Botulinum nanoemulsions
Inventors
Edelson, Jonathan • Nicolosi, Robert J.
Assignees
University of Massachusetts Lowell
Publication Number
US-8318181-B2
Publication Date
2012-11-27
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, which are characterized by nanoparticle size distributions where a majority of the particles have diameters between approximately 10 and 300 nanometers. These nanoemulsions are prepared by processes such as high pressure microfluidization, resulting in uniform nanoparticle populations. The compositions are suitable for administration by a variety of routes, including both conventional injection and transdermal delivery, and are designed to deliver botulinum toxin efficiently to target tissues.
This invention addresses the challenges and adverse effects associated with current botulinum toxin delivery systems, which primarily rely on injection. Standard injection methods can cause tissue damage, unintended toxin delivery to non-target sites, pain, bruising, and other complications. Additionally, stability issues with existing formulations can reduce their efficacy and safety.
The nanoemulsions described in the patent enable botulinum toxin to be delivered transdermally, effectively permeating the skin without requiring abrasion, permeation enhancers, or disruption of the skin's structure. The compositions may be incorporated into creams, lotions, patches, or other topical formulations and allow for non-invasive, potentially self-administered cosmetic and medical treatments such as wrinkle reduction and relief of muscular contracture states. The nanoemulsions maintain particle stability, improve toxin permeability, and reduce the likelihood of adverse skin reactions typically associated with transdermal delivery.
Claims Coverage
The patent contains three independent inventive features, primarily relating to methods of administering botulinum toxin nanoemulsions to the skin for therapeutic and cosmetic purposes.
Transdermal administration of botulinum toxin nanoemulsion
A method is disclosed involving: - Providing a subject. - Providing a composition comprising a nanoemulsion, in which a majority of its particles have diameters between approximately 10 and approximately 300 nanometers and the nanoemulsion comprises at least one botulinum toxin. - Administering the composition to the skin of the subject so that the botulinum toxin is delivered into the skin.
Treatment of wrinkles, facial lines, and/or neck lines with a botulinum toxin nanoemulsion
A method comprising: - Providing a subject exhibiting symptoms of wrinkles, facial lines, and/or neck lines. - Providing a nanoemulsion composition where a majority of particles have diameters between approximately 10 and 300 nanometers and the nanoemulsion includes at least one botulinum toxin. - Administering the composition to the subject's skin such that symptoms are reduced.
Delaying onset of wrinkle formation with a botulinum toxin nanoemulsion
A method comprising: - Providing a subject not exhibiting symptoms of wrinkles, facial lines, and/or neck lines. - Providing a nanoemulsion composition where a majority of particles have diameters between approximately 10 and 300 nanometers and the nanoemulsion includes at least one botulinum toxin. - Administering the composition to regions of the subject's skin that typically develop wrinkles prior to wrinkle formation such that onset of symptoms is delayed.
The inventive features focus on compositions containing botulinum toxin within nanoemulsions of tightly controlled particle sizes, and their methods of administration to the skin for therapeutic, cosmetic, and preventative benefits.
Stated Advantages
Nanoemulsions allow transdermal delivery of botulinum toxin without requiring abrasion, permeation enhancers, or disruption of the skin, thereby minimizing irritation and adverse skin reactions.
The compositions provide improved stability of botulinum toxin compared to free solutions, protecting the toxin from heat, alkaline and acidic conditions, degradative enzymes, and neutralizing antibodies.
Botulinum toxin within the nanoemulsion has enhanced skin permeability, allowing more efficient and effective delivery through the skin compared to free solutions.
The non-invasive topical approach enables self-administration, reducing the need for medical supervision or injection by trained personnel.
The nanoemulsions can minimize adverse effects associated with injections such as pain, tissue damage, hematoma, ecchymosis, and bruising.
The compositions can be formulated without toxic solvents or polymers, offering better biocompatibility and tissue absorption compared to existing nanoparticle systems that require such additives.
Stabilization of botulinum toxin within nanoemulsions may reduce immunogenicity and extend the shelf life of the formulations.
Documented Applications
Cosmetic treatment of facial wrinkles, facial lines, and neck lines through topical application or transdermal administration of botulinum toxin nanoemulsions.
Delaying the onset of facial and neck wrinkles by regular topical application of botulinum toxin nanoemulsions to regions prone to wrinkle formation.
Medical treatment of muscular contracture states, such as facial palsy, facial contracture, dystonia, hemifacial spasm, blepharospasm, spasticity, and cerebral palsy by localized transdermal administration.
Treatment of hyperhidrosis (excessive sweating) through topical administration of botulinum toxin nanoemulsions.
Relief of symptoms associated with conditions such as strabismus and benign prostatic hyperplasia.
Use as a muscle relaxant when administered by injection or transdermal delivery.
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