Recent Patents on Anti-Infective Drug Discovery - Volume 14, Issue 1, 2019

There is a need for the development of liposomes based nanomedicines formulation for better efficacy and safety of the available drugs in the market. Liposomes have various applications in the field of pharmaceutical and medical field for their drug target potential, diagnostic importance and imaging techniques. Natural plant based drugs and their derivatives have been used in the medicine, nutraceuticals, perfumery, cosmetic and beverages industry. More than half of the prescribed drugs in the worldwide are mainly derived from different natural sources. Development of plant derived product is an emerging field of food, pharmaceutical and health industries. Plants belonging to the Gentianaecae family are well known for their bitter taste and Swertia chirata is one of best plants among them. Various active phytochemical of Swertia chirata are bitter secoiridoids like gentiopicroside, amarogentin, swertiamarin, isovitexin and isogentisin. People use different species of Swertia in the form of decoction, infusion, paste and juice for the treatment of fever and enteric diseases. Swertia chirata possesses anticarcinogenic, antioxidative, hypoglycemic, antihepatotoxic, antimalarial, anti-inflammatory and antimicrobial activities. Amarogentin, a bitter secoiridoid glycoside present in Swertia chirata plant is an activator of human bitter taste receptor. Pharmacologically, amarogentin has antibacterial, antihepatitis, anticholinergic and chemopreventive activities, moreover, amarogentin has been proven for their anti-lieshmanial activity. Other studies also suggested that amarogentin acts on liver carcinogenesis, skin carcinogenesis and reduced tumour progression. In the present review, we have collected and compiled the data regarding biological sources, ethnomedicinal uses, phytochemistry, anticancer and anti-infective potential of amarogentin. For better understanding of various aspects of amarogentin, we have also discussed Swertia chirayita in a very concise manner. Further data related to various patents on amarogentin have also been discussed in this manuscript. However, we also admit that new advance biological research will also increase the medicinal and pharmacological value of amarogentin. Information regarding the chemistry of amarogentin, its biological sources, bioavailability as a pharmacological agent for the treatment and management of skin disorders and various forms of cancers will be beneficial to the scientists in the medicinal field.

Background: In recent decades, enormous efforts for different drug discovery processes have led to a number of drug molecules available today to overcome different challenges of the health care system. Unfortunately, more than half of these drugs are listed in either BCS (biopharmaceutical classification system) class II/ IV or both are eliminated from the development pipeline due to their limited clinical use. A nanotechnological approach bears much hope and lipoidal fabrication is found to be suitable for the delivery of such drugs. Nanoemulsion based gel i.e. nanoemulgel out of different nanolipoidal formulations has been found to be a suitable approach to successful drug delivery through topical routes. In past few years many herbal and synthetic active pharmaceutical ingredients (APIs) has been patented as nano sized emulsified gel for various therapeutic activities. Methods: Nanoemulgel is basically an emulsion-based topical gel formulation, where nanosized emulsion globules can be prepared with the help of high energy or low energy methods and further converted into nanoemulgel by adding a suitable gelling agent. Nanoemulgel fabrication enlists various kinds of polymeric materials, surfactants and fatty substances of natural, synthetic and semi-synthetic nature with a globule size range from 5 to 500 nm. Results: Nanoemulgel can be applicable to various acute and chronic diseases through topical routes. Conclusion: Nanoemulgel preparations of many recently approved drugs are being used successfully in different areas of health care and have re-defined the significance of topical route of delivery as compared to other routes. However, along with various improvements in the current state of the delivery system, the safety factor needs to be taken into account by toxicological studies of the materials used in such formulations.

Backgrounds: Acne vulgaris is a common chronic skin disease that affects around 9.4% (approx. 650 million people) of the global population. Growing research in the field of nanomedicine over the years has now been exploited in management of various human disorders. The nanomedicine concept has an immense opportunity for the effective management and control of acne disease by designing a novel, low-dose topical delivery system. Topical nanoemulsion-based gel preparations are said to have various benefits over the conventional formulations. The recent patents on topical anti-acne formulation (US 7241456B2; US 6897238B2; US 6284234B1) provided the concept to design thymol loaded nano-emulgel for topical application in acne. Methods: The objective of the current investigation was to design a thymol loaded nanoemulgel preparation by exploiting low-energy emulsification method for topical application in acne. Furthermore, developed formulation was characterized for thermodynamic stability, mean droplet size, zeta potential, drug content and in-vitro drug diffusion study. Results: The optimized thymol loaded nanoemulsion was found to be 13.60±0.117 nm with PdI 0.197±0.008. Nanoemulsions will provide an enormous surface area for better penetration of therapeutic agent into the pilosebaceous region, resulting better efficacy. Conclusions: From the above studies, it concluded that aqueous-based gel vehicle of the developed formulation system exploited for topical delivery has moisturising properties which can improve local tolerability also.

Lyme’s Disease (LD) is a severe, rapidly growing, broad spectrum chronic infection caused by the bacterium ‘Borrelia (B.) burgdorferi', which can be easily transmitted through the bite of certain species of ticks. The prevalence of LD is swiftly mounting in the present scenario in many countries from species to species. Although Lyme’s infection is now detectable via serologic examination of early and late Lyme neuroborreliosis (LNB), the management of persistent symptoms is still fraught with quora of doubt and debate. LD is a multisystem spirochete which results after the dissemination of B. burgdorferi from a dermal inoculation site after a tick bite. Lyme's infection can easily get transmitted to the central nervous system and develop various neurological symptoms due to inflammation and an autoimmune response from body may lead to life-threatening “Lyme Borreliosis”. The neurological symptoms are well mixed in presentation, late and confusing to get differentiated easily from other diseases. The use of antibiotics in post Lyme infection with neurological complications is still a topic of debate. Babesiosisstates, and human ehrlichiosis' the two other diseases, are associated with the same ticks that spread the LD. However, the prevalence of diagnosed human cases is usually much lower than that of actual cases of LD due to misdiagnosis, late diagnosis or undiagnosis at y such lateral neuroinfection stage after the tick bite. The current review focuses on the molecular neuropathology and current advancements in LD. There are very few patents or discoveries made on borrelia infection, drawing attention towards more focused and targeted research for the cure.

Background: Wolbachia is the most common endosymbiotic bacteria in insectborne parasites and it is the most common reproductive parasite in the world. Wolbachia has been found worldwide in numerous arthropod and parasite species, including insects, terrestrial isopods, spiders, mites and filarial nematodes. There is a complicated relationship between Wolbachia and its hosts and in some cases, they create a mutual relationship instead of a parasitic relationship. Some species are not able to reproduce in the absence of infection with Wolbachia. Thus, the use of existing strains of Wolbachia bacteria offers a potential strategy for the control of the population of mosquitoes and other pests and diseases. Methods: We searched ten databases and reviewed published papers regarding the role of Wolbachia as a promising drug target and emerging biological control agents of parasitic diseases between 1996 and 2017 (22 years) were considered eligible. Also, in the current study several patents (WO008652), (US7723062), and (US 0345249 A1) were reviewed. Results: Endosymbiotic Wolbachia bacteria, which are inherited from mothers, is transmitted to mosquitoes and interferes with pathogen transmission. They can change the reproduction of their host. Wolbachia is transmitted through the cytoplasm of eggs and have evolved different mechanisms for manipulating the reproduction of its hosts, including the induction of reproductive incompatibility, parthenogenesis, and feminization. The extensive effects of Wolbachia on reproduction and host fitness have made Wolbachia the issue of growing attention as a potential biocontrol agent. Conclusion: Wolbachia has opened a new window to design a costly, potent and ecofriendly drug target for effective treatment and elimination of vector-borne parasitic diseases.