The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office from August-September 2020.
Orally Bioavailable Lipid-Based Constructs;
W.B. Geho and J.R. Lau; SDG, Inc., Cleveland, OH; U.S. Patent # 10,751,418; August 25, 2020.
Among the various drug delivery routes, oral formulation is one of the preferred methods. One of the major glitches in the oral formulation of many pharmaceutical compounds such as peptides, proteins, certain small molecules, and nucleic acids is the compound’s incompatibility with the harsh environment of the digestive tract. The present invention includes compositions that facilitate and/or enable absorption of therapeutics, which are not typically orally bioavailable. A composition of the present invention is comprised of various lipid-based constituents, at least one therapeutic or diagnostic agent, an optional targeting molecule, and an optional, RES masking agent. Lipid-based constituents include liposomes, liposome fragments, and lipid particles. Targeting agents alter the composition’s bio-distribution and enhances the efficacy of an associated therapeutic agent.
Liquid Polymer Delivery System for Extended Administration of Drugs;
J.M. Downing, V. Saxena, and J. Middleton; Tolmar International Ltd., Dublin, IE; U.S. Patent # 10,786,515; September 29, 2020.
Earlier polymers used in drug delivery (DD) systems were all solids. The DD devices were prepared outside and then inserted in the body. In the next generation formulations, polymers were dissolved in solvents but produced viscous solutions. Low viscosity polymeric solutions produce an initial burst of drug release followed by a slower release up to 14 days. The present patent describes a liquid polymer composition comprising a biodegradable polymer with one carboxylic acid end group, a biocompatible organic solvent and an active pharmaceutical ingredient. With the system, a steady state release of drug was obtained for over two months.
Pharmaceutical Suspensions Containing Drug Particles, Devices for their Administration, and Methods of their Use;
A. Heller and J. Spiridigliozzi; SynAgile Corp., Wilson, NY; U.S. Patent # 10,786,474; September 29, 2020.
The present invention describes a pharmaceutical suspension containing drug particles, a drug delivery device anchored in the mouth for continuously administering the pharmaceutical suspension, and methods of their use. Continuous and semicontinuous administration is beneficial for drugs with a short half-life or a narrow therapeutic window. The invention features a pharmaceutical composition, which is physically stable and suitable for continuous or frequent intermittent intra-oral delivery. The invention also describes a drug delivery system. The device is configured to be removably inserted in a patient’s mouth. The device includes: (i) a fastener to removably secure the drug delivery device to a surface in patient’s mouth; (ii) an electrical or mechanical pump; (iii) an oral liquid impermeable drug reservoir containing any of the pharmaceutical compositions of the invention and (iv) an automatic stop/start device, which includes a propellent driven pump and rigid housing. The volume of the drug reservoir can be from 0.1 mL to 5 mL.
Mucus Penetrating Gene Carriers;
J.S. Suk and J.S. Hanes; Th e Johns Hopkins University, Baltimore, US; U.S. Patent # 10,729,786; August 4, 2020.
This patent describes the delivery of drugs across the mucus membrane to treat Cystic Fibrosis (CF). CF patients develop highly adhesive and hyper-viscoelastic sputum that can immobilize and trap gene carriers, thereby greatly reducing the flux of gene carriers that can reach the airway epithelium. The CF sputum contains mucin fiber, large macromolecules containing negatively charged glycans and hydrophobic regions. The pore size of CF sputum is about 145 nm. The patent includes nanoparticles comprising a mixture of a) branched polycationic polymers, and b) mucus-resistant/ diffusive graft co-polymers consisting of the branched polycationic polymers covalently coupled to polyalkylene glycol polymers. The surface charge of the nanoparticles has a zeta-potential of between about 5 mV and about -5 mV, and the average diameter of between 50 and 500 nm.
Method of Producing Particles;
S. Onoue, H. Sato, Y. Seto, T. Moritani, and T. Morinaga; Ricoh Co. and Shizuoka Prefectural University Corp., Japan; U.S. Patent # 10,772,836; September 15, 2020.
The present invention describes a method of producing pharmaceutical particles. Pulverization and emulsification methods are two of the known methods used for producing pharmaceutical particles. Both the methods have different limitations. The present invention provides a method for producing particles, which will have narrow particle size distribution and improved properties. The method includes applying vibration to a liquid including a physiologically active substance and included in a liquid column resonance liquid-chamber to form a standing wave based on liquid column resonance, to thereby discharge the liquid from at least one discharging port, which is formed in an amplitude direction of the standing wave, to at least one region corresponding to at least one anti-node of the standing wave; and drying the liquid discharged, to thereby form particles.
Herbal Formulations of Carnivorous Plants and Methods for Treating Inflammation;
B. Gowey; Gowey Research Group, PLLC, Flagstaff , AZ; U.S. Patent # 10,758,578; September 1, 2020.
The present invention features formulations and methods of treatment using herbal formulations containing carnivorous plants - pitcher plants such as Sarracenia flava and Sarracenia purpurea. Sarracenia flava is supposedly toxic since it contains the neurotoxin, coniine. However, the present invention has discovered that topical administration of the Sarracenia flava preparation to mammals can induce healing effects. Topical herbal preparation of the carnivorous plant contains glutathione, and it is effective for facilitating transmission of glutathione to fibroblast growth factors. The formulation increases fibroblast growth factors at measurable levels and adjusting fibrinogen levels to homeostatic levels in the subject, thereby ameliorating symptoms of and reducing inflammation in the subject.
Microparticles and Nanoparticles Having Negative Surface Charges;
B. Wu; Phosphorex, Inc., Hopkinton, MA; U.S. Patent # 10,780,053; September 22, 2020.
The patent describes preparation of a composition comprising microparticles or nanoparticles having negative surface charges. The method involves dissolving water-soluble polyacrylic acid and polyvinyl alcohol in an aqueous solution having pH between 8 and 12. PLGA is dissolved in a volatile solvent, which is not soluble or miscible with the aqueous solvent. An emulsion is formed, and the volatile is removed to provide nanoparticles having a zeta potential of from about -35mV to -85 mV. The emulsification process includes microfluidization.