Recent Patents on Drug Delivery & Formulation - Volume 14, Issue 2, 2020

The traditional oral dosage forms (tablets, capsules, syrups, and elixirs) suffer from various disadvantages. They are pretty challenging to administer to patients with dysphagia, mucositis, and vomiting tendency. Therefore, gaining patient compliance using conventional dosage forms is highly cumbersome. One of the most transformative and innovative approaches to overcome such challenges is Orodispersible Films, a Novel Drug Delivery System. They are easy to consume, no need to chew or swallow and they do not even require water for consumption. Therefore, several drugs have been converted into orodispersible films to gain patient compliance. With the advent of these film formulations, new innovations are erupting and accordingly, companies in India are actively protecting them by filing ordinary patent applications in India and internationally under the Patent Cooperation Treaty. Patenting in India poses unique patentability challenges when compared with rest of the world. Nonetheless, meeting all the challenges and obtaining a valid patent not only help in recouping the cost involved in developing new drugs and its novel drug delivery systems but also helps in taking legal action against alleged infringers. This review article identifies key active Indian players in the domain of ODF based on their patent filings in India (and abroad) and also identifies the challenges they face to obtain a grant.

Onychomycosis is a fungal infection of the nail plate or nail bed that leads to the gradual destruction of the nail. The main difficulties in the treatment of onychomycosis refer to the duration of treatments and their side effects. Thus, it becomes relevant to look for new therapeutic alternatives in the treatment of such common diseases that are efficient without causing the undesirable side effects on the patient's body. In this way, the objective of this study was to develop an anthroposophical formula for the treatment of onychomycosis, based on Phosphorus and Formica rufa, from an extensive bibliographic survey on the functions of these components, evaluating within the principles of Anthroposophy. Considering the set of knowledge and practices on the use of these components, it was possible to arrive at a proposal therapy that can be effective for the treatment of onychomycosis. After an extensive review of several existing patents, it was observed that formulations containing Phosphorus and Formica rufa together have not been described in other studies. Subsequently, our research group published a patent of the anthroposophical formula using these two components, with the number BR1020180750755, which will be efficient to help the recovery of nails, and facilitate normal growth.

Skin cancer, among the various kinds of cancers, is a type that emerges from skin due to the growth of abnormal cells. These cells are capable of spreading and invading the other parts of the body. The occurrence of non-melanoma and melanoma, which are the major types of skin cancers, has increased over the past decades. Exposure to ultraviolet radiations (UV) is the main associative cause of skin cancer. UV exposure can inactivate tumor suppressor genes while activating various oncogenes. The conventional techniques like surgical removal, chemotherapy and radiation therapy lack the potential for targeting cancer cells and harm the normal cells. However, the novel therapeutics show promising improvements in the effectiveness of treatment, survival rates and better quality of life for patients. Different methodologies are involved in the skin cancer therapeutics for delivering the active ingredients to the target sites. Nano carriers are very efficient as they have the ability to improve the stability of drugs and further enhance their penetration into the tumor cells. The recent developments and research in nanotechnology have entitled several targeting and therapeutic agents to be incorporated into nanoparticles for an enhancive treatment of skin cancer. To protect the research works in the field of nanolipoidal systems various patents have been introduced. Some of the patents acknowledge responsive liposomes for specific targeting, nanocarriers for the delivery or co-delivery of chemotherapeutics, nucleic acids as well as photosensitizers. Further recent patents on the novel delivery systems have also been included here.

Background: Cancer is a condition in which some cells in the body grow uncontrollably and can also spread in other parts of the body. Among males, oral and lung cancers account for 25 % cancer deaths, while in females, breast and oral cancers cause 25% death. Breast and cervical cancers are the underlying cause of the high mortality rate among women. Owing to limitations of conventional cancer therapy like low drug specificity, less solubility, multidrug resistance, poor access to tumor cells and low bioavailability development of environmentally sensitive and target specific nanocarriers are imperative. Objective: The objective of this study is to review advancements made in techniques to synthesize Mesoporous Silica Nanoparticles (MSN’s) as well as strategies to functionalize its silanol group for site-specific drug release in the tumor environment and to review recent patents published regarding it. To describe rationale for selection of MSN’s for cancer theranostics amidst other nanocarriers developed. Methods: In the first section of this review, the physical and chemical properties of MSNs making it an ideal delivery system for cancer therapy and diagnostics are discussed. In the next section, various techniques involved in synthesizing and loading MSNs, including the influence of basic components of MSNs and reaction conditions on its properties are reviewed. Then the wide application of MSNs and various exogenous and endogenous stimuli harnessed for site-specific delivery of cargo and recent patents on modifying environmental conditions for large scale synthesis of MSNs and its active targeting for cancer treatment and bioimaging are discussed. Results: Physico-chemical properties and synthetic protocols of MSNs justifying them to be a promising nanovector to overcome the ill effects of traditional chemotherapy. The superlative attributes of MSNs including, tunable size, morphology, high load volume, stability, ease of modifying external and internal surface leverage applications in various dimensions of therapeutics, diagnostics, and combinatorial drug delivery. MSNs surface functionalization can be harnessed for passive and active targeting by either coating the surface with polymers or attaching various ligands. Conclusion: An ideal nano-carrier must have high loading efficiency, easily detectable, and must have stimuli's sensitive, site-specific drug release. The patent study explores new dimensions on MSNs synthesis by claiming new cost-effective templates and silica source, a more safe environment for synthesis, reducing synthesis steps, duration of reaction, effective loading of low solubility drugs by magnetized nanocarriers, pathogen-specific release and development of novel photoluminescent rechargeable MSNs under mild conditions. It’s a challenging task for researchers to successfully translate their prototypes to industries and make it feasible for commercialization. We can further work on excellent targeting concepts and architecture of MSNs for the increased opportunity in cancer theranostics.

Background: Dental caries originate due to the localized dissolution of the hard tissues of teeth, mainly caused by acids, developed by the presence of microorganisms in the biofilm (dental plaque) on the surface of teeth causing “cavities”. Commercially available liquid mouthwashes containing synthetic active ingredients possess limitations like teeth staining, higher alcoholic content, taste disturbances, xerostomia, and stability issues. Objective: To make the solid preparation for oral hygiene (US6428770B1) in the form of herbal effervescent mouthwash tablet (CN106619318A, US8728446B2) using Azadirachta indica and Curcumin having antimicrobial, antibacterial, antiplaque, and anti-inflammatory activity. Methods: The optimization study of effervescent granules was performed by 33 factorial design. A total of 27 preliminary experimental batches were prepared by the fusion method, varying the amount of citric acid, tartaric acid, and sodium bicarbonate. A complex of curcumin was prepared with hydroxyl propyl β-cyclodextrin and further examined by scanning electron microscopy. The prepared tablets were evaluated for pre and post-compression parameters. The in vitro antimicrobial study was performed by Agar well diffusion method against S. mutans. Results: All the experimental batches of effervescent granules were evaluated for pH, effervescent time, and CO2 content. Six batches were further selected for final tablet preparation. The results of the pre-compression parameters revealed excellent flow properties and post-compression parameters; the results were also significant. The antimicrobial study revealed the F3 as a final best formulation. Conclusion: The developed herbal formulation (F3) has a good potential to maintain oral hygiene as compared to alcoholic mouthwash and further studies may be necessary to confirm the efficacy of the formulation since only a single bacterial strain was assayed.