Recent Patents on Drug Delivery and Formulation最新文献

Background: Vaginal drug delivery approach represents one of the imperative strategies for local and systemic delivery of drugs. The peculiar dense vascular networks, mucus permeability, and range of physiological characteristics of the vaginal cavity have been exploited for therapeutic benefit. Furthermore, the vaginal drug delivery has been curtailed due to the influence of different physiological factors like acidic pH, constant cervical secretion, microflora, cyclic changes during periods along with turnover of mucus of varying thickness.

Objective: This review highlights advancement of nanomedicine and its prospective progress towards the clinic.

Methods: Relevant literature reports and patents related to topics are retrieved and used.

Result: The extensive literature search and patent revealed that nanocarriers are efficacious over conventional treatment approaches.

Conclusion: Recently, nanotechnology based drug delivery approach has promised better therapeutic outcomes by providing enhanced permeation and sustained drug release activity. Different nanoplatforms based on drugs, peptides, proteins, antigens, hormones, nucleic material, and microbicides are gaining momentum for vaginal therapeutics.

Traditional nutraceuticals and cosmeceuticals hold pragmatic nature with respect to their definitions, claims, purposes and marketing strategies. Their definitions are not well established worldwide. They also have different regulatory definitions and registration regulatory processes in different parts of the world. Global prevalence of nutraceuticals and cosmeceuticals is noticeably high with large market share with minimal regulation compared to traditional drugs. The global market is flooded with nutraceuticals and cosmeceuticals claiming to be of natural origin and sold with a therapeutic claim by major online retail stores such as Amazon and eBay. Apart from the traditional formulations, many manufacturers and researchers use novel formulation technologies in nutraceutical and cosmeceutical formulations for different reasons and objectives. Manufacturers tend to differentiate their products with novel formulations to increase market appeal and sales. On the other hand, researchers use novel strategies to enhance nutraceuticals and cosmeceuticals activity and safety. The objective of this review is to assess the current patents and research adopting novel formulation strategies in nutraceuticals and cosmeceuticals. Patents and research papers investigating nutraceutical and cosmeceutical novel formulations were surveyed for the past 15 years. Various nanosystems and advanced biotechnology systems have been introduced to improve the therapeutic efficacy, safety and market appeal of nutraceuticals and cosmeceuticals, including liposomes, polymeric micelles, quantum dots, nanoparticles, and dendrimers. This review provides an overview of nutraceuticals and cosmeceuticals current technologies, highlighting their pros, cons, misconceptions, regulatory definitions and market. This review also aims in separating the science from fiction in the nutraceuticals and cosmeceuticals development, research and marketing.

Background: Cancer is a life-threatening global problem with high incidence rates. Prioritizing the prevention of cancer, chemopreventive agents have drawn much attention from the researchers.

Objective: This review focuses on the discussion of the progress in the development of chemopreventive agents and formulations related to the prevention of oral cancer.

Methods: In this perspective, an extensive literature survey was carried out to understand the mechanism, control and chemoprevention of oral cancer. Different patented agents and formulations have also exhibited cancer preventive efficacy in experimental studies. This review summarizes the etiology of oral cancer and developments in prevention strategies.

Results: The growth of oral cancer is a multistep activity necessitating the accumulation of genetic as well as epigenetic alterations in key regulatory genes. Many risk factors are associated with oral cancer. Genomic technique for sequencing all tumor specimens has been made available to help detect mutations. The recent development of molecular pathway and genetic tools has made the process of diagnosis easier, better forecast and efficient therapeutic management. Different chemical agents have been studied for their efficacy to prevent oral cancer and some of them have shown promising results.

Conclusion: Use of chemopreventive agents, either synthetic or natural origin, to prevent carcinogenesis is a worthy concept in the management of cancers. Preventive measures are helpful in controlling the occurrence or severity of the disease. The demonstrated results of preventive agents have opened an arena for the development of promising chemopreventive agents in the management of oral squamous cell carcinoma.

The structure of the eye is very complex in nature which makes it a challenging task for pharmaceutical researchers to deliver the drug at the desired sites via different routes of administration. The development of the nano-based system helped in delivering the drug in the desired concentration. Improvement in penetration property, bioavailability, and residence time has all been achieved by encapsulating drugs into liposomes, dendrimers, solid lipid nanoparticle, nanostructured lipid carrier, nanoemulsion, and nanosuspension. This review puts emphasis on the need for nanomedicine for ocular drug delivery and recent developments in the field of nanomedicine along with recent patents published in the past few years.

Background: Excessive blue light light-emitting diode (LED) exposure and consequent oxidative stress causes corneal damage and corneal injuries are the major problem arising these days due to excessive use of mobile phone, TV, environment pollution, etc. Objective: In the present investigation, the protectiveness of carboxymethyl Terminalia catappa (CTC) from blue light LED-induced corneal damage was explored.

Methods: For this purpose, Terminalia catappa (TC) was functionalized by carboxymethylation and its structural modification was confirmed by spectral attributes. Further, the CTC protective eye drop formulations (0.025-1%, w/v) were prepared and evaluated for their capability of protection from blue light LEDinduced corneal damage as compared to CTC protective eye gel (1.25-7%, w/v). The findings pointed towards excellent protection of CTC gel formulations as compared to CTC eye drop formulations. In addition, the prepared optimized CTC gel had thixotropic behavior as evident from percentage structural recovery which was 1.75 fold higher than marketed formulation (I-Comfort, HPMC 2%, w/v). The safety and non-toxicity of CTC protective eye drop and gel were confirmed by HET-CAM test. Further, a rat eye model was implemented that mimic blue light light-emitting diode induced corneal damage in day to day life to assess the protective effect of CTC protective eye drop and gel.

Results: The order of protectiveness of CTC formulations was found to be CTC protective eye gel (4%, w/v) (no corneal damage)>marketed eye gel (12.34% corneal damage)=CTC protective eye drop (0.75%, w/v) (17.48% corneal damage)> marketed eye drop (51% corneal damage). The mechanism behind the protective effect of CTC eye drop and gel was associated with good free radical scavenging activity and corneal adhesive property of CTC. It is established from the present work that, carboxymethyl Terminalia catappa has protective action against blue light light-emitting diode induced corneal damage.

The reason that the oral route attained such acceptance may be ascribed to its affluence of administration. Over the years, patient convenience- oriented exploration in the area of drug delivery has introduced potential innovative medicine delivery systems. The elegant drug delivery system is an amalgamation of science and dexterity with therapeutic prospect and presentability. It involves the administration of medications in a groundbreaking fashion with the assistance of cosmetics, wearable devices and oral drug delivery system which can also be used for ornamental purposes. Out of which, therapeutic chewing gum offers a highly suitable and amenable technique of dosing medications comprising children and elderlies. It is a potentially convenient means of administering medications either locally or systematically via the oral cavity. It bids innumerable gains over conventional drug delivery methods. Moreover, medicinal chewing gums involve the dynamic and constant masticatory actions for drug release. Currently, enriched expertise has made it promising to advance and fabricate medicated chewing gum with predefined properties and it could be a marketable triumph in the future. Apprehending this, several investigators and pharmaceutical companies are now engaged in developing innovative practices vis-à-vis medicated chewing gums by filing several patents in this area. The present manuscript also delivers a gestalt of various patented technology platforms based on different methods/ mechanisms employed for the preparation of medicated chewing gums.

Enteric coated dosage form bypasses the stomach and releases the drug into the small intestine. Advantages of enteric coated pellets in comparison with enteric coated tablets are a) Pellets provide rapid onset of action and faster drug release due to the smaller size than tablets and b) Pellets exhibit less residence time of acid-labile drugs in the stomach compared to tablets. Dosage form coat can be damaged by longer resistance time in the stomach. The present review summarizes the current state of enteric coated pellets where core pellets are prepared by extrusion-spheronization technique and the enteric coating is applied in a fluidized bed processor. Two approaches are involved in the preparation of core pellets. In the first approach, a mixture of drug and excipient(s)/co-processed excipient is passed through extruders to prepare core pellets. In the second approach, excipient core pellets are prepared by extrusion technique and the drug is layered onto it before the enteric coating. The excipients present in the core pellets decide immediate or extended release of drug in the intestine. The coprocessed excipient pellets provide less batch variability and provide a platform for layering of many drugs before enteric coating. Some patents included enteric coating pellets [CN105456223 (A), CN105596310 (A), CN105616371 (A), CN105663095 (A), CN101611766B, CN106511862 (A), CN106668018 (A), CN106727381 (A), CN106924222 (A), TW200624127 (A), US 2017/0165248A1, US 2017/0224720A1] are discussed.

Background: Non-steroidal anti-inflammatory drugs are most commonly used in the management of ocular inflammations. These drugs have poorly aqueous solubility and weakly acidic nature. They interact with cationic quaternary ammonium compound benzalkonium chloride, used as a preservative in ophthalmic formulations, to form insoluble complexes. To overcome this incompatibility solubilizers like polysorbate 80, lysine salts, tocopheryl polyethylene glycol succinate etc. are used which are quite irritating and affect the corneal integrity.

Objective: The objective of the present study is to formulate nonirritating, compatible, microbiologically stable ophthalmic formulation with good corneal permeation characteristics. The interaction between diclofenac sodium or ibuprofen with benzalkonium chloride was optimized using a central composite experimental design to prepare nanosuspensions by nanoprecipitation.

Methods: The optimized batches of nanosuspensions were evaluated for ex vivo corneal permeation study, preservative challenge test and physical stability. The optimal concentrations of benzalkonium chloride for diclofenac sodium (0.1%, w/v) and ibuprofen (0.1% w/v) nanosuspensions were determined to be 0.002%(w/v), which had a respective average particle size of 440 nm and 331 nm, respectively. The nanosuspensions of diclofenac sodium and ibuprofen provided 1.6 and 2.1- fold higher ex vivo corneal permeation than their respective conventional aqueous solution dosage forms. Further, the concentration of benzalkonium chloride used in the formulations showed adequate preservative efficacy.

Results: The optimized nanosuspension formulations of diclofenac and ibuprofen were found to be physically stable and microbiologically safe with greater corneal penetration than the conventional solution dosage forms.

Efficient delivery of ocular therapeutics with improved efficacy, enhanced bioavailability, and acceptable patient compliance presents unique challenges. This can be attributed to the presence of protective mechanisms, physicobiological barriers, and structural obstacles in the eye. Nanotherapeutic interventions have been explored extensively over the past few years to overcome these limitations. The present review focusses on the nanoformulations developed for the diagnosis and treatment of various ocular diseases besides providing an in-depth insight into the patents reported for the same.

Nanotechnology-based delivery systems have been considered a promising approach for topical application, considering their characteristics of penetration into/across the skin. The present review aimed to evaluate the recent international scenario of patents concerning the use of nanotechnology- based delivery systems as skin penetration enhancers. A survey of recent patent documents was conducted by using the Espacenet patent database including the terms "skin" in the title and "promot* or enhanc* and penetrat* or absorp* or permeat*" and "nano*" with the truncation symbol (*) in the abstract of documents. A total of 110 patents were published from 2008 to 2018, with 94 technologies being considered. The results demonstrated an increase in innovations concerning nanotechnologybased delivery systems as skin penetration enhancers in recent years. Most patent applicants are from China (60.6%) and Korea (21.3%), and companies (68%) were the most prominent owners. The majority of patent applications (76%) were intended for cosmetic purposes; the types of products and nanostructures were also investigated. Overall results demonstrated the increased interest around the world in patenting products involving skin permeation promotion and nanotechnology for pharmaceutical and, mainly, for cosmetics purposes.