The purpose of this column is to highlight and summarize recent key patents in the pharmaceutical arena issued by the US Patent Office in February 2020.
Theranostic Compositions and Uses Thereof; J.Y. Wong, R.D. Whitaker, N. Ruiz-Opazo, and V.L.M. Herrera; Boston University, US; US Patent # 10,568,970; February 25, 2020.
Compositions which have dual functionality, as a diagnostic reagent and a drug delivery agent, are known as theranostic agents. These agents are useful in both imaging and treatment of diseases. The present invention discloses compositions and methods useful in delivering nucleic acid agents to solve genetic heterogeneity in diseases, such as cancer, that do not respond to conventional treatments. Compositions disclosed herein comprise a microbubble with a Janus nanoparticle. The Janus nanoparticle is an asymmetrical nanoparticle and comprises an ultrasmall super-paramagnetic iron oxide nanoparticle (USPION). It has a nucleic acid delivery face and a targeting face, both distinct from one another. USPION is less than 50 nm in size. The nucleic acid delivery face comprises a nucleic acid molecule that is sandwiched between the microbubble and the Janus nanoparticle.
Modified Release Composition of Orlistat and Acarbose for the Treatment of Obesity and Related Metabolic Disorders; G. Alderborn, A. Forslund, U. Holmback, H.Lennernas, and J.S.P. Gruden; Empros Pharma AB, Solna, SE; US Patent # 10,561,617; February 18, 2020.
Orlistat is available as brand names Alli and Xenical. It helps patients reach and maintain a healthy weight. By blocking lipase, it prevents breakdown of fats prior to absorption. Acarbose is a diabetes medication and it is available as Precose. In this patent, there are four distinct parts and different drug-release patterns – G1 and G2A containing Acarbose and G2B and G3 containing Orlistat. Part G1 is for the delayed release of Acarbose. Parts G2A and G2B release Acarbose and Orlistat in the proximal small intestine rapidly. Part G3 releases Orlistat slowly.
Self-Assembled Gels for Controlled Delivery of Encapsulated Agents to Cartilage; J. Karp, N. Joshi, X. He, S. Bhagchandani; The Brigham and Women’s Hospital, Inc., US; US Patent # 10,568,840; February 25, 2020.
Present invention discloses a gel which can adhere to cartilage tissue - hyaline cartilage or articular cartilage. It provides a biocompatible gel composition for good adhesion, integration with cartilage tissue and controlled delivery of therapeutic agents. It can also be used in treating damaged cartilages. According to the patent, cartilage may be damaged through acute injury or degeneration over time. For example, osteoarthritis (OA) is a joint disorder that leads to thinning of cartilage and progressive joint damage. Nearly 40% of Americans over the age of 45 have some degree of knee OA, and those numbers are expected to grow as the population ages. The gel disclosed herein has an amphiphilic gelator and a cationic agent in its composition. Gelator in this composition is an enzyme-cleavable, generally recognized as safe (GRAS) compound.
Delivery of Active Agents Using a Chocolate Vehicle; K.W. Lang; Lesaffre Yeast Corporation, US; US Patent # 10,555,544; February 11, 2020.
Chocolate is well-suited as a vehicle for delivering active agents as it offers many advantages. The organoleptic characteristics of chocolate are excellent for masking unpleasant flavors associated with some active agents. Chocolate also imparts a smooth and creamy texture to the compositions that are otherwise undesirably gritty. Chocolate is a substantially anhydrous medium and it is resistant to microbial growth and to hydrolysis of water-sensitive active agents. Despite these advantages, chocolate has not found commercial acceptance as a pharmaceutical or nutraceutical delivery vehicle. The present patent provides the compositions comprising chocolate or chocolate compound as a delivery vehicle for active agents. Chocolate dosage forms may be formulated by carefully controlling the particle size of the active agent.
Star Polymers with Enhanced Antimicrobial Activity in Response to Light; W.Chin, J.L. Hedrick, N.F. Fine Nathel, V.A. Piunova, Z.X. Voo, and Y.Y. Yang; IBM Agency for Science, Technology and Research, US; US Patent # 10,561,146; February 18, 2020.
Bacterial infection is a significant threat to human health. Fighting against harmful bacteria is a great challenge due to development of resistance to antibiotics. As an alternative to conventional antibiotic techniques, reactive oxygen species (ROS) can exhibit strong antimicrobial, antiviral and antifungal activities. It can be toxic to various pathogens. But the conventional ROS can be unstable and can be equally toxic against host cells. The present patent disclosed the techniques regarding a star polymer with light activated enhanced antimicrobial functionality. For example, a polymer is provided that can comprise a plurality of degradable polycarbonate arms and the arms comprise of cations. Polycarbonate arms can have antimicrobial functionality. Further the polymer can comprise a singlet oxygen generator loaded within the core. The singlet oxygen generator can generate a single oxygen species in response to light. Cationic polymers can adhere to the negatively charged surface of bacteria. This contact of pathogen with the polymer electrostatically disrupts a membrane of the pathogen.
Silk-Based Drug Delivery System; D.L. Kaplan and L. Meinel; Tuft s College, US and Eidgenossisches Technische Hochschule, Zurich, CH; US Patent # 10,548,981; February 4, 2020.
Silkworm produces a silk fiber or bave, which has two fibroin fi laments or “broins”. Broin is surrounded by a coating of gum, which gives it significant mechanical integrity. The patent describes a method of mixing a therapeutic agent with a silk fibroin solution, which is then converted to different forms/articles such as – thread, fiber, fi lm, mesh etc. The conformation of the article is altered to increase crystallinity to provide controlled release of the therapeutic agent. The property of the article can be changed by contacting the article with an electric field, by applying pressure, or by contacting the article with salt. Various drug release profiles are obtained with such articles having different properties.
Topical Montelukast for Treatment of Atopic Dermatitis; A. Avramoff , H. Shifrin, I. Oleinik, R. Schlinger, T. Sheskin, and V. Rosenberger; Taro Pharma, US; US Patent # 10,548,837; February 4, 2020.
Montelukast tablets (Singulair) are used to treat allergies and prevent asthma attacks. The current patent describes a gel formulation of Montelukast or its suitable salt. The gelling agents are selected from hyaluronic acid and its salt, a cellulose derivative (carbomer) or a polymer of acrylic acid. The formulation contains a preservative and a penetration enhancer. About 0.5% to about 1% of Montelukast gets deposited within the skin following topical application. The inventors also prepared waterless topical formulations containing occlusive agents. The patent described animal data suggesting effi cacy of the formulations.