Recent Patents on Drug Delivery & Formulation (v.8, #1)

This patent review focuses exclusively on the oral delivery of mesalamine (5-ASA) and excludes oral mesalaminepro-drug and rectal delivery formulations. The formulation strategies of marketed formulations (Apriso®, Asacol®,Lialda® and Pentasa®) and non-marketed formulations are reviewed and explained by decoding formulation specifics thatenable the site specific delivery for the treatment of inflammatory bowel disease.

Carbon Nanotubes: A Potential Concept for Drug Delivery Applications by Rakesh Kumar, Meenakshi Dhanawat, Sudhir Kumar, Brahma N. Singh, Jayant K. Pandit, Vivek R. Sinha (12-26).
The unique properties of carbon nanotubes (CNTs) make them a highly interesting and demandable nanocarrierin the field of nanoscience. CNTs facilitate efficient delivery of therapeutics like drugs, proteins, genes, nucleic acids,vitamins and lot more. Even though highly beneficial, the biocompatibility of CNTs is a major issue in their questioningtheir potential application in targeting drug delivery. Studies confirmed subdued toxicity of CNTs following slightmodifications like functionalization, controlled dimensions, purification etc. A well-established mechanism for cellularinternalization is an insistent need to attain a more efficient and targeted delivery. Recent patents have been thoroughlydiscussed in the text below.

Drug delivery to the back of the eye following topical administration remains an unmet need for the scientificcommunity. Treatment of posterior segment diseases requires localized and long-term drug delivery to the retina, choroid,and Bruch's membrane. Until the last decade, there was limited evidence from large clinical trials that demonstrated theusefulness of pharmacotherapy compared to laser therapy or other vitreoretinal surgical techniques for the treatment ofretinal diseases. This paradigm has shifted in recent years, with strong evidence demonstrating superior efficacy of ophthalmicdrugs compared to previous gold standards. However, ophthalmologists are left with no options other than administeringthe therapeutics via implants and intravitreal injections, which are highly invasive and associated with patientnon-compliance. A non-invasive topical therapy would enhance patient compliance and minimize the side-effects associatedwith intraocular implants and intravitreal injections. In an attempt to enhance patient compliance, the focus of researchhas shifted to the development of novel small molecule-based eye drop formulations. This review article discussesthe relevant patents and summarizes the resurgence in the treatment of posterior segment eye diseases through topicaldrug administration.

Taste masking is an important factor in the development of oral dosage forms containing bitter active pharmaceuticalingredients. Currently numerous techniques are being applied to overcome this problem. Realizing this, severalresearchers and pharmaceutical companies are now engaged in developing novel techniques to address the problem oftaste masking evident by numerous patents filed in this area in recent times. In this review the most recent patents for tastemasking are discussed and how these patents overcome the limitations of conventional approaches of taste masking is alsohighlighted. Novel techniques based on some recent patents such as nanohybrid, melt extrusion, non-complex cyclodextrincompositions and off taste masking are providing new realms to taste masking of bitter drugs. The present article alsoprovides an overview of various patented platform technologies based on different techniques/mechanisms employedfor taste masking. The unique features and principles of taste-masking approaches used in various patented technologiesare also discussed. A better understanding of these new patents and patented technologies will help researchers andpharmaceutical industries to select the appropriate platform, or to develop innovative products with improved tastemasking properties.

The study was designed to investigate the in vitro dissolution profile and compression characteristics of colontargeted matrix tablets prepared with HPMC E15 LV in combination with pectin and Chitosan. The matrix tablets weresubjected to two dissolution models in various simulated fluids such as pH 1.2, 6, 6.8, 7.2, 5.5. The fluctuations in colonicpH conditions during IBD (inflammatory bowel disease) and the nature of less fluid content in the colon may limit the expecteddrug release in the polysaccharide-based matrices when used alone. The Hydrophilic hydroxyl propyl methylcelluloseether premium polymer (HPMC E15 LV) of low viscosity grade was used in the formulation design, which made anexcellent modification in physical and compression characteristics of the granules. The release studies indicated that theprepared matrices could control the drug release until the dosage form reaches the colon and the addition HPMC E15 LVshowed the desirable changes in the dissolution profile by its hydrophilic nature since the colon is known for its less fluidcontent. The hydrophilic HPMC E15 LV allowed the colonic fluids to enter into the matrix and confirmed the drug releaseat the target site from a poorly water soluble polymer such as Chitosan and also from water soluble Pectin. The dramaticchanges occurred in the drug release profile and physicochemical characteristics of the Pectin, Chitosan matrix tabletswhen a premium polymer HPMC E15 LV added in the formulation design in the optimized concentration. Various drugrelease mechanisms used for the examination of drug release characteristics. Drug release followed the combined mechanismof diffusion, erosion, swelling and polymer entanglement. In recent decade, IBD attracts many patents in noveltreatment methods by using novel drug delivery systems.

Review of Patents and Application of Spray Drying in Pharmaceutical, Food and Flavor Industry by Bhavesh B. Patel, Jayvadan K. Patel, Subhashis Chakraborty (63-78).
Spray drying has always remained an energetic field of innovation in pharmaceutical, food and flavor industrysince last couple of decades. The current communication embodies an in-depth application of spray drying in pulmonarydrug delivery for production of uniform and respirable size particles suitable for nebulizers, dry powder inhalers (DPI)and pressurized metered dose inhalers (pMDI). The review also highlights spray drying application in the manufacturingof mucoadhesive formulation suitable for nasal cavities to improve the drug absorption and bioavailability. Recent researchworks and patents filed by various researchers on spray drying technology for solubility enhancement have alsobeen accentuated. Benefits of spray drying in production of dry flavorings to meet a product with maximum yield andleast flavor loss are also discussed. The use of spray drying in production of various food products like milk or soymilkpowder, tomato pulp, dry fruit juice etc, and in encapsulation of vegetable oil or fish oil and dry creamer has been discussed.Current review also highlights the application of spray drying in the biotechnology field like production of dry influenzaor measles vaccine as well as application in ceramic industry. Spray drying based patents issued by the U.S. Patentand Trademark Office in the area of drug delivery have also been included in the current review to emphasize importanceof spray drying in the recent research scenario.