Pharmaceutical P.I.N. Points Patent Innovation News

The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in March 2021.

By: Neelam Sharma, MS and Hemant N. Joshi, PhD, MBA* - Tara Innovations, LLC

www.tarainovations.com and www.tara-marketing.com - *[email protected]

Nozzles for Nasal Drug Delivery; J.D. Hoekman, M. Hite, A. Brunelle, and J. Relethford; Impel Neuropharma, Inc., Seattle, US; U.S. Patent # 10,940,278; March 9, 2021.

Existing nasal drug delivery devices do not adequately deposit drug in the posterior regions of the nasal cavity such as the respiratory epithelium and olfactory region. Current devices generate a wide plume, which inadequately delivers a compound deep into the nasal cavity. The nozzles described in the patent enhance the drug deposition by consistently depositing at least a majority fraction of the dose into the distal parts of the nasal cavity. The nozzle includes a drug product inlet configured to receive a mixture of aerosolized propellant and an intranasal dosage form. The inlet is disposed at the proximal end. A nozzle body is secured to the drug product inlet. Two or more channels are disposed within the body. Two or more orifice apertures are disposed at the distal end of the nozzle.

Compositions and Methods for Ophthalmic and/or Other Applications; A. Popov, E.M. Enlow, H. Chen, and J. Bourassa; The Johns Hopkins University, USA; US Patent # 10,945,948; March 16, 2021.

Mucus helps to trap allergens, pathogens etc. and remove them by rapid turnover. This creates a hurdle delivering drugs across mucus. The patent describes an ophthalmic suspension of loteprednol comprising (a) a plurality of coated nanoparticles, sodium chloride, glycerin, EDTA, sodium citrate, ferric acid and water. The pH of the formulation is in the range of 5 to 7. Loteprednol nanoparticles are coated with poloxamer 407. Poloxamer acts as a surface-altering agent that reduces adhesion of the particles to mucus and facilitates their penetration through mucus. As a result, the drug is more effectively delivered and retained longer in the target tissue.

Multi-Catheter Infusion System and Method Thereof; S. Memtsoudis; Hospital for Special Surgery, New York, US; US Patent # 10,960,176; March 30, 2021.

Catheters are medical devices that can be inserted in the body to treat diseases or perform a surgical procedure. The present invention relates to a multi-catheter infusion system used for the administration of local anesthetics or other fluids (including but not limited to antibiotics or pain relief drugs) to a patient. Present patent addresses the limitations of conventional drug delivery systems. The multi-catheter infusion system includes a cannula and a plurality of catheters. The cannula includes a first end and the second end. First end for connecting to a drug delivery system and a second end for connecting to the plurality of catheters. The plurality of catheters is in fluid communication with the cannula for delivering a drug to a target area of a patient. Each catheter includes a multi-orifice distal end.

Methods of Treating SARS Cov-2 Virus with Protocatechuic Acid; L.L. Johnson; Private patent; US Patent # 10,959,969; March 30, 2021.

Protocatechuic acid (PCA) is chemically dihydroxy benzoic acid. It is known for its antioxidant and anti-inflammatory properties. PCA has been reported to induce apoptosis of human leukemia cells. It is present in many herbs including Roselle. Coronavirus is surrounded by many projections or spikes, which are the virulent contact agent with the host cell. The spikes and underlying thin wall coating of the viral body are vulnerable to physical disruption. Physical disruption is thus one potential method of stopping the cellular invasion and the clinical disease. The inventor has patented a composition comprising PCA crystals. PCA is administered in a pharmaceutically acceptable carrier in a biodegradable microsphere or a slow release bioabsorbable material. The daily dose is about 500 mg to 1000 mg.

Anti-Microbial Immunomodulation; H.D. Gunn, S. Dhanji, and D.W. Mullins; Qu Biologics, Inc., US; US Patent # 10, 946,083; March 16, 2021.

The innate immune system and the adaptive immune system provide protection from pathogenic infection by micro-organisms. Multivalent vaccines may be used to elicit a specific adaptive response to more than one serovar. This patent claims to be a method to modulate an immune system for the prophylactic treatment of an infection by a first microbial pathogen in a target tissue. The method comprises of administering the host with an effective amount of an antigenic formulation comprising antigenic determinants specific to a second heterologous microbial pathogen. The antigenic determinant could be whole cells or cell wall extracts. The target tissue here is lungs. the first microbial pathogen is Moraxella catarrhalis, Mycoplasma pneumoniae, or Haemophilus influenza and the second heterologous microbial pathogen is a Klebsiella pneumonia.

Surfactant-Free Water-Free Foamable Compositions, Breakable Foams and Gels and Their Uses; D. Tamarkin, E. Gazal, I. Papiashvili, Y. Hazot, D. Schuz, and R. Keynan; Vyne Pharmaceuticals, IL, USA; US Patent # 10,946,101; March 16, 2021.

This patent involves a method for treating rosacea with a surfactant-free foam composition. A significant amount of surfactant is needed to form foam. Drugs and other components may destabilize the foam. The present application relates to oleaginous foamable formulations with hydrophobic solvents. The application further describes semi-solid gel compositions that liquefy oil application of mild shear force such as gentle rubbing. The composition consists of: (i) a carrier with a hydrophobic solvent, at least one fatty alcohol, at least one fatty acid, at least one wax, (ii) an active agent, and (iii) a liquefied or compressed gas propellant. The foamable composition is free of polymeric agent.

Implants and Constructs Including Hollow Fibers; M.E. Labib, S.S. Dukhin, P. Materna, J.C. Robertson, C.Y. Lai, and Y. Tabani; Novafl ux Inc., US; US Patent # 10,952,961; March 23, 2021.

Various technologies exist for the controlled delivery of drugs to patients. For example, implanted fabric or meshes can be coated with small molecule drugs or biologics prior to implantation or drugs can be blended or impregnated into the fibers of a degradable (resorbable) fabric or mesh. Such drug delivery systems work but they have their own limitations. Present patent describes the implants and constructs including hollow fibers. Device can contain structural or solid fibers. All or some of the fibers can be resorbable. Fibers can be subdivided into numerous compartments that separately deliver drug. Deformations can be located at points of fiber intersection or joining. Different drug or drug formulations can be provided in different places. Fibers can be given appropriate surface treatments or coatings to achieve desired properties such as wetting of pores and surfaces. Different release characteristics in different directions can be achieved. The hollow fibers can contain solid particles of drug and can contain gel. Possible applications include hernia meshes, pouches, sutures, catheters, wound dressings, stents, nerve regrowth guides, refillable/drainable devices, and devices that deliver drug to lymphatic flow.

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