Pharmaceutical P.I.N. Points - Patent Innovation News

Neelam Sharma, MS, Lavanya Kundurthy, BE and Hemant N. Joshi, PhD, MBA - Tara Innovations, LLC www.tarainovations.com and www.tara-marketing.com, [email protected]

Drug Delivery System and Methods Providing Thereof

V. Demina, H. Manninga, S. Sotnikov, M. Stapf, and K.J. Ko Mann; Neuway Pharma GmbH, Germany; U.S. Patent # 11,279,938; March 22, 2022.

The Blood Brain Barrier (BBB) is a highly selective and permeable membrane between blood and the brain. Several strategies are known for affecting the transport of active pharmaceutical molecules across the BBB. A few of the known strategies are - cerebral vasodilation or focused ultrasound radiation. Another approach is the use of a drug delivery system on the basis of Virus-Like Particles (VLP) derived from John Cunningham virus (JCV). However, there is need to further improve the efficacy of this system. The present patent discloses the drug delivery system on basis of VLP from JCV, but with improved efficacy thereby allowing more drug to reach the Central Nervous System. The method comprises steps of disassembly of VLP into pentamers and reassembly into VLP.

In Situ Gelling Composition as a pH-Selective and Mucoadhesive Sustained Release Drug Delivery System

S. MD, S.T. Abdullah, and N.A. Alhakamy; King Abdulaziz University, Saudi Arabia; U.S. Patent #11,260,025; March 1, 2022.

The present patent describes a method for the sustained-delivery of a bioactive agent, such as resveratrol as an in-situ gelling composition. Composition includes nanoparticles comprising soy protein and a bioactive agent encapsulated as a nanocomposite in a sodium alginate in-situ gelling film. In situ gelling systems are polymeric formulations. They are in a sol-state before administration, and they are capable of forming gels in response to different endogenous stimuli, such as temperature increase, pH change and the presence of ions. A sodium alginate deposition film has the ability to encapsulate the drug by the conversion of the alginate films into alginic acid gels when in contact with simulated gastric media (e.g., 0.1N-HCl). The film may be administered after water reconstitution or after incorporation into a solid dosage form, e.g., a gelatin capsule.

Method for Preparing Biofilm-Coated Drug Nanocrystal and Application Thereof

W. Lu, Z. Chai, X. Hu, C. Xie, H. Hou, and H. Wang; Shanghai Whittlong Pharma Institute, China; U.S. Patent # 11,260,032; March 1, 2022.

A Nano Drug Delivery System (NDDS) includes a biofilm-coated drug nanocrystal. A biofilm-coated NDDS is formed by coating a rigid supporting nanoparticle with a layer of biofilm, where the supporting nanoparticle is usually made of an organic polymer material or an inorganic material. The biofilm-coated NDDS can carry drugs by adsorbing the drugs onto the biofilm or loading the drugs in the supporting skeleton. The drug nanocrystal has a particle size of 10-1000 nm. The drug-carrying method of adsorbing on the biofilm is generally suitable for substances, which have specific adsorption to the biofilm. The NDDS has advantages of high drug loading capacity, good biocompatibility, long systemic circulation time and sustained release of drugs.

High Concentration Alpha-Glucosidase Compositions for the Treatment of Pompe Disease

K. Valenzano, J. Crowley, R. Khanna, and J. Flanagan; Amicu Therapeutics, USA; U.S. Patent # 11,278,599; March 22, 2022.

Pompe disease is a genetic disorder in which complex sugar called glycogen builds up in the body’s cells. The disease results from the deficiency of an enzyme called Acid Alfa Glucosidase (GAA), which breaks downs complex sugars in the body. The patent covers administration of GAA enzyme in combination with Active-site-specific Chaperone (ASSC, e.g., deoxynojirimycin or DNJ). The GAA enzyme is stabilized conformationally when combined with an ASSC and is well-suited to withstand, for example, thermal and pH challenges. The ASSC is administered orally and GAA is administered intravenously.

Porous Photonic Crystals for Drug Delivery to the Eye

W. Freeman, M.J. Sailor, L. Cheng, F. Cunin, E. Anglin, and Y.Y. Li; The Regents of the University of California, USA; U.S. Patent # 11,241,380; February 8, 2022.

It is difficult to deliver drugs in sufficient quantity and continuously in the eye. The invention provides a minimally invasive controlled drug delivery system including porous films or porous film particles, having pores configured and dimensioned to receive a drug therein. Photonic crystals are produced from porous silicon and porous silicon/polymer composites. Porous silicon is especially advantageous in that porous silicon films have a large free volume (typically 50-80%), and thus a high capacity for a drug can be custom designed at the nanoscale. Particles can be injected into the eye with a 25 or 27-gauge needle. A photonic crystal is an optical nanostructure in which the refractive index changes periodically. The photonic crystals of silica are especially advantageous because of the relative ease with which the optical properties, pore size, and surface chemistry can be manipulated.

Self-Nanoemulsifying 3D-Printed Tablet Composition and Method of Use Thereof

T.A. Ahmed, R.I. Felimban, H.H. Tayeb, K.M. El-Say, W.Y. Rizg, and F.H. Fuad; King Abdulaziz University, Saudi Arabia; U.S. Patent # 11,253,481; February 22, 2022.

The goal of the invention is to provide a self-nano-emulsifying 3D (three dimensional) printer ink composition and a method of using such a composition to manufacture a 3D-printed tablet having compartmentalized active pharmaceutical ingredients with customizable drug release rates. Patients need a tailored therapy to ensure better medical care. Selection of the appropriate therapy for a wide range of patients is based on an individual’s genetic and/ or molecular and cellular analysis. The 3D printing technology has been contemplated as a useful drug delivery manufacturing system in that a 3D structure can be manufactured by fusing or depositing different materials by applying the strategy of layer-by-layer additive manufacturing. Patient-specific 3D-printed medications are becoming increasingly beneficial in personalized treatments, especially for the practice of precision medicine. The 3D-printed tablet composition includes glimepiride and/or rosuvastatin in a curcuma oil based Self-Nano-Emulsifying Drug Delivery System (SNEDDS).

Formulations and Methods for the Treatment of Cancers

D.G. Tang, and X. Chen; Stemirna Biotechnology, China; U.S. Patent # 11,278,524; March 22, 2022

Prostate cancer is an androgen-fueled malignancy and the Androgen Receptor (AR) represents the prime therapeutic target. However, Androgen Deprivation Therapies (ADT) including chemical castration and use of androgen receptor antagonists have had limited success, since the targeted tumors become refractory to treatment and progress into castration resistant prostate cancer. A formulation described herein comprises an androgen receptor signaling inhibitor (enzalutamide) and a B-cell lymphoma 2 inhibitor (venetoclax). The present invention is directed to a related formulation further comprising a Bromodomain-and-Extra-Terminal protein inhibitor and a phosphoinositide 3-kinase inhibitor.

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