Current Drug Therapy - Volume 17, Issue 2, 2022

Backgrounds: Plant and derived herbal drugs have been used in the traditional medicine system to treat various human health complications from a very early age. Commercial products prepared from natural herbs have always been valuable for society in the form of health supplements to medicament. In ancient times, herbal products were mainly prepared from plants and derived phytochemicals. Plants contain a rich source of pure phytochemicals called secondary metabolites, and examples are flavonoids, glycosides, tannins, terpenoids, etc. Plants and their parts, including fruits, flowers, vegetables, etc., are the best source of Flavonoid class phytochemicals. Methods: Present work summarized the scientific information of karanjin for their beneficial health aspects and pharmacological activities, including its analytical aspects. In the present investigation, scientific data on karanjin have been collected from various scientific databases such as Google, Google Scholar, Science Direct, and PubMed and analyzed to know the beneficial health aspects of karanjin in medicine. Further pharmacological activity data has been collected and analyzed in the present work to know their biological potential in medicine. Analytical methods used for the separation, isolation, and identification of karanjin to standardize different natural products have also been discussed in the present work. Results: Scientific data analysis signified the biological importance of Flavonoid class phytochemicals in the medicine as they are well known for their anti-ischemic, vasodilatory, anti-bacterial, antiinflammatory, anti-oxidant, anti-viral, and anti-cancer activities. Scientific data analysis revealed the presence of karanjin in numerous medicinal plants such as Fordia cauliflora, Lonchocarpus latifolius, Millettia pinnata, Millettia pubinervis, Pongamia pinnata, and Tephrosia purpurea. Pharmacological activity data revealed the biological potential of karanjin against cancerous disorders, glucose metabolism abnormalities, gastrointestinal disorders, arthritis, inflammatory disorders, colitis, psoriasis, and brain-related disorders. However, analytical data signified the importance of RP-HPLC, TLC, HPTLC, UPLC-ESI-MS/MS, and HSCCC techniques in the medicine to quantify karanjin in different samples. Conclusion: Presented information about karanjin in this review paper will be beneficial to the scientific peoples of the world to know the beneficial health aspects of karanjin in medicine.

Human skin has been explored for decades as a potential route for the delivery of various substances. It has shown considerable promise for the delivery of medications into the systemic circulation. It is also beneficial to treat local skin symptoms through the skin itself. However, the rigid stratum corneum layer has served as the biggest barrier to transdermal drug delivery. Various methods have been designed to overcome the barrier of the stratum corneum layer to allow the molecule to pass through it. These methods have been broadly classified into chemical and physical approaches. This study is an overall review of the physical approaches being used in transdermal drug delivery for overcoming the stratum corneum layer. Physical approaches also include direct and indirect methods; we will be considering the direct approaches herein.

Rheumatoid arthritis (RA) is the most common musculoskeletal disease in the world. The clinical prospects have increased tremendously since the advent of biological agents as therapy options. NSAIDs such as indomethacin, celecoxib, and etoricoxib are used often in the treatment of RA but off-target effects decrease their use. DMARDs such as methotrexate and etanercept were also effective in the treatment of RA, but tolerance to methotrexate developed in many cases. Janus kinase inhibitors (JAKi) have also gained popularity as a treatment option for rheumatoid arthritis. Tofacitinib is the foremost JAK inhibitor used to treat RA as an individual agent or in combination with other DMARDs. The most frequently used route of administration for JAKi is oral. Since oral formulations of JAK inhibitors have a number of health hazards, such as systemic toxicity and patient noncompliance, topical formulations of JAK inhibitors have emerged as a preferable alternative for administering JAK inhibitors. Tofacitinib delivered topically seems to have the potential to eliminate or reduce the occurrences of negative effects when compared to tofacitinib taken orally. Given the scarcity of knowledge on the techniques for topical distribution of JAKi, more effort will be required to develop a stable topical formulation of JAKi to address the limitations of the oral route. The current review looks at JAK inhibitors and how they have been used to generate topical formulations of them.

Tyrosine Kinase (TK) is considered one of the important family members of the kinase family due to its important role in various cellular processes like cell growth, cell differentiation, apoptosis, etc. Mutation, overexpression, and dysfunction of tyrosine kinase receptors lead to the development of malignancy; thus, they are considered one of the important targets for the development of anti-cancer molecules. The tyrosine kinase family is majorly divided into two classes; receptor and non-receptor tyrosine kinase. Both of the classes have an important role in the development of tumour cells. Currently, more than 40 FDA-approved tyrosine kinase inhibitors are used to treat various types of cancers. Tyrosine kinase inhibitors mainly block the phosphorylation of tyrosine residue of the corresponding kinase substrate, so activation of downstream signalling pathways can be inhibited. The promising results of tyrosine kinase inhibitors in solid tumours have revolutionized oncology research. In this article, we summarized the role of some important members of the tyrosine kinase family in the development and progression of tumour cells and the significance of tyrosine kinase inhibitors in the treatment of various types of cancer.

Background: Coronary Heart Disease (CHD) patients are at risk of suffering from drug interactions, leading to a higher risk of mortality and morbidity among these patients. This study aims to identify the potential drug-drug interactions (PDDIs) and CHD patients' related factors. Methods: A cross-sectional study was performed among the CHD patients to identify the PDDIs from 2014 to 2017 at a Secondary Hospital. The PDDIs were categorized according to the interaction mechanism, onset, severity, and documentation. Results: Among 91 CHD patients, 151 PDDIs were identified consisting of pharmacokinetics mechanism and delayed onset, 50.33%, and 83.44%, respectively. Furthermore, there was a correlation between the number of PDDIs and the number of drugs (r = 0.496; p < 0.001). Conclusion: This study revealed that the more the drugs were prescribed to CHD patients, the more the PDDIs risk would occur. The regular monitoring of the CHD patient’s prescriptions is noteworthy to avoid the PDDIs.

Background: The evolving need and facilitation of topical formulations have risen in the present era. Topical industries are continually striving to satisfy patients with newer and innovative products. However, dry skin is the critical factor contributing to drug penetration into the skin. Objectives: The current research aims to develop cost-effective and commercially feasible industrial scale microemulsion of wheat germ oil to enrich skin hydration, enhancing the drug permeation rate. Methods: The Pseudo-ternary phase diagram was constructed for screening of microemulsion components. Wheat germ oil containing O/W microemulsion was prepared and evaluated for physicochemical parameters, thermodynamic stability study, globule size determination, enhancement of skin hydration, and skin permeation rate by ex vivo study. Results: The wheat germ oil containing microemulsion was prepared by incorporating tween 20 [surfactant] and ethanol [co-surfactant]. All physicochemical parameters were in the ideal range. Following the thermodynamic stability study, the TEM study showed globule size of optimized microemulsions in the range of 69.64 nm to 84.42 nm. The skin moisture tester showed a high hydration level for more than eight hours. An Ex vivo study revealed higher drug flux [Jss] of Pomegranate peel Extract [17.99 μg/cm2/h] with an enhancement ratio of 1.69. Conclusion: The topical formulation application has become challenging for researchers due to the skin's dryness and lower water content. However, the developed WGO microemulsion aids more penetration and is helpful in achieving higher drug flux. In addition, it is a cost-effective, easy to prepare, and patient-friendly drug delivery system.

Background: Pro-inflammatory mediators such as tumor necrosis factor-alpha (TNF-α), interleukin (IL), and oxidative stress are crucial players in the pathophysiology of inflammatory bowel disease (IBD) that contribute to perpetuating intestinal inflammation. Targeting them presents a novel approach to disease management. In the present study, the potential of an antiosteoarthritic ILinhibitor drug, diacerein (DIA), was investigated in 2, 4, 6-trinitrobenzene sulfonic acid (TNBS)- instigated ulcerative colitis (UC) in Wistar rats. A comparative study was also undertaken to investigate the potential of combination therapy of DIA with the standard drug 5-aminosalicylic acid (5-ASA) versus monotherapy. Methods: Colitis was developed by single intra-colonic administration of TNBS (100mg/kg); whereas drugs 5-ASA (25.5 mg/kg), DIA (100 mg/kg), and DIA+5-ASA (100 + 25.5 mg/kg) were administered orally for five days post-induction to various groups of rats. Parameters like disease activity score, colon/ body weight ratio, colon length, diameter, and gut pH were assessed, and histopathological analysis was carried out. Biochemical markers of colonic inflammation such as IL-1β, TNF-α, reduced glutathione (GSH), and malondialdehyde (MDA) were also estimated. Results: Combination of DIA and 5-ASA demonstrated the most significant reduction of the colon to body weight ratio and disease activity score. It prominently restored the colon length, diameter, and gut pH to normal. It attenuated the biochemical alterations induced by TNBS, indicating a highly significant defensive outcome against colonic inflammation. The histopathological report demonstrated the renovating effect of the combination of disrupted colonic histology with minimally distressing liver, stomach, or pancreas compared to individual drugs. Conclusion: The combination remarkably downregulated the level of inflammation by suppressing both provocative cytokines and reactive oxygen species production. It can be evaluated further used in a clinical setup as a novel and promising drug therapy for UC.