The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in October-November 2021.
Neelam Sharma, MS, Lavanya Kundurthy, and Hemant N. Joshi, Ph.D., MBA*
Tara Innovations, LLC, www.tarainovations.com and www.tara-marketing.com
*[email protected]
Methods for Improving Safety of Blood-Brain Barrier Transport; R.J. Watts, J. Yu Zuchero, J. Couch and M. Dennis; Genentech, Inc., US; U.S. Patent # 11,167,038; November 9, 2021.
The blood vessels that vascularize the central nervous system (CNS) possess unique properties, termed the blood–brain barrier (BBB). BBB allows these vessels to tightly regulate the movement of ions, molecules between the blood and the brain. Brain penetration of large molecule drugs is severely limited by impermeable BBB. Utilizing transcytosis trafficking pathways of endogenous receptors expressed at the brain capillary endothelium is one way to overcome BBB obstacle. Monoclonal antibodies have been designed towards these receptors to enable receptor-mediated delivery of large molecules to the brain. However, the safety of administration of such antibodies and conjugates has not been fully understood. The present invention relates to compositions and methods for improving the safety of BBB receptor-mediated transport.
Compositions and Methods for Treating SARS-CoV-2 Infections; V. C. Bond, M.B. Huang, and J.W. Lillard, Jr.; Morehouse School of Medicine, US; U.S. Patent # 11,180,534; November 23, 2021.
This application relates to methods for treating viral infections. More particularly, to an antiviral composition comprising a multipartite virus inhibiting secretion modulating region (VI-SMR) peptide for treatment and prevention of SARS-CoV-2 viral infections. A method for treating a SARS-CoV-2 infection or reducing the viral load comprises administering to the subject infected with SARS-CoV-2 an effective amount of a pharmaceutical composition comprising a VI-SMR peptide comprising an SMR peptide from HIV-1 Nef in combination with a CPP, a Clu-BP, or both, where the VI-SMR peptide further comprises an anti-SARS-CoV-2 AF peptide, an anti-SARS-CoV-2 VAI peptide, or both.A method for reducing viral load in a SARS-CoV-2 infected patient can results in at least a 2 or 3 log.sub.10 reduction in viral RNA copies per mg of lung tissue compared to a negative control.
Composition for Enteric Hard Capsule and Method for Producing Enteric Hard Capsule; N. Maruyama; Shin-Etsu Chemical Co. Ltd., Japan; U.S. Patent # 11,141,381; October 12, 2021.
Gelatin or HPMC capsules are unsuitable for pharmaceutical products which are unstable in an acid or irritate the stomach. In such cases, hard capsules with enteric polymer coating are used. But this additional coating step results in low productivity and high cost. To address this problem, a hard capsule has been developed by using an enteric polymer itself as a capsule base material. Each conventional method of producing enteric hard capsules requires a water-soluble gelling agent. There is a problem that the resulting enteric capsules exhibit insufficient water resistance or acid resistance. This patent provides a method for producing an enteric hard capsule by taking advantage of conventionally unknown thermal gelation characteristics of a neutralized aqueous solution of an enteric polymer. The resulting enteric capsule shows sufficient water resistance and acid resistance. The inventors have found that certain HPMCAS has excellent thermal gelation characteristics. The HPMCAS having a particular substitution degree is used as the base material for an enteric hard capsule.
Self-Emulsifying Formulation of Bisphosphonates and Associated Dosage Forms; X. Yuan, Y. Hui, and T. Zhang; Halo Science LLC, US; U.S. Patent # 11,173,169; November 16, 2021.
Bisphosphonates are therapeutic agents with strong affinity for bones. Bisphosphonates or "bisphosphonic acids" are used in the diagnosis and treatment of disorders and conditions related to bone resorption, calcium metabolism and phosphate metabolism. Bisphosphonates inhibit the digestion of bone by encouraging osteoclasts to undergo apoptosis, or cell death, thereby slowing bone loss. Oral administration of bisphosphonic acids shows adverse gastrointestinal effect. Also, they have low oral bioavailability. The present invention relates to drug delivery of novel self-emulsifying formulations of bisphosphonates or bisphosphonic acids. The invention also relates to dosage forms or other controlled release drug delivery systems. The self-emulsifying formulation and controlled release system will modify the interaction between active agent and digestive tract. The self- emulsifying formulation helps to lessen GI side-effects, but also improve drug bioavailability.
Foam-Forming Compositions for Delivering an Active to a Body Cavity; A.R. Lindal, and D.B.I. Sagna; Pharmiva AB; Sweden; U.S. Patent# 11,135,166; October 5, 2021.
The patent describes a foam-forming composition for application to skin, wounds and body cavities. When blown, it forms a foam and the foam melts at a body temperature to release the content. Foam has low density, which makes the administration to sensitive areas less painful and it easily spreads over large surface. The formulation contains water, solid lipid crystals with melting point between 25°C to 37°C and a non-lipophilic propellent to form the foam. The foam can be manufactured by two modes. One is during the manufacturing process by mixing polar gases into the product and the product is then stored in the form of a foam at normal pressure. The other way is to introduce a blowing gas into the formulation and to store the product at elevated pressure, up to 10 bar, in a pressurized can.
Transdermal Non-Aqueous Nanoemulgels for Systemic Delivery of Aromatase Inhibitor; A.A.N. Sallam, and H.M. Younes; Qatar University, Qatar; U.S. Patent # 11,185,504; November 30, 2021.
Some breast cancers require estrogen to continue growing. Aromatase is the enzyme that synthesizes estrogen and aromatase inhibitors inhibit the enzyme. The present invention describes non-aqueous nanoemulgels for topical or transdermal delivery of potent drugs, particularly aromatase inhibitors such as letrozole and anastrozole. Nanoemulgels has an emulsion in the nano scale and a gel base, both combined as a single formulation. The nanoemulsion part protects the drug from degradation. The oily phase comprises glyceryl monooleate (GMO) and isohexadecane and the emulsifying gelling agent is SEPINEO P 600. The inventors used propylene glycol and diethylene glycol ethyl ether as cosolvents, the cosolvents form nanoglobules of the oily dispersed phase.
Capsule for Drug Delivery Systems of Targeted Tissue-Specific Delivery Type Using Carbosilane Dendrimer; M. Suzuki, K. Hatano, S. Yoshida, Y. Yamashita; Saitama University and Quarrymen & Co. Inc., Japan; U.S. Patent # 11,160,877; November 2, 2021.
This patent does not discuss a typical hard-shell capsule. The invention provides an endocytosis enhancing agent by using carbosilane dendrimer for the drug delivery system; which is stable in the living body and enables it to specifically deliver the active ingredient to the target tissue, and it further enhances the incorporation of a compound having a variety of molecular weight or biopolymers into the cells. In the patent, a target sequence presented part (TSPP) is composed of a fluorescent protein, and a protein or peptide for a target tissue specific delivery; and wherein said endocytosis enhancing agent comprises a space for containing an aqueous solvent or organic solvent inside of a capsule being composed of said aggregatable molecule, and said space encapsulates a protein having molecular weight of 200,000 daltons or less or peptide dissolved in said aqueous solvent, or a hydrophobic molecule dissolved in said organic solvent. The capsule has diameter from 50 to 500 nm.
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