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 2018.
Vitamin D3 and Analogs Th ereof for Treating Alopecia; Berg LLC, USA; J. Jimenez, N. R. Narain, and J. P. McCook; U.S. Patent # 9,901,637, February 27, 2018.
Alopecia is a common and distressing side effect of many chemotherapeutic agents. The present invention provides methods and pharmaceutical compositions and relates to the use of vitamin D compounds, such as vitamin D3 or calcitriol and its analogs or a metabolite, to prevent or treat alopecia. The pharmaceutical compositions of the invention comprise an effective amount of a vitamin D compound in a formulation that topically delivers the vitamin D compound to the epidermis layer but substantially avoids delivery to the dermis layer. The pharmaceutical composition also comprises about 40% (w/w) propylene glycol and about 60% (w/w) anhydrous absolute ethanol (200 proof, U.S.); or about 30% (w/w) propylene glycol, about 10% (w/w) ethoxydiglycol or transcutol, and about 60% (w/w) anhydrous absolute ethanol (200 proof, U.S.).
Formulations for Targeted Release of Agents to Low pH Tissue Environments or Cellular Compartments and Methods of Use Thereof; Yale University, USA; W. M. Saltzman, J. Zhang, J. Zhou, and Z. Jiang; U.S. Patent # 9,895,451; February 20, 2018.
The patent relates to polymer compositions and methods for improved systemic delivery of diagnostic, prophylactic and therapeutic agents in vitro and in vivo, targeted to low pH tissue environments or cellular compartments. It describes a polymeric formulation for delivery of a nucleic acid comprising of a poly (amine-co-ester-co-ortho) ester or poly (amine-co-amide-co-ortho) ester. It also provides methods of forming active agent-load nanoparticles and methods of using the nanoparticles for drug delivery. The nanoparticles can be coated with an agent that reduces surface charge and an agent that increases cell-specific targeting. The loaded nanoparticles are less toxic and more efficient at drug delivery, as compared to a control or other transfection reagents.
Combination Drug Therapies for Cancer and Methods of Making and Using Them; Vicus Therapeutics, LLC, USA; N. Bascomb, J. Maki, and F. Young; U.S. Patent # 9,889,120; February 13, 2018.
Nexavar™ (sorafenib) is an anticancer medicine used to treat liver, kidney or thyroid cancer. It can cause the following serious side effects – decreased flow to heart, bleeding, high blood pressure, skin reactions, etc. The patent claims a combination drug therapy comprising a beta-blocker (propranolol), an anti-inflammatory agent (etodolac) and sorafenib. The recommended dosing is as follows - Week 1: 20 mg propranolol, 75 mg etodolac in the AM 20 mg propranolol in the afternoon, or at about 3 PM 300 mg etodolac in the PM; Week 2: (a) 35 mg propranolol, 75 mg etodolac, 400 mg sorafenib in the AM 25 mg propranolol at in the afternoon, or at about 3 PM 600 mg etodolac in the PM, or (b) 35 mg propranolol, 75 mg etodolac, 400 mg sorafenib in the AM 25 mg propranolol at in the afternoon, or at about 3 PM 600 mg etodolac, 400 mg sorafenib in the PM; Week 3: same as Week 2; Week 4 : 35 mg propranolol, 25 mg propranolol at in the afternoon, or at about 3 PM.
Method for Delivery of Treatment Formulation to Paranasal Sinus; Sinopsys Surgical, Inc., USA; C.L. Oliver, D.F. Schomer, H. Ross, W.W. Cimino, and B.J. Willoughby; U.S. Patent # 9,901,721; February 27, 2018.
Chronic sinusitis is a very common condition and is usually treated with prescription medicines. Current drug therapies include oral administration as pills and nasal topical administration, neither of which are a 100% effective. In addition to medication, for patients with particularly severe symptoms, surgical drainage may be the only additional option. This patent describes a device which does not require surgical drainage but will help effective administration of the drug to treat the sinusitis. This patent claims an implant device, which aids in delivering a treatment formulation to a paranasal sinus of a human. An aspect of the invention involves implantation of a device in a human to fluidly connect the lacrimal apparatus a paranasal sinus through such a fistula. The implant device has a proximal end and a distal end located at opposite longitudinal ends of the device. An internal passage extends between the proximal end and the distal end, through the conduit.
Passaging and Harvesting Formulation and Method for Human Pluripotent Stem Cells; Lonza Walkersville, Inc., USA; Y. Nie, J. A. Rowley, T. Fellner, and P.Walsh; U.S. Patent # 9,885,019; February 6, 2018.
Pluripotent stems cells are capable of giving rise to several different cell types. Traditionally, human Pluripotent Stem Cells (hPSC) are harvested and passaged as colony fragments by mechanical scraping with or without pre-treatment with enzymes and this process is labor intensive. This patent discloses a formulation and a method for harvesting and subsequent passing of hPSC without the use of enzymes and/or scraping to dislodge cells from cell culture vessels. The patent relates to mainly three criteria: one is formulations including sodium citrate and a method of use thereof; second is methods of identifying formulations based on the Ca2+ chelator concentration and osmolarity; and third is use of such formulations. The patent claims that concentration of sodium citrate is 1 to 15 mMol/Liter and osmolarity of 418-570 mOsmol/Liter.
Liposomal Drug Delivery System for Bone Cements; University College Cardiff Consultants Ltd., UK; S. Denyer, S. Evans, W. Ayre, and J. Birchall; U.S. Patent # 9,895,466; February 20, 2018.
The patent describes a novel antibiotic delivery vehicle for delivering and dispersing antibiotic in bone cement such that the resultant product exhibits uniform mixing of antibiotic in the cement. The formulation provides improved antibiotic release profile and surprising structural advantages without compromising the mechanical strength and fatigue properties of the cement. The patent claims that liposomal delivery comprises at least one antibiotic, a block co-polymer adsorbed on to the liposome having molecular weight less than 2000 and higher proportion of polypropylene oxide to polyethylene oxide. The patent also claims that liposome formulation is selected from the group where liposome is less than 600 nm in diameter when measured using laser diffraction; a liposome is less than 150 nm when measured using Transmission electron microscopy.
Bilayered Calcium Sulfate/Calcium Phosphate Space-Making Composites with Multiple Drug Delivery Capabilities; University of Kentucky Research Foundation, US; D. Puleo, B. Orellana, and M. McQuinn; U.S. Patent # 9,895,354; February 20, 2018.
This patent provides methods of improving bone regeneration or augmentation through the introduction of bilayered composites comprising an outer shell and an inner core. Bilayered composites provide localized drug delivery wherein one layer degrades in situ within a subject at a rate faster than the other layer. It also provides mechanical support to tissues while improving administration of therapeutic compounds dispersed within one or both layers. One layer may comprise a material selected from the group consisting of dicalcium phosphate dihydrate (DCPD), calcium polyphosphate etc. The other layer may comprise a material selected from the group consisting of calcium sulfate (CS), 3-tricalcium phosphate, amorphous calcium phosphate etc. The release of therapeutic compounds and the carriers thereof can be tailored depending on the layer in which the therapeutics are loaded.