Recent Patents on Drug Delivery & Formulation (v.8, #2)

Subconjunctival/episcleral, intrascleral, and suprachoroidal routes of drug delivery for treatment of posteriorsegment eye diseases have become more feasible and popular in the past few years. These routes have the advantage ofbypassing the main barriers to topical drug penetration, the ocular surface epithelium, the conjunctivallymphatics, and inthe case of deep intrascleral and suprachoroidial delivery, the sclera barrier. Many ocular drug delivery application devices,drug delivery methods, and therapeutics that have been developed for intravitreal use can also be used subconjunctivally,intrasclerally, and in the suprachoroidal space. Alternatively, site-specific devices, such microneedles, and therapeutics,such as hydrogel matrices, have been developed to enhance ocular drug delivery. This manuscript will review therecent research advances and patents on episcleral, intrascleral, and suprachoroidal routes of ocular drug delivery.

Lozenges as Delivery System for Upper Respiratory Catarrh Medication by Monika Bansal, Sachin K. Singh, Monica Gulati (92-100).
Lozenges, the small medicated candies that dissolve slowly in the mouth have always been a favoured deliverysystem, particularly for drugs meant for relieving sore throats and cold symptoms. This predilection can be attributedmainly to their ability to keep the naso-pharyngeal mucosa moist, enhance the swallowing reflex and provide longer contacttime of the drug with the naso-pharyngeal mucosa. A number of innovative technologies have been developed to improvethe conventional forms of lozenges i.e. hard candies and compressed tablets. These include the use of novel ingredients/techniques to enhance taste, reduce calorie content, facilitate quick manufacture and modify the drug release characteristics.Though used extensively for delivery of all kinds of medications for upper respiratory tract disorders, lozengesremain one of the least researched delivery systems. This article reviews various aspects of lozenges as a delivery system.The rationale behind the use of lozenges as the most favoured dosage form for delivery of anti-tussive substances is presented.Delving deeper, various anti-tussive substances that have been delivered as the lozenges including the patentsthereof, are also discussed briefly along with the innovative approaches that have been utilised for their formulation improvements.

Microsponge is developing as a novel drug delivery system for controlled release of medicinally active ingredients.It is generally prepared by polymerization or quasi emulsion solvent diffusion technique and has been successfullyused for targeted drug delivery. Microsponges are preferred over the microspheres owing to their better drug loadingcapacity. The present article deals with recent advancements in the microsponge preparation and its pharmaceutical applicationsand commercial utility considering patents.

Advancement in Microsphere Preparation Using Natural Polymers and Recent Patents by Uzma Farooq, Rishabha Malviya, Pramod K. Sharma (111-125).
In present study, Authors review all aspects of microsphere based novel drug delivery system; including needof natural polymers, different approaches for preparation and recent advancements. Microspheres are a novel drug deliveryapproach to control release of pharmacologically active ingredient as per patient needs. Natural polymers are cheap,biodegradable and have been proved safe for pharmaceutical formulation. Microspheres of naturally derived polymershave been prepared by several techniques like coacervation phase separation, emulsion polymerization, modified quasiemulsionsolvent diffusion, emulsion cross-linking, thermal denaturation, emulsification solvent evaporation, spray dryingand suspension polymerisation. It can be concluded from the whole patented study that due to the formation of polymericnetwork system, enzyme, hormones or other active moiety can be easily entrapped within the matrix. Rate of hydrationand swelling of the natural polymer controls the release pattern of the drug from the matrix.

Oral Solid Self-Emulsifying Formulations: A Patent Review by Bapurao Tarate, Rahul Chavan, Arvind K. Bansal (126-143).
Self-emulsifying compositions are lipidic drug delivery systems that provide a number of delivery advantages.A variety of excipients are available for designing of these drug delivery systems. These systems can be classified as TypeI, II, III, and IV, and alternatively as solid, semi-solid, and liquid. Till date many patents have been published on selfemulsifyingcompositions, and a few commercial products have also been launched. The purpose of this review is to haveinsights into the patent literature capturing the developments in the area of oral solid self-emulsifying formulations.Though the main emphasis is on developments in solid self-emulsifying formulations, an overview of different manufacturingtechniques has also been provided. These formulations can be grouped as conventional, granules, pellets, tablets, supersaturable,controlled release, eutectic-based, and positively charged. The components of self-emulsifying formulations describedin this review are not limited only to oils, surfactants, and cosurfactants but also include binders, polymers, diluents, alkalinizingagents, stabilizing agents, preservatives, and viscosity adjusting agents. The inventions highlighted in this article provideuseful guidelines for enhancement of oral bioavailability of drugs through this drug delivery platform.

An Overview of Recent Patents on Nanosuspension by Nirav Modh, Dharmik Mehta, Punit Parejiya, Amirali Popat, Bhavesh Barot (144-154).
Pharmaceutical scientists involved in drug discovery and drug development are facing serious problems withnewer poorly water soluble drugs with respect to their dissolution and bioavailability. Reducing the particle size of activepharmaceutical ingredient has been an efficient and reliable method for improving the bioavailability of insoluble drugs.Nanosuspension has emerged as an efficient and promising strategy for delivery of insoluble drugs due to its uniqueadvantages such as ease of modification, process flexibility, targeting capabilities, altered pharmacokinetic profile leadingto safety and efficacy. These unique features of nanosuspension have enabled its use in various dosage forms, includingspecialized delivery systems such as oral, parenteral, peroral, ocular and pulmonary routes. Currently, efforts are beingdirected to extend their applications in site-specific drug delivery. Large numbers of products based on nanosuspensionare in the market and few are under clinical trials. The commercialization potential of nanosuspension based formulationfor oral route is well established and products for other routes will enter the market within short span. Among the varioustechniques available, only wet milling technique has been successfully used for commercial production of nanosuspension.Nanosuspension based patents have extensive potential of reaching faster in the market as compared to other nanotechnologybased formulations. This review covers various aspects of techniques of preparation, route of administration andcommercialization of nanosuspension with main focus on the recent patents granted in the field.

Recent Advances in the Oral Delivery of Insulin by Rekha M. Ramesan, Chandra P. Sharma (155-159).
Insulin was discovered over 90 years ago. However oral insulin still remains a challenging and elusive goal.Extensive efforts are being made worldwide for developing noninvasive drug delivery systems, mainly via oral route as itis the most widely accepted means of administration. The main barriers faced in oral protein delivery are the enzymaticdegradation and poor permeability across the intestinal wall. The approaches for developing an oral insulin delivery systemmainly focus on overcoming these barriers. To overcome the gastro-intestinal barriers various types of formulationssuch as insulin conjugates, permeation enhancers, micro/nanoparticles, liposomes etc. are investigated. In the recent yearsa number of advances have taken place in understanding the needs and workable mechanisms of improved oral peptidedelivery systems. In this review the recent patents on oral insulin is focused. Emphasis is on the technologies based onpermeation enhancers and nanoparticle based carrier systems.

Patent Selections: (160-162).