Botulinum nanoemulsions
Inventors
Edelson, Jonathan • Nicolosi, Robert
Assignees
University of Massachusetts Lowell
Publication Number
US-10532019-B2
Publication Date
2020-01-14
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 nanoparticle compositions, specifically nanoemulsions, containing botulinum toxin for cosmetic and medical applications. These nanoemulsions are characterized by a particle size distribution exclusively within the nanometer range, with specific embodiments describing particles between 10 and 300 nanometers in diameter. The nanoemulsions are prepared using processes such as high pressure microfluidization, resulting in uniform and stable particles suitable for administration by various routes including injection and transdermal delivery.
The core problem addressed by this invention is the adverse effects and challenges associated with current botulinum toxin delivery methods, which rely primarily on injection techniques. Such methods can cause tissue damage, unintended delivery to undesirable locations, pain, hematoma, ecchymosis, and bruising. There remains a need for improved systems and formulations that can provide safer, more effective, and user-friendly delivery of botulinum toxin.
The invention overcomes these limitations by formulating botulinum toxin in nanoemulsion form, which enables efficient transdermal delivery without requiring chemical or mechanical disruption of the skin. This allows for topical cosmetic formulations that may be self-administered without medical supervision while maintaining or improving stability and bioactivity of the botulinum toxin. The compositions are suitable for a variety of medical and cosmetic uses, such as smoothing wrinkles, treating hyperhidrosis, and addressing muscular contracture states.
Claims Coverage
The patent contains one independent claim, which introduces several inventive features regarding the composition and formulation of botulinum toxin nanoemulsions.
Sterile liquid pharmaceutical nanoemulsion with botulinum toxin
The pharmaceutical composition is a sterile liquid formulated for administration by injection. It comprises a nanoparticle composition that is an oil-in-water or water-in-oil nanoemulsion, in which oily particles are dispersed within an aqueous dispersion medium or vice versa. The composition contains: - An oil - An aqueous medium - A surfactant - Botulinum toxin The oil and surfactant are present at a ratio within a range of 0.5–2.
The inventive features are focused on a specifically formulated nanoemulsion comprising botulinum toxin, oil, aqueous medium and surfactant, with a defined oil-to-surfactant ratio, suitable for sterile pharmaceutical injection.
Stated Advantages
Improved stability of botulinum toxin, protecting it from heat, alkaline or acidic conditions, degradative enzymes, and host organism antibodies.
Transdermal delivery is achieved without alteration or irritation of the skin, as abrasive agents or permeation enhancers are not required.
Reduction and minimization of adverse side effects associated with conventional injection, such as pain, tissue damage, bruising, and injection-site complications.
Compositions are suitable for self-administration and do not require medical supervision.
Nanoemulsions provide improved membrane permeability, leading to enhanced delivery and efficacy.
Compositions are stable over prolonged periods of time under a variety of conditions.
Nanoemulsions are substantially free of toxic solvents and may also be free of polymers.
Documented Applications
Cosmetic treatment to smooth facial wrinkles and reduce unsightly facial expressions.
Medical treatment of muscular contracture states.
Treatment of hyperhidrosis (excessive sweating).
Relief of neuromuscular disorders, including use in treating conditions such as palsy, dystonia, hemifacial spasm, tremor, spasticity, cerebral palsy, and contractures.
Treatment of facial palsy, blepharospasm, strabismus, and dystonia.
Treatment of benign prostatic hyperplasia.
Topical application for delaying onset or reducing severity of wrinkles and muscle overactivity.
Formulation in transdermal patches or cosmetic products (e.g., creams, gels) for both medical and cosmetic applications.
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