The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in January 2020.
Osmotic Delivery Systems and Piston Assemblies for Use Therein; T.R. Alessi, M.A. DesJardin, S. Lam, S.D. Lautenbach, and P.C. Zamora; Intarcia Therapeutics, Inc., US patent # 10,527,170; January 7, 2020.
Osmotic drug delivery systems have been studied for many decades. Osmosis can be defined as the net movement of water across a selectively permeable membrane driven by a difference in the osmotic pressure across the membrane. In this patent, the osmotic drug delivery system has a columnar body typically made up of a polymeric material. A piston assembly is positioned in the lumen to isolate the active agent formulation from the osmotic agent formulation. The device has a rim at the distal end for engaging and sealing against the interior wall of the reservoir, and a spring retained at the distal end. The piston is movable within the reservoir in response to pressure within the reservoir.
Pegylated Lipid Nanoparticle with Bioactive Lipophilic Compound; P. J. Gaillard and J. Rip; Eyesiu Medicines B.V., Leiden, NL; US Patent # 10,525,012; January 7 2020.
The present invention discloses compositions of stable, inert, clear and solvent-free lipid nanoparticles via systemic, ophthalmic and/or topical route for diagnostic and/or therapeutic use. It is comprised of a water-soluble polymer, a biocompatible lipid and a lipophilic agent. Hydrophobic nature of therapeutic compounds have poor solubility and bioavailability which is a major hurdle in their development. To overcome this hurdle, the use of high amounts of solubilizers, surfactants in new drug formulations, liposomes, emulsions and micelles have been used. The use of high amounts of surfactants and solubilizers also bring side effects with them. The invention disclosed here addresses the need of formulations for the treatment or alleviation of a skin, mucosal or eye disease or disorder, without causing (severe) side effects at the site of administration.
Drug Delivery Systems and Methods for Treatment of Bladder Cancer; D. Giesing; Taris Biomedical LLC, US Patent # 10,543,346; January 28, 2020.
In any cancer therapy, the goal is to minimize exposure of anti-cancer compounds to healthy tissues. Delivery of therapeutic agents to the urinary bladder is difficult. Typical system administration provides low exposure to the bladder and more exposure to healthy tissue. This patent covers local administration of oxaliplatin into the bladder. In one embodiment, a drug delivery device is inserted into the bladder to continuously release the drug. In another, a mucoadhesive formulation containing drug is delivered to the bladder which releases the drug over a long time. In another, a liquid form of oxaliplatin is pumped into the bladder. The patent also describes a device for intravesical administration of oxaliplatin.
Adiponectin Peptidomimetics for Treating Ocular Diseases; H. Hsu; Allysta Pharma, Belmont, CA; US Patent # 10,537,608; January 21, 2020.
Tears are distributed by blinking, undergo evaporation from the ocular surface, and drain through the nasal lacrimal duct. Tears comprise three layers: an innermost layer of hydrophilic mucin, a slimy substance produced by the goblet cells that coats the ocular surface epithelium; an aqueous tear layer produced by the lacrimal glands which floats on the mucin layer and is approximately 0.9% saline; and a superficial thin lipid layer produced by the Meibomian glands, which helps with uniform tear spreading and to slow down tear evaporation. The patent describes a formulation containing an adiponectin peptidomimetic compound and a suitable carrier. The formulation can also contain cyclosporine and an anti-inflammatory agent.
Subscribe to our e-Newsletters
Stay up to date with the latest news, articles, and events. Plus, get special offers
from American Pharmaceutical Review – all delivered right to your inbox! Sign up now!
Dermal Drug Delivery Using Amphiphilic Dendron-Coil Micelles; S. Hong and Y. Yang; The University of Illinois, Urbana, IL; US Patent # 10,543,171; January 28, 2020.
Polymeric micelles have been introduced as potential platforms for transdermal drug delivery due to their small size, skin permeability, biocompatibility, high drug and gene adaptability, tunable surface functionality and release profiles. Polymeric micelles are small, spherical particles (<200 nm in diameter) made up of polymer chains. These polymer chains are block copolymers (i.e., typically linear polymers that are composed of repeating blocks of two polymers that differ in hydrophilicity, charge or polarity). One of the most promising types of block copolymers capable of self-assembling is the dendron-coil (DC) Unlike linear polymers, a dendron offers multiple surface groups enabling multivalent interactions with other molecules including, for example, one or more drugs. The present invention provides methods of transdermal delivery of a drug (or drugs) to a patient by topically administering to the patient a composition comprising a micelle. In the methods, the micelle comprises amphiphilic dendron-coils that encapsulates the drug, and each amphiphilic dendron-coil comprises a hydrophobic core-forming block, a polyester Dendron and a poly(ethylene) glycol (PEG) moiety.
Method of and Apparatus for Formulating Multicomponent Drug; Y. Mori and K. Noda, Tsumura& Co, Tokyo, Japan; US Patent # 10,533,979; January 14, 2020.
Natural product-originated drugs such as “kampo” medicines are composed of multiple components. The quantitative and qualitative profiles of such drugs change due to a geological factor, an ecological factor, collecting season, a collecting area, weather during the growing period, and the like of raw material crude drugs. This patent describes a method of and an apparatus for formulating a multicomponent drug such as kampo medicine. The method and apparatus obtain a chromatogram from the multicomponent drug, evaluate whether the base meets the criteria for productization and subject the base which meets the criteria to produce a dosage-form.
Cancer Prevention and Therapy by Inhibiting Soluble Tumor Necrosis Factor; N.L. Vujanovic and L. Vujanovic; University of Pittsburgh; US Patent # 10,543,264; January 28, 2020.
Present invention discloses methods to inhibit development of tumors by administering a dominant negative tumor necrosis factor (DN-TNF)-alpha protein. Cancer is an abnormal state with an uncontrolled proliferation of one or more cell populations which interferes with normal biological functioning. Cancer is the second leading cause of mortality in the United States with over 1.2 million new cases diagnosed per year and causing death of well over a half-million people annually.