A targeted drug delivery system is the need of the hour. Guiding magnetic iron oxide nanoparticles with the help of an external magnetic field to its target is the principle behind the development of superparamagnetic iron oxide nanoparticles (SPIONs) as novel drug delivery vehicles. SPIONs are small synthetic γ-Fe 2

Licochalcone A (I), isolated from the roots of Chinese licorice, is the most promising antimalarial compound reported so far. In continuation of our drug discovery program, we isolated two similar chalcones, medicagenin (II) and munchiwarin (III), from Crotalaria medicagenia , which exhibited antimalarial activity against Plasmodium falciparum . A library of 88 chalcones were synthesized and evaluated for their in vitro antimalarial activity. Among these, 67, 68, 74, 77, and 78 exhibited good in vitro antimalarial activity against P. falciparum strains 3D7 and K1 with low cytotoxicity. These chalcones also showed reduction in parasitemia and increased survival time of Swiss mice infected with Plasmodium yoelii (strain N-67). Pharmacokinetic studies indicated that low oral bioavailability due to poor ADME properties. Molecular docking studies revealed the binding orientation of these inhibitors in active sites of falcipain-2 (FP-2) enzyme. Compounds 67, 68, and 78 showed modest inhibitory activity against the major hemoglobin degrading cysteine protease FP-2.

Poor bioavailability of Docetaxel (DCT) arising due to its low aqueous solubility and permeability limits its clinical utility. The aim of the present study was to develop DCT loaded self-emulsified drug delivery systems (D-SEDDS) and evaluate its potential ability to improve the oral bioavailability and therapeutic efficacy of DCT. D-SEDDS were characterized for their in vitro antitumor activity, in situ single pass intestinal perfusion (SPIP), bioavailability, chylomicron flow blocking study and bio-distribution profile. The D-SEDDS were prepared using Capryol 90, Vitamin E TPGS, Gelucire 44/14 and Transcutol HP with a ratio of 32.7/29.4/8.3/29.6 using D-Optimal Mixture Design. The solubility of DCT was improved upto 50 mg/mL. The oral bioavailability of the D-SEDDS in rats (21.84 ± 3.12%) was increased by 3.19 fold than orally administered Taxotere (6.85 ± 1.82%). The enhanced bioavailability was probably due to increase in solubility and permeability. In SPIP, effective permeability of D-SEDDS was significantly higher than Taxotere. D-SEDDS showed 25 fold more in vitro cytotoxic activity compared to free DCT. Chylomicron flow blocking study and tissue distribution demonstrated the intestinal lymphatic transport of D-SEDDS and higher retention in tumor than Taxotere. The data suggests that D-SEDDS showed desired stability, enhanced oral bioavailability and in vitro antitumor efficacy.

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Blood and plasma are the biomatrices traditionally used for drug monitoring and their pharmacokinetic profiling. Blood is the circulating fluid in contact with all organs and tissues of body and thus is the most representative fluid for measuring systemic drug levels. However, venipuncture suffers from the caveat of being an invasive technique which often makes people reluctant to participate in clinical studies. Thus, there is a need for noninvasive bio-fluids that are ethically appropriate, cost-efficient and toxicologically relevant. These alternate bio-fluids may prove clinically useful as alternatives to plasma/serum in therapeutic drug monitoring, pharmacokinetic and toxicokinetic studies, doping control in sports medicine and to monitor local adverse effects. These may be of particular interest in the case of special population groups such as neonates, children, the elderly, terminally ill patients and pregnant or lactating women, and offer the advantage of circumvention of the demand for specialized personnel for sample collection. This review describes such noninvasive bio-fluids (saliva, sweat, tears and milk) that have been considered for pharmacokinetic drug analysis, emphasizing their sample preparation, its associated difficulties and their correlation with plasma.

Supervisor’s supporting comments Wahajuddin has shown strong enthusiasm with equal intensity of hard work in bioanalytical research since the day he joined as a scientist in this department. His intrinsic learning abilities made him acquire deep knowledge in the area of bioanalysis and he quickly became competent in conducting regulatory/exploratory studies in pharmacokinetics, biopharmaceutics and drug metabolism – harnessing the strengths of bioanalysis. Due to his skills and knowledge in advanced pharmaceutical analysis tools and techniques, he has also been given the responsibility to work as course coordinator for MS (Pharm.) Pharmaceutics at the newly established National Institute of Pharmaceutical Education and Research, which is an institute of national importance under the aegis of the Ministry of Chemicals and Fertilizers, Government of India. Through our Young Knowledge Promotion Initiative and Young Leadership Promotion Initiative, Wahajuddin was given the responsibility of being the corresponding author and first co-author in the majority of papers that have been published by our group, since he was instrumental in generating ideas, planning and executing the studies, compiling and analyzing the data and in writing and communicating the manuscripts. This enabled him to publish very good work in journals such as the Journal of Chromatography B, the Journal of Separation Science, Food & Chemical Toxicology, the Journal of Nutritional Biochemistry and Menopause within a very short period. Many other manuscripts are at various stages of communication and publication. His contribution also resulted in filing a patent application from the Central Drug Research Institute in 2007 (patent No.: #0081NF2007). He has also presented his work at many international conferences, symposia and seminars. He recently presented his work at the International Pharmaceutical Federation Pharmaceutical Science World Congress 2010 in association with American Association of Pharmaceutical Scientists Annual Exposition 2010 held on 14–18 November 2010 in New Orleans, USA. I am sure that he will achieve even greater feats in times to come and strongly recommend his candidature for Bioanalysis: Young Investigator 2011. Nominated by: Girish Kumar Jain, Deputy Director & Head, Division of Pharmacokinetics & Metabolism, Central Drug Research Institute, CSIR, Lucknow, India. gk_jain@cdri.res.in

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There are regular reports of extrapulmonary infections and manifestations related to the ongoing COVID-19 pandemic. Coronaviruses are potentially neurotropic, which renders neuronal tissue vulnerable to infection, especially in elderly individuals or in those with neuro-comorbid conditions. Complaints of ageusia, anosmia, myalgia, and headache; reports of diseases such as stroke, encephalopathy, seizure, and encephalitis; and loss of consciousness in patients with COVID-19 confirm the neuropathophysiological aspect of this disease. The brain is linked to pulmonary organs, physiologically through blood circulation, and functionally through the nervous system. The interdependence of these vital organs may further aggravate the pathophysiological aspects of COVID-19. The induction of a cytokine storm in systemic circulation can trigger a neuroinflammatory cascade, which can subsequently compromise the blood-brain barrier and activate microglia- and astrocyte-borne Toll-like receptors, thereby leading to neuronal tissue damage. Hence, a holistic approach should be adopted by healthcare professionals while treating COVID-19 patients with a history of neurodegenerative disorders, neuropsychological complications, or any other neuro-compromised conditions. Imperatively, vaccines are being developed at top priority to contain the spread of the severe acute respiratory syndrome coronavirus 2, and different vaccines are at different stages of development globally. This review discusses the concerns regarding the neuronal complications of COVID-19 and the possible mechanisms of amelioration.