Botulinum nanoemulsions
Inventors
Edelson, Jonathan • Nicolosi, Robert
Assignees
University of Massachusetts Lowell
Publication Number
US-9486408-B2
Publication Date
2016-11-08
Expiration Date
2026-12-01
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Abstract
The embodiment described herein are related nanoemulsions comprising botulinum toxins. In one embodiment, the nanoemulsions are prepared by high pressure microfluidization and comprise a particle size distribution exclusively between 10 and 300 nm. The nanoemulsions contemplated by the present invention are useful for the cosmetic and medical treatment of muscular contracture states. For example, botulinum toxin may relax facial muscles such that skin wrinkles become smoother and less noticeable. Further, the present invention contemplates a cosmetic formulation that may be self-administered, for example, in the privacy of one's home and without medical supervision.
Core Innovation
The invention provides nanoemulsion compositions containing botulinum toxin, designed for both cosmetic and medical use. These nanoemulsions are formed by dispersing oily particles within an aqueous dispersion medium, with a majority of the particles having diameters between approximately 10 and 300 nanometers. The nanoemulsions incorporate at least one botulinum toxin, a surfactant, and an oil, prepared preferably by high shear processes such as microfluidization, which ensures a narrow and uniform particle size distribution.
A key aspect of the invention is the ability of the formulated nanoemulsion to deliver botulinum toxin transdermally, that is, through the skin, without the need for chemical, mechanical, electrical, or magnetic permeation enhancers or agents that cause abrasion or disruption of the skin. The botulinum toxin is able to penetrate the stratum corneum and other skin layers effectively, allowing the therapeutic agent to reach subdermal targets. The nanoemulsion can be formulated as various topical compositions, including creams, lotions, gels, ointments, sprays, powders, or emollients.
The problem addressed is that traditional botulinum toxin delivery is primarily by injection, which can cause adverse effects such as tissue damage, unintended delivery to undesirable locations, pain, hematoma, ecchymosis, and bruising. Existing non-injection transdermal delivery methods often require skin disruption or enhancers that may irritate the skin. The nanoemulsion technology overcomes these limitations by enabling effective, minimally invasive, and user-friendly administration of botulinum toxin.
Claims Coverage
There is one independent claim in this patent, which outlines the main inventive features of the topical nanoemulsion composition for botulinum toxin delivery.
Topical nanoemulsion composition with oily particles dispersed in an aqueous medium
The composition comprises a nanoemulsion where oily particles are dispersed within an aqueous dispersion medium, with the majority of the oily particles having diameters between approximately 10 and 300 nanometers. It includes at least one botulinum toxin, a surfactant, and an oil, and the oil and surfactant are present in a ratio between 0.5 and 2.0. The composition is formulated such that the botulinum toxin can penetrate human skin without the use of abrasive or disrupting agents, which are defined as chemical, mechanical, electrical, or magnetic permeation enhancers. It is further formulated as a cream, lotion, gel, ointment, spray, powder, emollient, or combination thereof for transdermal administration.
The main inventive feature is a stabilized topical nanoemulsion composition facilitating transdermal delivery of botulinum toxin without requiring skin-disrupting agents, characterized by controlled particle size and specific formulation parameters.
Stated Advantages
Enables transdermal delivery of botulinum toxin without chemical or physical disruption of the skin.
Minimizes adverse effects associated with injection, such as tissue damage, pain, hematoma, and bruising.
Provides improved stability of botulinum toxin compared to free solution by protection against denaturation and degradation.
Allows for self-administration in a non-clinical setting, eliminating the need for medical supervision.
Facilitates uniform and controlled particle size distribution for consistent dosing and tissue absorption.
Reduces the risk of irritation or noticeable skin alterations during transdermal delivery.
Documented Applications
Cosmetic treatment of facial wrinkles, including smoothing skin and reducing the appearance of lines.
Treatment of hyperhidrosis (excessive sweating).
Medical treatment of muscular contracture and/or overactivity.
Treatment of neuromuscular disorders such as cerebral palsy, facial palsy, blepharospasm, dystonia, and strabismus.
Treatment of platysma bands (neck muscle bands) and related cosmetic issues.
Treatment of benign prostatic hyperplasia symptoms.
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