus oil and surfactant) ratio. The document also describes preparation approaches for forming the nanoemulsion by mixing the formulation components into mixtures, adding water dropwise, and then stirring or homogenizing to obtain the nanoemulsion.
Claims Coverage
The independent claims cover three formulation sets for oil in water nanoemulsions, each defined by explicit component selections and weight-ratio/weight-percentage constraints, with optional dependence on adding a penetration enhancer. The inventive features are grounded in the specified composition constraints (water-to-ethanol-plus-oil-plus-surfactant, and oil-to-surfactant), the selection of active ingredient (Schisandrin B or epidermal growth factor or palmitoyl-pentapeptide-3), and the requirement that the product nanoemulsion is an oil in water nanoemulsion.
Oil in water nanoemulsion formulation with Schisandrin B or epidermal growth factor under a water-to-ethanol-plus-oil-plus-surfactant ratio constraint
Isopropyl myristate, polysorbate 80, ethanol, water, and an active ingredient selected from Schisandrin B and epidermal growth factor, wherein a weight ratio of the water to the ethanol plus isopropyl myristate and polysorbate 80 is in a range of 3:7 to 2:8, and the nanoemulsion is an oil in water nanoemulsion.
Oil in water nanoemulsion formulation with propylene glycol monocaprylate, polysorbate 20, penetration enhancer, and palmitoyl-pentapeptide-3 under an oil-to-surfactant ratio constraint
Propylene glycol monocaprylate, polysorbate 20, a penetration enhancer, water, and palmitoyl-pentapeptide-3, wherein a weight ratio of the oil to the surfactant is in a range of 1:9 to 2:8 and the nanoemulsion is an oil in water nanoemulsion.
Fixed oil in water nanoemulsion formulation with Schisandrin B and a water-to-(ethanol plus oil and surfactant) ratio of 27:73
8 wt % isopropyl myristate, 38.4 wt % of polysorbate 80, 17 wt % of ethanol, 26 wt % of water, and 1.5 wt % of Schisandrin B, wherein a weight ratio of the water to the ethanol plus the oil and the surfactant is 27:73 and the nanoemulsion is an oil in water nanoemulsion.
Overall, the claims define oil in water nanoemulsions using specified oil and surfactant components, constrained weight ratios (water-to-ethanol-plus-oil-plus-surfactant; oil-to-surfactant; and water-to-(ethanol plus oil and surfactant)), and selected active ingredients (Schisandrin B, epidermal growth factor, or palmitoyl-pentapeptide-3), optionally including a penetration enhancer.
Stated Advantages
Improved skin penetration and reduced reliance on harmful organic solvents are described in the provided patent content.
Documented Applications
Transdermal delivery using oil in water nanoemulsions assessed using Franz-type diffusion cells with pig ear skin.
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