Objectives: To study the larvicidal effect of Vitex negundo Linn against mosquito larvae by larvicidal bioassay and in silico molecular docking studies. Methods: The larvicidal bioassay of Vitex negundo Linn was assessed by using WHO standard protocol and an in silico molecular docking study was performed by using Molegro Virtual Docker against Culex quinquifasciatus. The early third instar larvae of Aedes aegypti, Aedes albopictus and Culex quinquefasciatus were exposed to the extract concentrations in three replicates and different temephos concentration were taken as positive control and solvent control was also used. Results:The study results shows that of Vitex negundo Linn possess the potential larvicidal activity against third instar larvae of Culex quinquifasciatus when compared to Aedes aegypti L and Aedes albopictus. Percentage mortality and half-maximal effective concentration (EC 50 ) value were calculated against the above mentioned three species like wise Culex quinquifasciatus (83.77 ppm), Aedes aegypti (341.7 ppm), and Aedes albopictus (487.9 ppm). The highest larval mortality was found against Culex quinquifasciatus of 100 % at 500 parts per million. In silico molecular docking studies using Molegro Virtual Docker against Odorant binding protein (PDB: 2L2C) of Culex quinquifasciatus was performed as it showed better results in in vitro study. The results reveal that phytoconstituent like Vitexicarpin showed good docking scores against the Odorant Binding Protein 2L2C and the moldock score of Vitexicarpin was found to be -87.3733, whereas moldock score of standard Azadirachtin was found to be -110.77. Conclusion: The present study reveal that the Vitex negundo Linn possess the potential larvicidal activity against the Culex quinquifasciatus species.
Background: This work is envisaged to understand the use of various superdisintegrants and their drug release effect in the formulation of Ranolazine fast-dissolving tablets (FDTs). Materials and Methods: The FDTs were formulated by using direct compression methods using different superdisintegrants like sodium starch glycolate, croscarmellose sodium and crospovidone. The superdisintegrant's effect at different concentrations was studied with help of precompression studies such as Hausner's ratio, compressibility index, differential scanning calorimetry (DSC) and post-compression studies like friability, disintegration and dissolution studies. Results: The effect of various superdisintegrants on desired drug release was studied and its concentrations were optimized. Based on the evaluation results of various trials, the effective concentration was found to be 15mg/tab of crospovidone. It has a disintegration time of 25 sec and a cumulative percentage drug release of 99.77±0.41. Conclusion: In this study, Ranolazine FDTs were developed and successfully optimized. The ideal superdisintegrant and its concentration were selected. Among the various superdisintegrants, crospovidone was more effective compared to other superdisintegrants. Hence, it is recommended to use crospovidone as an ideal superdisintegrant in the Ranolazine FDTs formulations.
In globally, cancer is a second leading disease next to cardiovascular diseases in non-communicable diseases, which affect the all ages, sex, social status, ethnicity and primary cause of illness related death. Traditionally, systemic delivery drug systems like chemotherapy via oral capsule, injections of nanoparticles/micro particles, immunotherapy and others, which can inhibit or halt the progression of tumors. The short half-life of drugs which cannot achieve the targeted dose level to the tumor site and not able to target desired cell and commonly produces the organ toxicity. Recently, researchers have been attempting to direct delivery agents for cancer therapy. One of the best methods is a local therapy system, which deliver the drug directly via implantable procedure and it’s achieved the maximum concentration of the desire drug at the tumor site, non-target systemic exposure and minimize the organ toxicity to the patients. Biomaterial implants are widely used in the local concurrent delivery of chemotherapy and anti-angiogenic agents, local delivery of poly-chemotherapy, gene therapy as an alternative to drug delivery, scaffolds for cancer immunotherapy and polymer-based composites of drug molecules. There are different types of polymers like poly anhydride poly [bis (p-carboxy-phenoxy) propane-sebacic acid] copolymer [p(CPP:SA)], fatty acid dimer-sebacic acid copolymer (FAD-SA), poly (lactic-co-glycolic acid) copolymer (PLGA), poly (ε-caprolactone) (PCL), poly (glycerol monostearate-co-caprolactone), alginate and silica, used in successively cancer therapy. In order to minimize the risk of unwanted side effect of different types of biomaterials implants, it’s biocompatible to reduce the ability to elicit the inflammatory effect to the implanted area or the site. Therefore, the key role of choosing the appropriate and biocompatible implants to particular therapy is an indispensable. This should be validated with respect to risk benefit ratio in case of cancers. Biomaterial based implant local delivery systems provide more versatile and tailorable approach to against treatment of different types of the cancer.
BACKGROUND: Mucormycosis has been infesting the universe for a while back, often with no prompt treatments. The disease devastation is spreading at an alarming rate. Many researchers are still hoping for a good potential drug that could help the healthcare system in this tussle. Molecular docking is an in silico tool that has gained popularity over the last few decades. Knowing the mechanism of enzymatic action is aided by imitating membrane protein actions in binding ligands. AIM: The aim of this perspective is to determine whether an existing drug, daclatasvir, has antifungal activity. OBJECTIVE: The primary objective of this in silico study was to investigate the potential effects of the binding affinity of daclatasvir with the crucial protein (1XFF) of mucormycosis, as well as the binding pattern of the active site amino acids with the drug molecule. MATERIALS AND METHODS: To calculate the binding affinity of daclatasvir to the fungal protein 1XFF, Auto Dock Vina was used for molecular docking studies. The CDOCKER protocol was used to determine the receptor-ligand interaction by configuring various parameters. RESULTS: The docking energy of the ligand (daclatasvir) on the protein (1XFF) was found to be -16.7216 kcal/mol, while the interaction energy was found to be - 42.1314 kcal/mol. CONCLUSION: The binding pattern completely alters the dynamics of the protein, resulting in the breakdown of the fungal wall. The vital protein (1XFF) of Rhizopus oryzae is proposed as a possible protein target for the non-structural protein 5A inhibitor/antiviral drug daclatasvir in this study.
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