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 June-July, 2020.

Prosthetic Implantable Antibacterial Surgical Mesh; A.M.S. Altaf, S.A. Abdulhady, F. Abdel-Hady, and M.A.M. Yassien; King Abdulaziz University, Jeddah, SA; U.S. Patent # 10,688,224; June 23, 2020.

The present invention discloses an implantable surgical prosthetic mesh. The mesh has a nanofiber with one or more antibiotics and a polysaccharide. It also has a non-polysaccharide polymer deposited on the mesh. The mesh is shown to be effective in eliminating or minimizing the bacterial population in the mesh and surrounding tissue for at least 14 days from surgical implantation of the mesh. The nanofibers comprise: chitosan, one or more antibiotics and a polymer blend made from polyvinyl alcohol and polyvinylpyrrolidone. The nanofibers are formed by mixing a solution of chitosan with a solution of the antibiotic and the polymer blend. This solution mixture forms nanofibers by the electrospinning process. Nanofibers have an average diameter of 50 nm to 300 nm and a bore size of 300 nm to 900 nm. The antibiotic is released from the nanofibers steadily for at least 14 days.

Shape Memory Particles for Biomedical Uses; Q. Guo, J.J. Green, R.A. Meyer, C.J. Bishop, A. Kumar, and G.L. Semenza; Th e Johns Hopkins University, US; U.S. Patent # 10,695,427; June 30, 2020.

Shape memory polymers are unique in that they can undergo shape-transformations upon triggering by diff erent external stimuli such as heat, light and electricity. A major roadblock for such polymers for biomedical applications is the lack of biocompatibility of either the triggering environment or the shape memory polymers themselves. The present invention discloses a composition comprising an anisotropic shape memory particle with a drug loaded polymeric matrix and at least one stimulisensitive nanoparticle. Stimulating the stimuli-sensitive nanoparticle releases the drug from the anisotropic shape memory particle at a target location inside the patient and treats the disease or disorder in the patient.

Method of Forming Inorganic Nanocages; H. Matsui, Z. Wei, and J. Fang; Research Foundation of the City University of New York, US; U.S. Patent # 10,688,556; June 23, 2020.

Metal nanoparticles have been synthesized in various shapes due to their applications in medical imaging, medical therapeutics, catalysis and plasmonics. Synthesis of nanoparticles with sizes of 10 nm or less with specific shapes is a technical challenge. The present patent discloses a method of forming inorganic nanocages. Nanocages are formed by etching nanocubes. The nanocubes are added to an aqueous system having an amphiphilic lipid dissolved in an organic solvent (e.g., a hydrophobic alcohol) to form reverse micelles. As the water evaporates the micelles shrink as etching of the flat surface of the nanocubes occurs. In this way hollow nanocages are produced. The nanocage is covalently attached to a polymer shell (e.g., a dextran shell).

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Combination Vaccine Devices and Methods of Killing Cancer Cells; O.A.R. Ali, D.J. Mooney, and G. Dranoff ; President and Fellows of Harvard College, Dana-Farber Cancer Institute; U.S. Patent # 10,682,400; June 16, 2020.

Many cancers are hard to treat because they use the host immune system for their own purpose. One-way cancer cells evade the immune system is by upregulating immune-inhibitory proteins. Agents that block these immune-inhibitory proteins have been explored as potential therapies that reenable the endogenous antitumor immune response. These agents when used alone are ineffective in killing poorly immunogenic tumors. The present invention discloses compositions, methods, and devices for enhancing an endogenous immune response against a cancer. The device comprises an inhibitor of an immune-inhibitory protein; a scaffold composition; a cell recruitment composition; and a bioactive composition, where the bioactive composition is incorporated into or coated onto the scaff old composition, and where the bioactive composition causes modification of cells in or recruited to the device.

Zinc Meloxicam Complex Microparticle Multivesicular Liposome Formulations and Processes for Making the Same; L.D. Garcia, S. Kurz, S. Ardekani, K.D.A. Los, K. Stone, E.G. Schutt, and V. Kharitonov; Pacira Pharm., San Diego, US; U.S. Patent # 10,709,665; July 14, 2020.

Meloxicam is a non-steroidal anti-inflammatory drug, which helps to reduce pain, inflammation and fever. Some of the major side-effects of meloxicam are – abdominal pain, diarrhea, heartburn, headache, and itching. The present invention describes meloxicam divalent metal complexes encapsulated in multivesicular liposome (MVL) formulations. Complexation with zinc improves the liposomal encapsulation of meloxicam and minimizes side effects with an improvement in efficacy by extended release. Some portion of zinc meloxicam is present in a microcrystalline form. Zinc meloxicam is generated by mixing the solution of meloxicam with the solution containing a suitable zinc salt.

Ophthalmic Compositions of Cyclosporine; G.S. Rangabhatla, K. Vara Prasad, A. Sandeep and P. Ratna; Shilpa Medicare Ltd., Raichur, India; U.S. Patent # 10,702,578, July 7, 2020.

The present invention relates to an ophthalmic composition containing 0.03 to 2% cyclosporine, 0.05 to 5% tamarind seed polysaccharide and a carrier. The molecular weight of tamarind seed polysaccharide is from 450,000 Da to about 750,000 Da. The formulations may also contain other excipients such as HPMC, and polysorbate 80. Tamarind seed polysaccharide is also known as xyloglucan. This formulation was shown to be less toxic and more biocompatible with more emphasis on the biomimetic approach for the treatment of dry eye disease.

Petrolatum-Based Delivery Systems and for Active Ingredients; B. Burnam; Global Health Solutions, Rome, GA; U.S. Patent # 10,722,461; July 28, 2020.

Petroleum jelly is commonly used in topical formulations, mainly ointments. An independent claim in the patents mentions more than 80% of petroleum jelly, a polar solvent and active ingredients are soluble in the polar solvent. Polar solvent containing actives are mixed with petroleum jelly. The polar solvent is dispersed as small droplets producing an emulsion. This emulsion does not need any emulsifier. It is emphasized that the active ingredients do not react with petroleum jelly. Also, the active ingredients stay well suspended in the matrix and do not separate.

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