The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office.
Amyloid Binding Agents; J. Yang, and E.A. Theodorakis; The Regents of the University of California; U.S. Patent # 9,551,722; January 24, 2017.
The patent provides the compounds, methods for detection and treatment of disease related to amyloidbased neurodegenerative diseases. Alzheimer’s disease (AD) is a well known neurodegenerative disorder and is characterized by accumulation of amyloid (A.beta.) peptides in the brain. While the exact three-dimensional structure of the aggregated A.beta. peptides is not known, a model structure that sustains the property of aggregation has been proposed. This creates opportunities for in vivo imaging of amyloid deposits that not only can help evaluate the time course and evolution of the disease but can also allow the timely monitoring of therapeutic treatments. The patent claims the method of detecting amyloid peptide wherein contacting compound as described herein with an amyloid peptide thereby forming a detectable amyloid complex, and therefore detecting the detectable amyloid complex.
Medical Devices Containing Therapeutic Agents; J. Clarke, T. O’Connor, B.J. O’Brien, D. McMorrow, J. Weber, and A. Flanagan; Boston Scientific Scimed, Inc.; U.S. Patent # 9,533,078; January 3, 2017.
The present invention claims an implantable or insertable medical device, which comprises of a substrate and one or more therapeutic-agent-containing regions where one or more characteristics of such regions, like the composition, the crystalline, the size, the shape, the spatial distribution over the substrate, the total dose associated, the rate of drug release and the adhesion to the underlying substrate are controlled. Other aspects of the invention relate to methods of forming such devices and to methods of using such devices. The medical device is comprised of a discontinuous layer of therapeuticagent called the first area and an inorganic nanoporous layer disposed over the therapeutic-agent-containing layer called the second area.
Targeted Delivery of Anti-Fungal Agents; T. Meehan, and Q. Ong; EDH Biotech Corp; U.S. Patent # 9,539,273; January 10, 2017.
Antigen-antibody reaction is used widely for targeted drug delivery systems. Lability of the reagent and size limitations are some of the drawbacks. The inventors found that derivatives of stilbenes bind strongly to chitosan, model chitin in fungal cells. The advantages of the stilbene-derived targeting agents include high target affinity, stability, nontoxicity, and small molecular size. Fungi express chitin in their cell walls, a component unique to pathogenic and other fungi. Additional approaches for synthesizing and assembling stilbene-derived, targeted nanoparticles that encapsulate antifungal drugs, such as Amphotericin B, for targeted drug delivery to organisms containing chitin-like substances have been presented. Chitin-targeted dendrimers have been shown to be very efficient at killing S. cerevisiae in liquid cultures compared to non-targeted dendrimers.
Sustained Release of Nutrients in vivo; F. Sexton, S. Krishnan, V.K. Vendra; New World Pharmaceuticals LLC; U.S. Patent # 9,538,775; January 10, 2017.
The invention relates to compositions for increasing performance of athletes by providing appropriately timed release and increased absorption of nutrients including carbohydrates, amino acids, and electrolytes. The patent claims nutritional supplements consisting of a hydrogel particle, which has a diameter less than or equal to about 1000 µm. The particle comprises at least one biologically active agent, one or more compounds which are non-toxic and are crosslinked, for time controlled and sustained release of the biologically active agent in vivo and at least one compound that is pH-sensitive and does not swell at pH 1-3 and at least one compound that is temperature-sensitive.
Nanocrystals, Compositions, and Methods that Aid Particle Transport in Mucus; A. Popov, E.M. Enlow, J. Bourassa, C. R. Gardner, H. Chen, L.M. Ensign, S.K. Lai, T. Yu, J. Hanes, and M. Yang; Kala Pharmaceuticals, Inc. and The Johns Hopkins University; U.S. Patent # 9,532,955; January 3, 2017.
A mucus layer present at various points of entry into the body is naturally adhesive and serves to protect the body against pathogens, allergens, and debris by effectively trapping and quickly removing them via mucus turnover. For effective delivery of therapeutic, diagnostic, or imaging particles via mucus membranes, the particles must be able to readily penetrate the mucus layer to avoid mucus adhesion and rapid mucus clearance. Several lines of evidence suggest that conventional nanoparticles are not capable of crossing mucosal barriers. The present invention describes the compositions and methods involved in making mucus-penetrating particles (MPP) without any polymeric carriers, or with minimal use of polymeric carriers. The patent claims the composition comprising coated particles containing a solid pharmaceutical agent or a salt and a coating comprising a surface-altering agent surrounding the core particles, which is covalently attached to the core particle or non-covalently adsorbed to the core particles.
Transdermal Delivery of High Viscosity Bioactive Agents; R.F. Ross; Kimberly-Clark Worldwide, Inc., U.S. Patent # 9,550,053, January 24, 2017.
High viscosity compositions loaded with drugs are delivered via oral or injectable routes. In both cases, there are many obstacles. In this patent, a transdermal delivery device has been developed to provide a painless route. The patent claims a device for delivery of a bioactive agent across a dermal barrier. This device is comprised of a microneedle and a plurality of nanostructures fabricated on a surface of the microneedle, the nanostructures being arranged in a predetermined pattern, wherein at least a portion of the nanostructures have a cross-sectional dimension of less than about 500 nm and greater than about 5 nm and an aspect ratio of from about 0.2 to about 5. The microneedle further contains a channel; and a reservoir that is in fluid communication with the channel of the microneedle and that contains a composition having a viscosity of greater than about 5 centipoise and comprising a bioactive agent.
Dosage Form to Increase Prasterone Bioavailability; J.M. Pohl; Health Science Funding, LLC, US Patent # 9,550,804; January 24, 2017.
Prasterone, also known as dehydroepiandrosterone, or DHEA is a dietary supplement. DHEA is a pro-hormone produced in the body. It is mostly promoted to replace DHEA in the body that declines with aging. This invention provides a way to formulate prasterone to both increase its oral bioavailability, and decrease the variability of its oral bioavailability. The claim includes administration of prasterone to a female patient with a risk of breast cancer. Micronization of the active pharmaceutical can increase the surface area and improve bioavailability. However, upon compression, prasterone particle size may increase by agglomeration. The inventor proposed to coat the micronized particles with a durable liquid vehicle such as tocopherol, fish oil, olive oil etc. The inventor also proposed the use of a soft gelatin capsule.