Prof. Rafik Karaman
Bioorganic Chemistry, College of Pharmacy, Al-Quds University, Jerusalem, Palestine.

Short Biosketch

ISBN 978-81-19217-61-8 (Print)
ISBN 978-81-19217-62-5 (eBook)
DOI: 10.9734/bpi/napr/v2

This book covers key areas of pharmaceutical research. The contributions by the authors include phytochemistry, medicinal applications, anti cancerous potential, flavonoids, pharmacology, omicron variants, mutant variety, bioanalytical method, chromatographic separation, medicinal herbs, trace elements, toxic elements, plant drugs, antiepileptic activity, epilepsy, hypersynchronous discharges, anti-diabetic activity, neurodegenerative diseases, reactive oxygen species, tumor necrosis factors, gynecology, Nifedipine’s solubility, metal chelating, scavenging activity, anaerobic microorganism, inflammation, hormonal therapy, anti-infection medications, pharmaceutical dosage, postpartum haemorrhage, haemodynamic stability, muscle coordination, anxiolytic activities. This book contains various materials suitable for students, researchers and academicians in the field of pharmaceutical research.

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Chemoprevention is a new approach that employs natural plant and herbal products to prevent, delay, or even halt the progression of cancer, which is the second most common cause of death after cardiovascular disease and a major cause of mortality in affluent nations. In the pursuit of anti-neoplastic effects, traditional plant remedies are often combined with synthetic drugs. Capparis decidua, a plant species, has been found to possess several pharmacological properties, including anti-diabetic, anthelmintic, antibacterial, antifungal, analgesic, anti-nociceptive, anti-rheumatic, hypo-lipidemic, anti-tumor, anti-giardial, antioxidant, anti-inflammatory, hepato-protective, and anticonvulsant effects, among others. The caper plant's incredible bioactivity is attributed to its various phytochemicals, such as alkaloids (capparisinine, capparisine, stachydrine, and iso-codonocarpine), phenolics, flavonoids, sterols, and fatty acids. This section covers the traditional applications, phytochemistry, and pharmacology of Capparis decidua, which has tremendous potential with various mechanisms to address the research gap for future researchers.

Omicron: A Grim Reality Amidst COVID-19

Saima Mazhar, Farzeen Tanwir, Ayesha Mehwish, Yasmeen Mahar, Anum Baqar, Maryam Faiz Quereshi, Areeba Younis, Ariba Naveed, Syed Wajahat Haseeb, Mahail Khan, Mariya Azam Khattak

Novel Aspects on Pharmaceutical Research Vol. 2, 20 May 2023, Page 11-20

Since the outbreak of the plague Covid-19, which has killed more than 5.57 million people worldwide, the world has been in pain for the past two and a half years. The spread of new coronavirus Omicron variants after alpha, beta, gamma, and delta continues. The virus, which was discovered in Botswana and South Africa in November, has spread rapidly throughout the world in recent weeks, outpacing any previously known coronavirus variant. When compared to other variants, Omicron has been shown to be highly contagious and less receptive to vaccines. November 26, 2021, was when the omicron variant was classified as a variant of concern by the WHO (CDC, 2021) [1]. The goal of this study was to provide a brief overview of what we already know about the Omicron virus and what more needs to be learned about its various variants.

The Development and Validation of RP-HPLC Method for Lamivudine, Dolutegravir, and Tenfovir in Human Plasma

Padmavathi Sakinala, Shaik Abdul Rahaman, J. Naga Sharmila, M. Sireesha, G. Pujitha

Novel Aspects on Pharmaceutical Research Vol. 2, 20 May 2023, Page 21-40

The present work aimed to develop a simple, rapid, and accurate method for the estimation of Dolutegravir, Lamivudine and Tenofovir disoproxil fumarate in human plasma, as per US-FDA guidelines. Moreover and the present method is the first for the estimation of this combination in a biological matrix. For the estimation of Lamivudine, Dolutegravir, and Tenfovir disoproxil fumarate in human plasma using the Cobicistat as internal standard by RP-HPLC (Reverse Phase-High Performance Liquid Chromatographic) technique, a straightforward, precise, and accurate method has been developed. The pure drug samples of Dolutegravir, Lamivudine and Tenofovir in were purchased from Selleck chem LLC supplied by Pro lab marketing. HPLC grade Acetonitrile, HPLC grade Methanol and all other chemicals were obtained from Merck chemical division, Mumbai. The Chromatographic separation was achieved on discovery C18, 250 mm x 4.6 mm, 5\(\mu\), Column at 300C temperature.

The separation was achieved employing a mobile phase consists of 0.1% v/v Ortho phosphoric acid and Acetonitrile taken in the ratio of 65:35 (v/v). The flow rate was maintained at 1.0 ml/min, detection wave length was 277 nm. Retention time of Lamivudine, Dolutegravir and Tenfovir were found to be 2.994 min, 4.350 min and 5.688 min respectively. The peaks were found to be free of interference. The method was validated over a dynamic linear range of 60-2400 ng/ml, 190-7600 ng/ml, and 18-720 ng/ml for Lamivudine, Dolutegravir and Tenfovir respectively, with a Correlation coefficient of 0.998. The precision and accuracy of samples of six replicate measurements at lower limits of quantification level were within the limits. The analytes were found to be stable in human plasma at -28°C for 37 days. The determination of Lamivudine, Dolutegravir, and Tenfovirin in human plasma is appropriate due to the stability, sensitivity, specificity, and reproducibility of this method. According to US-Food and Drug Administration guidelines, the reported method was validated, and it was discovered to be substantially within the acceptable range.

The main aim of the present research work is to determine the trace elemental concentration in Andrographics paniculata (A. paniculata) and Aegle marmmelos (A. marmmelos) which are growing in Telangana using against various diseases by EDXRF Technique. X-ray fluorescence spectrometer is one of the most widely used and versatile technique was used to study the trace element analysis. In this present work we measured thirteen elements and determine their elemental composition presence in selected medicinal plant samples of A. paniculata and A. marmmelos (by using EDXRF technique). From this it should be noted that, the variation in elemental composition of same plants from different regions, which can be compared with Standard certified values of NIST 1515 apple leaf given a good agreement. The variation in elemental composition can be changing of climate conditions and various mechanisms of plants. It is hoped that our elemental composition data of these medicinal plants available in Telangana region is very useful to pharmaceutical labs for invention of new drugs used for curing various diseases.

Activity of Some New Substituted Fluoro Benzothiazole Derivatives as Antiepileptics

I. Shanmukha , M. Vijay Kumar, E. Jayachandran , B. C. Revanasiddappa

Novel Aspects on Pharmaceutical Research Vol. 2, 20 May 2023, Page 51-58

The present study aimed to investigate the antiepileptic activity of fluoro substituted benzothiazole derivatives (FBTDs) in experimental induced epilepsy in mice. The investigation of new antiepileptic drugs is the study of synthetic compounds that may belong to new structural classes and exhibit desirable effects with more beneficial effects than existing drugs. Epilepsy is a tendency to have recurrent seizures. It can affect anyone, at any age, from any walk of life. It is one of the most common serious neurological conditions. The acute oral toxicity was determined as per OECD guideline 423 and minimum effective dose was also determined for pharmacological screening. The antiepileptic activity of FBTDs was studied against maximal electroshock (MES) and strychnine (1 mg/kg, s. c.) induced seizures in mice. In MES test, the duration of tonic hind limb extension was significantly reduced by all FBTDs at a dose of 100 mg/kg except, P-3, and OX-9 whereas in strychnine induced model, the seizure latency was sustained by all FBTDs at a dose of 100 mg/kg except P-4. P-7 and OX-9. The novels synthesized FBTDs exhibit anticonvulsant activity, The ticonvulsant action of FBTDs is better against strychnine induced seizures than MES seizures. P-1, P-2, P5 and P-9 were shown significant anticonvulsant activity against both MES and strychnine induced models.

A Review on the Pharmacological Effects of Curcumin in Diabetes, Cancer, and Neurodegenerative Diseases

Nidhi Agrawal , Hasnain Raza , Meenakshi Jaiswal , S. K. Lanjhiyana, Manoj Kumar Sahoo

Novel Aspects on Pharmaceutical Research Vol. 2, 20 May 2023, Page 59-71

As a diet-derived agent, curcumin has been used traditionally in many forms for the treatment of inflammation and pain but most of the recent studies uncovered the role of curcumin as an antidiabetic, anti-carcinogenic, anti-infectious, antidepressant, and antipsychotic agent. This dietary supplement has the ability to block a number of cells signaling pathways at various levels which underlies its diverse effect. By modulating cell cycles and interacting directly with molecular targets like glutathione peroxidase, nuclear factor kappa-B cells, cyclooxygenase-2, hepatic superoxide dismutase, reactive oxygen species tumor necrosis factors, etc. curcumin can prevent the development of cancer. In this chapter, we demonstrated the therapeutic effects of curcumin in various cancers, neurodegenerative disorders, microbial infections, and diabetes interconnected with its molecular pathways during preclinical trials.

The aim of the study is to reinvestigate the solubility property of NIfedipine as a chemical for deeper understanding of its pharmacodynamics and efficacy. Nifedipine is chemically dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, a dihydropyridine derivative used frequently as anti-hypertensive. It is a L- type calcium channel blocker (CCB). There were only a few analogical inconsistencies between Nifedipine's clinical output report and chemical investigation of solubility. By the words of pharmacology books it is a lipophilic substance. But ardent logical question then arises about how being a lipophilic substance it can be used in pregnancy complications like eclampsia and pre-eclampsia without causing any hypotensive crisis in the growing foetus. The ambition of this research is to conduct a re-check and proper quantification of partition co-efficient (logP) of Nifedipine and clarify such discrepancy and rectify if any technical miscalculation during its property verification after discovery. The method used is the “gold standard” shake-flask method followed by analysis using UV-spectrophotometry.

Areca catechu L. Nut Extracts' Phytochemical Extraction and Comparative Investigation of their Antioxidant Properties

A. Ajesh Kumar, S. S. Syed Abuthahir , Hassan Y. Aboul-Enein

Novel Aspects on Pharmaceutical Research Vol. 2, 20 May 2023, Page 83-96

This chapter aims to compare the antioxidant properties of different solvent extracts of Areca catechu L. The FRAP assay demonstrated that all Areca catechu L. nut extracts have antioxidant capabilities because their IC50 values are lower than that of ascorbic acid. The remaining antioxidant assays, such as DPPH radical scavenging, H2O2 scavenging, and Fe2+ chelating, revealed higher antioxidant activities in ethyl acetate extract and nonpolar solvent extracts such as n-hexane and chloroform. Half maximal inhibitory concentration (IC50) of ethyl acetate and n- hexane extracts of Areca catechu L. nut is less than that of the IC50 of ascorbic acid in DPPH radical scavenging assay and hydrogen peroxide scavenging activity respectively. Antioxidant properties of Areca catechu L. nut vary depending upon the different solvent extract. More research on the therapeutic effects of Areca catechu L. nut will be conducted as a result of the isolation of components from various solvent extracts.

A Detailed Review on Acne vulgaris

T. V. Kadam, A. B. Darekar

Novel Aspects on Pharmaceutical Research Vol. 2, 20 May 2023, Page 97-108

This study focuses on the causes and treatments options for acne vulgaris. The most well-known pilosebaceous follicle skin condition, acne vulgaris is characterized by papules, knobs, growths, comedones, pustules, and regular scars that are primarily dispersed on the face, middle, and upper back. Inflammation of pimples is a common skin condition that affects people of all ages. The gram-positive anaerobic microorganism Propionibacterium acnes, which is regarded as discharge-framing microorganisms, causes inflammation of the skin.  For the treatment of inflammation of the skin, several restorative plant parts and dermatological drugs are used.  The mainstay of treatment for topical specialists includes benzoyl peroxide, anti-infection medications, retinoid, and others; they may be administered in combination. Systemic treatment, which includes isotretinoin, hormonal therapy, and oral anti-microbials, must be chosen based on the needs of the patient. Photographic assistance is also helpful for them when receiving physical therapy for a certain sort of injury evacuation. They eventually run into treating dermatologists because there are numerous traditional and cutting-edge topical and systemic experts available to treat acne vulgaris.

A Novel UPLC Method Development and Validation of Mirabegron Determination in Pharmaceutical Dosage Forms

B. Anupama, A. Viswanath, . Azizunnisa, Md. Vaseemunnisa

Novel Aspects on Pharmaceutical Research Vol. 2, 20 May 2023, Page 109-119

The main aim of this investigation is to develop an accurate, simple and fast Ultra-Performance Liquid Chromatography (UPLC) method for the determination of Mirabegron in pharmaceutical dosage forms Mirabegron is a drug that eases the symptoms of overactive bladder. Mirabegron activates the \(\beta\)3 adrenergic receptor in the bladder's detrusor muscle, causing muscular relaxation and bladder capacity expansion. There have been a few measurement techniques found, however they are cumbersome and time consuming. The amount of Mirabegron in pharmaceutical dosage forms was determined using a simple, exact, precise and useful UPLC technique that was established in the current study. On Acquity BEH C18 (50*3.0mm. 1.7m), chromatographic separation was achieved by the isocratic elution mode using mobile phase containing Potassium di hydrogen phosphate: Methanol (70:30) v/v with a UV detection wavelength of 254 nm. Validation of the developed UPLC method was done as per the guidelines of the International Conference on Harmonization in terms of system suitability, precision, accuracy, specificity, sensitivity, linearity, and robustness.

To prevent postpartum haemorrhage (PPH), the routine administration of a uterotonic agent like oxytocin is standard practice. Failure of prophylaxis with oxytocin occurs commonly, necessitating the use of further oxytocin or other treatments to maintain haemodynamic stability. Oxytocin has its limitations as it requires cold storage and transport, and in low-resource settings, the cold chain is not commonly available. By modifying the oxytocin molecule, its half-life has been prolonged and its enzymatic degradation reduced. The modified molecule is named carbetocin. Heat-stable carbetocin is a promising alternative to oxytocin, which can overcome the persistent problems with oxytocin quality as it does not require a cold chain for storage and transport.

Evaluating the CNS Activity of Methanolic Extract of Anogeissus latifolia Leaves on Various Experimental Rat Models

K. Hemamalini, K. Veeresh , M. Vijusha , N. Pruthvi Raju , A. Rajani

Novel Aspects on Pharmaceutical Research Vol. 2, 20 May 2023, Page 130-139

The purpose of this study was to evaluate the muscle coordination and anxiolytic properties of methanolic extracts of Anogeissus latifolia (combretaceae) in mice utilizing varied models of using mice. In the research, diazepam served as the standard medication. The extracts were given orally at two doses of 300 mg and 400 mg/kg. The current study's findings suggest that Anogeissus latifola leaf methanolic extract is efficient in causing a significant protection against muscle coordination and anxiolytic effects, as demonstrated by several CNS models compared to controls.  It is well known that the Methanolic extract of leaves of Anogeissus latifolia, which is proposed as its hypotensive principle. This investigation proved the plant's muscle coordination and anxiolytic properties as used in traditional medicine.

Development of Matrix Tablets by Extrusion/ Spheronization Process Using Laboratory Extruder

R. K. Mohamed Mutahar, Nagaraja Sreeharsha, Aqsa Farheen, Sanjay Kumar Gupta , Azmath Fatima

Novel Aspects on Pharmaceutical Research Vol. 2, 20 May 2023, Page 140-169

The primary goal of this study is to formulate and evaluate matrix tablets (MTs) of Nicotinic acid by extrusion/Spheronization process using extruder. Wherein, a detailed examination of the influence of the process factors has also been concentrated. Extrusion is a process of converting raw material into a product of uniform shape and density by forcing it through a die under controlled conditions. Extruded MTs were initially made directly from the extruder rod die and then again by compressing the extruded granules using mixed polymers during spheronization. These MTs were then compared to those made by compressing powders directly. These extruded MTs had a longer release pattern and were found to have superior physical qualities, features of drug solubility, and uniformity of drug content. As all formulations best fit into first order release kinetics and Higuchi's equation, the in vitro drug release data supports the diffusion-controlled nature of the release mechanism. The data were fitted into the Korsmeyer-Peppas model, which exposed abnormal transport kinetics, to confirm the results of the diffusion mechanism. The release rate result t20%, t50%, and t80%, of formulations tend to show similar to market product (MP) release rate. According to the model independent pair-wise approach 1 and 2 analysis, the MP profile and the dissolution profile of formulations can be superimposed. It was evident from the accelerated stability analyses of the improved formulations GEM.2 and TEM.2 that very little of the medication content deteriorated. At the end of six months, the release pattern was essentially unaltered and could be regarded as stable. Therefore, it can be said that extrusion/ Spheronization has higher potential as a process for creating MTs.