Oral Pharmaceutical Composition of Isotretinoin; R. Rao, A.K. Fanda, S.K. Jain, and R.B. Singh; Sun Pharma. Ltd.; U.S. Patent # 9,700,535; July 11, 2017.
The oral bioavailability of a drug is affected by various factors, which include aqueous solubility, absorption of drug through GI tract, first pass effect, or food effect. The food-drug interactions can either decrease or increase the extent of drug absorption. Isotretinoin is known to have a food effect, i.e., its absorption is dependent on the presence of food in the stomach. The present invention provides an oral oil-free dispersion comprising isotretinoin, surfactants having HLB value of 10 or greater and co-solvents. The composition can also be filled into capsules. It exhibits reduced food effect in comparison to the marketed Epuris™ capsules indicated by higher Cmax and AUC in fasting state.
Dendronized Polymers for Nucleic Acid Delivery; Z. Guan and H. Zeng; The Regents of the University of California; U.S. Patent # 9,745,421, August 29, 2017.
RNA interference (RNAi) is a biological process in which RNA molecules inhibit gene expression or translation, by neutralizing targeted mRNA molecules. The therapeutic treatment potential of RNAi has been hampered due to its unsafe and inefficient intracellular delivery of siRNA (small interfering RNAs). The present invention provides for an innovative biodegradable peptide-based dendronized polymer (“denpol”) architecture, that can be used as a carrier for the intracellular delivery of nucleic acids. The dendronized polymers combine the multi-valency of dendrimers, with the conformational flexibility of linear polymers for optimal binding of nucleic acids (e.g., siRNA). The patent also claims a pharmaceutical composition comprising a dendronized polymer/siRNA polyplex and provides for a method of treating a disease or disorder.
Enhanced Delivery of Drug Compositions to Treat Life Threatening Infections; J.E. Hitt, T.L. Rogers, B.D. Scherzer, I.B. Gillespie, P.C. Garcia, N.S. Beck, C.J. Tucker, T.J. Young, D.A. Hayes, R.O. Williams III, K.P. Johnston, J.T. McConville, J.I. Peters, R. Talbert, and D.S. Burgess, Board of Regents, The University Texas System; U.S. Patent # 9,724,344; August 8, 2017.
The patent describes an enhanced delivery of antifungal agents into lungs and how the concentration stays at the therapeutic level for at least one hour after being delivered to the lung. These drugs are known to have poor bioavailability after pulmonary administration. The method of preparation involves: mixing an effective ingredient with a solution agent; spraying the effective ingredient-solution agent mixture through an insulating nozzle located at or below the level of a cryogenic liquid. The invention also developed other methods to produce porous respirable nanoparticles suitable for deep lung deposition. In one of the claims, the respirable nanoparticle aggregates were prepared by a process comprising ultra-rapid freezing of an amorphous antifungal drug solubilized in a freezable solvent on a solid substrate to form the respirable nanoparticle aggregates.
Small Cationic Antimicrobial Peptides; R.E.W. Hancock, K. Hilpert, A. Cherkasov, and C. Fjell; The University Of British Columbia; U.S. Patent # 9,707,282; July 18, 2017
The treatment of bacterial infections with antibiotics is one of the mainstays of human medicine. Unfortunately, the effectiveness of antibiotics has become limited due to an increase in bacterial antibiotic resistance in the face of decreasing efforts and success in discovery of new classes of antibiotics. The present invention relates generally to peptides and more specifically to antimicrobial and immunomodulatory host defense peptides. The present invention claims an isolated immunomodulatory peptide comprising the amino acid sequence set forth in SEQ ID NO: 1214, or a variant thereof comprising an Ile, Arg or Val at position 5, or an amino acid sequence having at least 90% identity thereto. The invention provides a bioinformatic method of predicting new peptides with good antimicrobial activity through the creation of a random library of peptides.
RNAi-Mediated Inhibition of Histamine Receptor H1-Related Conditions; J.M. Yanni, J.E. Chatterton, D.A. Gamache, and S.T. Miller; Arrowhead Research Corp.; U.S. Patent # 9,745,585; August 29, 2017.
The present invention relates to the field of interfering RNA compositions for treatment of a histamine receptor H1 (HRH1)-related condition. Such conditions include allergic conjunctivitis, ocular inflammation, dermatitis, rhinitis, asthma, or allergy, for example. The patent claims a composition comprising an effective amount of a single-stranded siRNA having a length of 19 to 49 nucleotides, or a double-stranded siRNA wherein each strand has a length of 19 to 49 nucleotides. The invention also claims a composition which can be administered via an aerosol, buccal, dermal, intradermal, inhaling, intramuscular, intranasal, intraocular, intrapulmonary, intravenous, intraperitoneal, nasal, ocular, oral, otic, parenteral, patch, subcutaneous, sublingual, topical, or transdermal route.
Pharmaceutical Composition for Transcolonic Absorption; T. Yokota, M. Murakami, and K. Nishina; National University Corporation, Tokyo Medical and Dental University; U.S. Patent # 9,731,025; August 15, 2017.
High molecular, water-soluble compounds such as hormones, cytokines, nucleic acids etc. have low epithelial permeability and cell membrane permeability. The present invention aims to provide a pharmaceutical composition for transcolonic absorption capable of delivering a physiologically active substance having an intracellular site of action into specific tissue cells with high specificity, noninvasively by a means of administration other than injection. The invention described method of noninvasive administration of vitamin E-conjugated siRNA (VE-siRNA). Endogenous chylomicrons are formed in the small intestine, the majority of which penetrate through the mucosal epithelium of the small intestine into lymphatic vessels and ascend along the lymphatic vessels; after draining into the vein, they are metabolized into chylomicron remnants by lipoprotein lipase (LPL), whereby the endogenous chylomicron is delivered to the liver. The patent helps to deliver endogenous chylomicrons comprising VE-siRNA into the liver cells by absorption from the small intestine.
Sustained Release Eye Drop Formulations; V.G. Wong and L.L. Wood; Ramscor, Inc.; U.S. Patent # 9,737,606; August 22, 2017.
The present invention relates to biocompatible, biodegradable, sustained-release formulations of active agents for topical administration to the eye. Current topical eye drop formulations, which often elicit some degree of irritation, provide only shortterm exposure of beneficial agents to the eye and thus, often require several administrations daily. The formulation consists of 10% to 15% (w/w) dexamethasone or a derivative, analog, or a salt dispersed or suspended in 85% to 90% (w/w) of a biocompatible, biodegradable excipient mixture. Their aim is to deliver medications in a continuous and sustained manner. The formulations deliver therapeutic and non-toxic levels of active agents over the desired extended time frame, often primarily at the site of administration.