Botulinum nanoemulsions
Inventors
Edelson, Jonathan • Nicolosi, Robert
Assignees
University of Massachusetts Lowell
Publication Number
US-10576034-B2
Publication Date
2020-03-03
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, with a majority of particles having diameters between approximately 10 and 300 nanometers. These nanoemulsions are prepared using high shear methods such as microfluidization or high pressure homogenization to yield a stable, uniform particle size distribution. The composition is designed for both cosmetic and medical use, allowing for the delivery of botulinum toxin in a format that does not require injection.
A key problem addressed by the invention is the adverse effects and challenges linked with traditional injection methods of botulinum toxin delivery, which can result in tissue damage, improper targeting, pain, hematoma, ecchymosis, and bruising. Existing methods often necessitate special techniques or equipment and may require skin disruption for non-injection routes, adding complexity and risk.
The inventive botulinum nanoemulsions enable transdermal delivery of the toxin without agents or techniques that alter or disrupt the skin, offering effective permeation through the stratum corneum. These compositions can be incorporated into creams, patches, and other topical formulations, offering self-administration potential and reducing the need for medical supervision or invasive procedures.
Claims Coverage
There are two independent claims providing the main inventive features: a method of inhibiting acetylcholine release at neuromuscular junctions via transdermal nanoemulsion administration, and a method of treating diseases or conditions involving acetylcholine release at neuromuscular junctions using a transdermal botulinum toxin nanoemulsion.
Transdermal administration of botulinum nanoemulsion for neuromuscular acetylcholine inhibition
A method comprising transdermally administering a composition to a subject's skin, where the composition is a nanoemulsion in which a majority of particles have diameters between approximately 10 and 300 nanometers and contains at least one botulinum toxin. This administration inhibits the release of acetylcholine at the neuromuscular junction.
Transdermal treatment of conditions involving acetylcholine release using botulinum nanoemulsion
A method of treating a disease, disorder, or condition involving release of acetylcholine at a neuromuscular junction by transdermally administering a nanoemulsion composition to the skin, characterized by a majority of particles between about 10 and about 300 nanometers in diameter, with at least one botulinum toxin present.
The inventive features focus on transdermal delivery of a botulinum toxin nanoemulsion with specified nanoparticle size, achieving inhibition of acetylcholine release at neuromuscular junctions and treating related medical or cosmetic conditions.
Stated Advantages
Provides transdermal delivery of botulinum toxin without requiring chemical, physical, electrical, or mechanical disruption of the skin.
Reduces or eliminates adverse effects associated with injection, such as tissue damage, pain, hematoma, ecchymosis, bruising, and improper delivery.
Offers improved stability of botulinum toxin compared to free solution, protecting against conditions such as heat, alkaline environments, and degradative enzymes.
Enables effective self-administration, allowing for application outside medical settings and potentially increasing convenience for users.
Nanoemulsions maintain uniform and stable particle size over time, enhancing formulation reliability and efficacy.
Documented Applications
Cosmetic treatment of wrinkles, including facial lines, neck lines, and hyperkinetic facial lines.
Medical treatment of muscular contracture and overactivity, including neuromuscular disorders such as facial palsy, blepharospasm, dystonia, tremors, spasticity, cerebral palsy, and limb spasticity following stroke.
Treatment of hyperhidrosis (excessive sweating).
Treatment of prostate hyperplasia.
Alleviation of migraines.
Treatment of ophthalmic conditions, including strabismus and retroorbital muscle conditions.
Treatment of constipation.
Incorporation into topical formulations such as creams, gels, ointments, lotions, sprays, patches, and oils for use in cosmetic or medical contexts.
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