Recent Patents on Drug Delivery & Formulation (v.4, #3)

Recent Patents and Trends in Orally Disintegrating Tablets by Farhan A. AlHusban, Amr M. El-Shaer, Rhys J. Jones, Afzal R. Mohammed (178-197).
Orally disintegrating tablets (ODTs) offer many advantages over the conventional oral dosage forms in terms of convenience and ease of use. Over the last decade, substantial advances in the formulation of ODTs have been achieved in academia and industry that resulted in the emerging of a large number of patents. The aim of this review is to summarise the most recent patents in ODT formulations and highlight their motivations, inventive steps and significances in the development of ODT formulations. Five major techniques have been applied in manufacturing of ODTs, namely conventional tablet press, moulding, freeze drying, tablet loading and pulverization, with majority of the patents dedicated to the use of conventional tablet pressing. The patents have addressed various issues concerning the manufacturing of robust and practical ODT formulations by disclosing new manufacturing techniques, advantageous materials, and innovative formulation steps. However, future developments are required to reduce the cost and widening the application of the new manufacturing techniques, while simplifying and shortening the formulation steps will be crucial in the well established ones.

A pharmacological chaperone is a relatively new concept in the treatment of certain chronic disabling diseases. Cells maintain a complete set of functionally competent proteins normally and in the face of injury or environmental stress with the use of various mechanisms, including systems of proteins called molecular chaperones. Proteins that are denatured by any form of proteotoxic stress are cooperatively recognized by heat shock proteins (HSP) and directed for refolding or degradation. Under non-denaturing conditions HSP have important functions in cell physiology such as in transmembrane protein transport and in enabling assembly and folding of newly synthesized polypeptides. Besides cellular molecular chaperones, which are stress-induced proteins, there have been recently reported chemical, or so-called pharmacological chaperones with demonstrated ability to be effective in preventing misfolding of different diseasecausing proteins, specifically in the therapeutic management of sight-threatening eye diseases, essentially reducing the severity of several neurodegenerative disorders (such as age-related macular degeneration), cataract and many other protein-misfolding diseases. This work reviews the biological and therapeutic activities protected with the patents of the family of imidazole-containing peptidomimetics Carcinine (and#946;-alanylhistamine), N-acetylcarnosine (N-acetyl-and#946;-alanylhistidine) and Carnosine (and#946;-alanyl-l-histidine) which are essential constituents possessing diverse biological and pharmacological chaperone properties in human tissues.

Patented Herbal Formulations and their Therapeutic Applications by Mohamed Musthaba, Sanjulae Baboota, Tanwir M.D. Athar, Kamal Y. Thajudeen, Sayeed Ahmed, Javed Ali (231-244).
Recently, there is a greater global interest in non synthetic, natural medicines derived from plant sources due to better tolerance and minimum adverse drug reactions as compared to synthetic medicines. Herbal products are also commonly used by the patients with certain chronic medical conditions, including breast cancer, liver disease, human immunodeficiency, asthma and rheumatological disorders. WHO estimates that about three-quarters of the world's population currently uses herbs and other forms of traditional medicines for the treatment of various diseases. The herbs are formulated in different modern dosage forms, such as Tablets, Capsules, Topical cream, Gel, Ointment and even some novel drug delivery forms, like extended release, sustained release, and microencapsules dosage forms. Patenting of herbal formulations has increased over the past few years and scientific evidence of therapeutic activity has been reported by performing various in vitro and in vivo experiments. This manuscript deals with various patented herbal formulations with their therapeutic application against various disases.

Bioavailability Enhancement of Coenzyme Q10: An Extensive Review of Patents by Sarwar Beg, Shamama Javed, Kanchan JKohli (245-257).
Coenzyme Q10 (CoQ10) is a major antioxidant principle found in human body which plays a vital role in maintaining several biochemical pathways of body. It acts as a potential mediator in transferring electrons in oxidoreductive reactions of electron transport chain. Chemically, it is a basic quinone containing moiety having a large and high molecular weight structure. Deficiency of this in body leads to several potential disorders like dysfunctions in cellular energetics, neurological degeneration, higher oxidative stress induced damage, breast cancer etc. The high molecular weight and lipophilicity of CoQ10 makes it poorly water soluble and consequently leads to low systemic availability. Several advancements have been made to enhance the bioavailability of CoQ10 using various approaches like size reduction, solubility enhancement (by solid dispersion, prodrug, complexation, ionization) and use of novel drug carriers such as liposomes, microspheres, nanoparticles, nanoemulsions and self-emulsifying system. The primary objective of the present review is to assemble patents representing the various approaches used for enhancement of CoQ10 bioavailability.

Therapeutic Potential of Mucoadhesive Drug Delivery Systems - An Updated Patent Review by Suresh K. Maurya, Kamla Pathak, Vikas Bali (256-265).
There has been a burgeoning interest among the research scientists to associate the drugs to polymeric particulate systems due to the propensity of these systems to interact with the mucosal surface. Transmucosal delivery of drugs through mucosal lining of nasal, rectal, vaginal, ocular and oral cavity entails advantages like prolongation of residence time at the absorption site, enhanced contact with underlying mucosa eventually leading to enhanced absorption of the active ingredient. Such systems not only provide local targeting of drugs but also offer a better control over their systemic delivery. Hence, the objective of the present review is to provide an overview of the mucoadhesive drug delivery systems with special emphasis on the intellectual aspects of these systems. This paper also attempts to extend the information present on mucoadhesive drug delivery systems in the existing literature by focussing on the update on the patents granted as well as applications published for these systems. Some newer mucoadhesive formulations like mucoadhesive microparticles and nanoparticles have also been discussed.

Patent Selections by Bentham Science Publishers (266-267).
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