Editor(s)
Dr. Farzaneh Mohamadpour,
Department of Organic Chemistry, University of Sistan and Baluchestan, Iran.

ISBN 978-93-5547-693-7 (Print)
ISBN 978-93-5547-694-4 (eBook)
DOI: 10.9734/bpi/capr/v4

This book covers key areas of Pharmaceutical Research. The contributions by the authors include hemoglobin, iron deficiency, microcytic hypochromic anemia, High performance liquid chromatography, microemulsions, novel drug delivery, potential drug delivery, bioavailability, bioavailability, antibacterial activity, homeopathy, quantum mechanics, acetylcholine  receptor  antibody,  autoimmune  disease,  neuromuscular  junction, heart rate, autoimmune neuromuscular transmission, Covid-19 disease, vaccination, colon specific delivery, dosage forms, drug candidates, colonic micro-floras, conventional dissolution methods, gamma scientigraphy, animal studies, Colon specific targeting, approaches for colon delivery, novel and controlled formulations, therapeutic benefits, pH dependent system, colonic microfloras, colonic cancer, pharmaceutical excipients, autoimmunity, molecular mimicry, colorectal cancer, drug candidates, pH sensitive polymers, novel controlled system, psychmotor behavior, locomotor activity, Infectious diseases, silver nanoparticles, drug delivery system, mechanism of actions, biomedical applications, therapeutic efficacies, cytotoxicity, phytochemistry, pharmacodynamic concentration, morbidity. This book contains various materials suitable for students, researchers and academicians in the field of  Pharmaceutical Research.

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Chapters


The present study has been undertaken as the anemia is the most prevailing and commonly treated clinical state that is managed by numerous nutritional supplements without much being done to know the underlying etiology or without evaluation of hemoglobin for its abnormalities.

Clinicians encounter a morphological class of anaemia known as Microcytic hypochromic anaemia (MCHC), also known as low cell volume anaemia, in modern practice, which has a variety of underlying etiologies.

Iron deficiency anaemia, beta thalassemia trait, hemoglobinopathies caused by Hb E, Hb D, Hb C, and other factors are among the underlying causes. So, before beginning treatment, we must first screen haemoglobin for variations and aberrant hemoglobins.

Methods: This is an observational (Prospective and Retrospective) study carried out in Department of Pathology, JNMC, Sawangi (Meghe), Wardha. Blood samples of 100 patients will be evaluated by High performance liquid chromatography Bio-Rad variant to look for various patterns of hemoglobin involved and the hemoglobinopathies associated with it.

The observations will be made in accordance with the objectives and tallied before being subjected to statistical tests to determine their significance and conclusions.

The conclusion will be based on the findings for study of protocol

The Brief Insight on Microemulsions: A Proficient Tiny Carrier

Nirmal Shah, Dipti Gohil , Bhumika Rana

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 13-22
https://doi.org/10.9734/bpi/capr/v4/6681F

Pharmaceutical sciences play an exceptional role in improving quality of life all through the globe by providing proficient medications in concerned conditions. A suitable drug delivery is an essential element in achieving efficient therapeutic response of drug molecule. Conventional dosage forms are utilized since several decades but experiencing certain debilitating issues of low bioavailability due to poor absorption, dosing recurrence, dose dumping, plasma variance and so on. Consequently, developments of some novel pharmaceutical innovations are required to acquaint into the drug delivery for providing safety and efficacy of existing medications. Amongst all, microemulsion, composed of mixture of oil, water and surfactant, have emerged as promising drug delivery vehicles. This tiny carrier, because of its high surface area, can possibly modify fundamental properties and bioactivity of drug. Essential features, such as sheltering of encapsulated drug with expanded stability, better entrapment, improved pharmacokinetics and biodistribution, compatibleness with biological system, low toxicity, and some more traits, make them a choice of ultimate delivery system for the improvement in therapeutic benefit of drug molecules. Such uniqueness of microemulsion offers a fortunate intent to achieve maximum bioavailability with safe and successful drug delivery. This chapter boon an extensive overview of microemulsion with an emphasis on their types, manufacturing technologies, advanced research sand applications.

Enhanced Aqueous Solubility and Antibacterial Activity of Cefuroxime Axetil

Moushumi Tabassoom Salam , Ashim Kumar , Ranjan Kumar Barman

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 23-41
https://doi.org/10.9734/bpi/capr/v4/2643B

The objective of this investigation was to improve the solubility and consequent antibacterial activity of cefuroxime axetil (CA), a \(\beta\) -lactamase-stable broad spectrum second generation cephalosporin through solid dispersion (SD) technique. CA loaded SDs (CSDs) were made using a solvent evaporation process with various amounts of microcrystalline cellulose (MCC) as a carrier. The characterization of CSDs was done by in-vitro dissolution study, thermal analysis (DSC), crystallinity (PXRD), interactions (FTIR) and morphology (SEM). With a drug-carrier (CA: MCC) ratio of 1:3, CSD-2 had the highest solubility rate among the formulations, 2.59 fold stronger than pure CA. DSC, PXRD, FTIR, and SEM investigations confirmed that the increased dissolution rate was due to drug conversion from crystalline to amorphous form during SDs production. Antibacterial activity of CSD-2 against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 25922) showed 1.94- and 6.75-fold higher relative zone of inhibition (RZOI), respectively than pure CA. In terms of improved dissolving rate and antibacterial activity, CSD-2 has been proven to be the most effective optimized formulation. As a result, it could be a promising alternative to traditional CA dosage formulations. Before proposing it as a novel formulation, more research is needed to evaluate its pharmacokinetic features, in-vivo antibacterial activity, and safety.

Homeopathic Remedies as the Pharmacological Means of Informational Medicine

Mordeniz Cengiz

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 42-60
https://doi.org/10.9734/bpi/capr/v4/2970B

Homeopathy, a branch of alternate medicine, works on a holistic level because it focuses on readjusting false perceptions and healing negative energy signals and follows the rule of similar and uses potentiated substances called remedies carrying information. Although some empirical evidence exists, there is little academic research and lack of a theoretical model to explain their effects.

Homeopathy uses two instances of generalized entanglement: one between the remedy and the original substance (potentiation principle) and one between the individual symptoms of a patient and the general symptoms of a remedy picture (similarity principle). The remedy, itself is one entangled state and the homeopathic method is another entangled state between the symptomatology of the patient and the remedial substance. The homeopathic remedy is the substance which is not present but would become a kind of receptacle which ‘absorbs’ symptoms. The whole symptom picture is coherent.

Homeopathic treatment acts on the information level, but no physical explanation is given yet for the nature of the energy changes. Quantum mechanics seems to be a way to understand the success of homeopathic medicine in a physical context. To explain the therapeutic mode of homeopathic action, bio-molecular mechanisms, such as the memory of water and ‘non-local’ macro-entanglement, and patient- practitioner-remedy (PPR) interacting in terms of quantum matter-type fields. Since quantum properties can be physical without being observable, a similarity could exist between homeopathy and quantum theory which could be useful for modeling the homeopathic process. Homeopathic remedies can be considered as the pharmacological means of evidence for informational medicine.

Highlighting the Role of Acalypha indica Linn. Extract on Heart Rates with Myasthenia Gravis Rat Model

Desak Gede Budi Krisnamurti, Rani Wardani Hakim, Radiana Dhewayani Antarianto, Siti Farida , Erni Hernawati Purwaningsih, Jan Sudir Purba

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 61-71
https://doi.org/10.9734/bpi/capr/v4/1970B

The present study determine the effect of extract of roots AI against the AChR and enzyme acetylcholinesterase in animal models NMJ-MG (Sprague-Dawley rats were injected with rocuronium bromide) on the autonomic nervous system on heart muscle, in this case, is heart rate (HR). Myasthenia gravis (MG) is a neuromuscular junction (NMJ) autoimmune disease caused by antibodies that attack components of the postsynaptic membrane, impairing neuromuscular transmission and causing skeletal muscle weakness and tiredness. The autonomic nervous system uses acetylcholine as a neurotransmitter. Immune attack on striated cardiac muscle can result in heart failure, arrhythmia, and abrupt death. Involvement of the heart rate (HR) has been claimed and reported, but a causal connection between MG and altered cardiac function has not been found.

For this study of experimental autoimmune MG (EAMG) is used rocuronium, prostigmine, and Acalypha indica (AI) Linn. compared with HR.

From the results, the study found that sympathetic activity of HR variability in EAMG injected with rocuronium 10 mg/kg body weight (BW).

in 10 min significantly found increasing in measures of short-term variations in HR variability, indicating parasympathetic impairment.

We conclude that in MG, cholinergic transmission is affected more diffusely than previously thought. Furthermore, AI was given orally.

30 mg/kg BW has an effect similar to the injecting of prostigmine 10 mg/kg BW that can reduce HR. Driven by the fact that the pharmacological treatment of MG is unsatisfied, it needs the therapeutic development for MG using herbal ingredients of AI. The  result indicate  the  need  for  routine  evaluation  of  autonomic functions in   patients   with   MG   both   to identify   patients   at   high   risk  for earlier   consideration of cardioprotection and long-term   follow- up   studies.   Furthermore,   on   the   basis   of   these   results   using drugs rocuronium, prostigmine,   and   AI   are   associated   with   HR on   EAMG,  AI has the  same effect with prostigmine. To know and  learn  more  advanced study required.

Heterologous Prime-boost as COVID-19 Vaccine Strategies: Towards a Nationwide Implementation

Ibrahim M. S. Shnawa

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 72-83
https://doi.org/10.9734/bpi/capr/v4/16535D

Immune priming can be done in two ways: by immunization or through hyper-immunization. Priming mammalian animal models starts the main immune response, which leads to the development of effector cells. Boost stimulates immune cells, causing them to become memory immune cells participating in subsequent immune response events. Prime, homologous prime-boost, and/or heterologous prime-boost techniques are used in vaccination procedures. This theme can be used in mammalian laboratory animals as well as humans. Murine, lapin and primates immune system  functions are similar but not identical to that of human beings. So far, in terms of vaccine development and production. There may be differences in reactions and/or vaccination side effects when moving from a mammalian research animal to a human. The conventional and customary strategy in national and international immunization regimens for vaccine-preventable infectious illnesses for human welfare is homologous prime-boost. Heterologous prime boost techniques are becoming less popular among vaccine providers and the medical community. Day by day, current trials were undertaken all over the world to determine the efficacy of using heterologous prime-boost in mass immunization of covid-19. The present chapter was focused on to this validity. Workers reached one of three conclusions as; i- it reactivate immunogenicity, reacto-genicity and /or efficacy ii-Are of comparable efficacy and iii- Preference advise to apply it for mass vaccination of covid-19.International authority recommendation in this concern is still not in hand. Though, there were few published human volunteer trails for heterologous covid-19 vaccine strategies.

A Review on Colon Specific Drug Delivery Systems: Novel Approach in Pharmaceutical Perspective

Reena Kaushik, S. K. Lanjhiyana, Sanmati K. Jain, Sweety Lanjhiyana, A. C. Rana, Vipul Kumar

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 84-93
https://doi.org/10.9734/bpi/capr/v4/16539D

The objective of the current article is to study on colon specific delivery systems and those factors affecting for effective delivery of drug candidates into the targeted sites for desired pharmacological actions. Colon has proven to be a region where topical, local and systemic absorption of drug candidates can take place in an effective manner. It follows oral route that are preferred as per patient compliance factors along with reduced systemic side effects. This route is found preferred over the uncomfortable rectal route of drug administration, where having lesser patient compliances factors. Various factors affecting the colon delivery are Anatomy and physiology of colon, Colonic pH, colonic flora, GI transit time, fluid volumes, formulation factors etc. Colon specific delivery approach allows for targeting of drug(s) directly into the desired site of actions for management of diseases viz., colonic cancer, amebiosis, Crohn’s disease, ulcerative colitis, etc. Drug targeting using matrix or reservoir based delivery systems are possible into the colon directly due to reason that those delivery system are capable of protecting itself from assaults of acidic medium of stomach and alkaline medium of small intestinal of upper GI tract.

Recent Advancements of In-vitro and In-vivo Evaluation Strategies for Colonic Delivery Systems: An Overview

Reena Kaushik, S. K. Lanjhiyana, Sanmati K. Jain , Sweety Lanjhiyana, A. C. Rana

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 94-104
https://doi.org/10.9734/bpi/capr/v4/16545D

The objective of present current review article covers recent advancements explored for in-vitro and in-vivo evaluation strategies of colonic delivery systems and its potential pharmaceutical applications. Colon targeted drug delivery systems are designed in such a manner that by passes premature drug release into upper hostile bio-environment of gastro intestinal (GI) tract, while directly release of content on arrival into colonic region only. Hence this article highlight on those in-vitro and in-vivo evaluation strategies that utilize to confirms for resistance of delivery systems from assaults of upper bio-environment of GI tract viz., GI motility, pH changes from acidic to alkaline medium, fluid contents, gastro enzymatic activity etc. effectively. Those reported evaluation parameters help us to overcome the limitations of formulation and confirms for successful development of drug delivery devices for colon specific targeting. This review also focussed on utilization of few polysaccharides as an excipient materials for development of various colon-targeted formulations.

A Review on Designing and Formulation Approaches for Development of Novel Colon Specific Drug Delivery Systems

Reena Kaushik, S. K. Lanjhiyana, Sanmati K. Jain, Sweety Lanjhiyana, A. C. Rana

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 105-115
https://doi.org/10.9734/bpi/capr/v4/3199B

The objective of the recent review article is to study on factors governing for designing and formulation approaches for development of the potential colon specific drug delivery systems. Those factors were affecting the overall drug release pattern out from the delivery systems, drug absorption and bioavailability at the site of actions. It is also reviewed on role and affects of those inert polymers that were using in the form of matrix or reservoir into the formulations. Drug delivery systems using for colon targeting has potential for treatment of numerous diseases such as colonic cancer, ulcerative colitis, irritable bowel syndrome, Crohn’s disease, etc. During the last few decades, it has been established that the colonic region has potential for both local and systemic drug absorption efficiently as per reports of various researchers. These methodology based delivery systems were affected with one or more factors viz., gastrointestinal (GI) anatomy and physiology, pH differences, presence of microflora, transit time, fluid volume etc. of human body.  This present article highlights for few approaches that have been explored for dosage form development for colon targeting that contains drug candidate(s) utilizing for all possible therapeutic benefits.

Studies on Compatibilty of Rivaroxaban with Pharmaceutical Excipients Using DSC and FTIR Spectrophotometry

Rama Rao Nadendla, J. Satynarayana, Jaya Krishna Burri

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 116-134
https://doi.org/10.9734/bpi/capr/v4/3143B

Rivaroxaban (RN) is a powerful oral anticoagulant that was recently developed. It was the most commonly prescribed drug during COVID-19 pandemic situations. The goal of this study is to use a differential scanning calorimeter and an FTIR spectrophotometer to investigate the compatibility of rivaroxaban with crospovidone, sodium startch glycolate, magnesium stearate, talc, microcrystalline cellulose, aerosil, HPMC K100 M, and croscarmellose sodium. DSC thermograms, of rivaroxaban and physical mixture of individual pharmaceutical excipient, exhibited the range of transition of the drug in between 224ºC and 232ºC. The FTIR graphs revealed that the wave numbers of rivaroxaban corresponded to all of the selected pharmaceutical excipients. As a result of the DSC and FTIR examinations, it was determined that RN was not interacting with chosen pharmaceutical excipients and that it may be used in future research. The results of the present investigation concluded that these combinations are compatible and can be used for further studies, so as to develop pharmaceutical formulations with rivaroxaban.

Postinfection-post Vaccination Autoimmune Neural Long COVID-19: A Review

Ibrahim M. S. Shnawa

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 135-146
https://doi.org/10.9734/bpi/capr/v4/2858A

The normal physiological autoimmune condition might include auto-antibodies and auto-reactive immune cells in normal human subjects. On, post- sars-cov-2 infection and post-vaccination periods either the virus built in spike protein in case of post-infection. Or the peptide expressed from the spike protein sequence within the human COVID-19 mRNA vaccines have an auto-reacting epitopes within the human vaccinee cells. Both the virus spike protein and the vaccinee cells include either pan-sharing or mono-specific molecular mimicking epitopes that develop after repeated exposure to immune system cells causing autoimmune responses. The immune conversion state can lead to autoimmune tissue damage in the form of single or many organ abnormalities that express the patho-biologic characteristics of autoimmune long covid-19. The inclusion of long CoVID-19 on the list of autoimmune registry 2021 accords with this mechanistic interpretation of the long covid-19. Some workers feel that autoimmune long COVID-19 is a condition caused by autoantibodies. Other researchers believe that both auto-antibodies and auto-reacting immune cells are involved, while there is still some disagreement. This chapter presented a literature show case analysis of neural autoimmune long COVID-19 together with a suggestion to a laboratory animal model for Post-infection-Post-vaccination autoimmune long COVID-19 was suggested. Both of these disease entities are being over-lapping.

Modern Pharmaceutical Technologies for Drug Targeting: A Review on Colon Specific Drug Delivery Systems

Reena Kaushik, S. K. Lanjhiyana, Sanmati K. Jain , Sweety Lanjhiyana, A. C. Rana

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 147-156
https://doi.org/10.9734/bpi/capr/v4/16667D

The aim of present review is to highlights the significance of modern pharmaceutical approaches for drug targeting to colonic region for successful drug delivery at the desired site of actions. During last few decades globally an ample amount of research and development has been taken place into the field of colon drug targeting due to its potential pharmacological benefits. Colon delivery systems have proven itself as potential drug carriers for the treatment of numerous diseases, reduced side effects, prevents drug from assaults of acidic and alkaline medium of upper GI tract, reduce dose dumping etc. on other hand. The present article highlights for various strategies or technologies that have been explored for colon targeting viz., time dependent system, intestinal pressure-controlled colon delivery capsules, CODES™ technology, pH-dependent systems, enzyme-triggered systems, receptor-mediated systems, etc. for possible potential pharmaceutical therapeutic applications.

Investigating the Effect of Khat Habituation on Psychomotor Behavior in Mice

Hussein O. Al-Kadi, Shawqi H. Al-Awdi, Mohanad M. Shehab

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 157-164
https://doi.org/10.9734/bpi/capr/v4/3483E

The purpose of this study was to look into the effects of khat habituation on psychomotor behaviour in mice, as well as the effects of khat withdrawal on the reversal of khat habituation effects.

In this investigation, 18 adult mice weighing 20–30 g were employed. The animals were divided into three groups, one of which was used as a control. After overnight starvation, khat in a dose of 2 g/kg was given with food to promote khat-habituation. After one week, the tested animals were given access to both khat-containing and non-khat-containing items, with the majority of the animals favouring the khat-containing foods. The animals which preferred khat-containing food were regarded as showing khat-habituation and   were continued to feed khat-containing food in a dose of 2g/kg/day for two months to develop chronic khat habituation, animals which had not preferred khat- containing food were excluded from the study and were regarded as resistant to khat  habituation.  Animals were given food for 14 days without any khat to induce khat-withdrawal. To evaluate the impact of khat habituation on locomotor activity and the impact of khat withdrawal on the reversal of khat effects, the locomotor activities of animals were observed and graded in accordance with the behaviour scale. Animals that had become khat-habituated exhibited a considerable rise in stereotypical psychomotor behaviour, which peaked 15 to 30 minutes after khat use. Following a 14-day khat withdrawal, mice's psychomotor behaviour returned to normal. Chronic khat habituation significantly increases mice's psychomotor behaviour, however this effect is only temporary and can be reversed if the habit is broken.

Silver Nanoparticles as Drug Delivery System in Combating Infections and Cancer

Ardhendu Kumar Mandal

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 165-179
https://doi.org/10.9734/bpi/capr/v4/16408D

Chemotherapy remains a serious difficulty for delivering medications to precise sites of interest against numerous life-threatening infectious diseases, despite advances in medical and pharmaceutical sciences. The majority of medications have a significant toxicity, which causes a variety of side effects and lowers quality of life. Inadequate therapeutic index, limited drug absorption, the development of multiple drug resistance, and undesirable systemic side effects have all been linked to the use of conventional microbicidal agents to treat infections. Due to their ultra small controlled sizes, high surface area, and improved reactivity with active functional structures, antimicrobial silver nanoparticles (AgNPs) have emerged as a potent and efficient agent against infection. AgNPs, after exposure, adhere to cells, penetrate inside the cells, and generate reactive oxygen species (ROS) producing oxidative stress, protein dysfunction, and modification of signal transduction pathways, and damage membranes and deoxyribonucleic acids (DNAs), leading to cellular damages.  The surface-ligand coating of AgNPs-incorporated drug as drug delivery vehicle enlightens their sustained drug release with reduced side effects when administered into the body. This review focuses mainly the synthesis, surface-functionalization, mechanism of actions, biomedical applications, therapeutic efficacies, toxicity, biodistribution and elimination of the AgNPs as potential nanomedicinal drug delivery system for targeted therapy against infections and cancer.

The Potency and Efficacy of Essential Oils from Selected Aromatic Crop Species Commercially Grown in Uganda: A Review of their Use in Animal and Human Therapeutics

Patience Tugume, Maud Kamatenesi-Mugisha, George Byarugaba Bazirake, Waisindye Noah, Savina Asiimwe

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 180-204
https://doi.org/10.9734/bpi/capr/v4/2445A

There is increased use of essential oils from aromatic crops in the beverage pharmaceuticals, apiary and cosmetics industries in addition to aromatherapy due to production of active compounds. Essential oils have been proven to have bactericidal, virucidal, fungicidal, anti-parasitic and insecticidal effects. The aim of this review was to provide an overview of efficacy and potency of essential oils from selected aromatic crop species commercially produced in Uganda. We reviewed relevant articles, books, theses, dissertations, patents, and other English only reports using potency, traditional medicinal uses, pharmacological or biological activity, toxicity, phytochemistry, and efficacy of Cymbopogon citratus, Salvia rosmarinus, Eucalyptus citriodora and Lavandula anguistifolia as the key search terms. We searched databases such as PubMed, Web of Science, Scopus, Science Direct and search engines such as Google Scholar between June and November 2021. The essential oils were reported to have antibacterial, antifungal, anticancer, anthelmintic, insecticidal, larvicidal, acaricidal and antioxidant effects. Additionally, rosemary oil inhibited aflatoxin growth and secretion, stimulated the nervous system and stabilized mayonnaise during storage. The biological activities exhibited by essential oils in this review validate their current and potential use in the pharmaceutical, cosmetic and food industries. 

Therational Design of Precision Drugs

Karel Petrak

Challenges and Advances in Pharmaceutical Research Vol. 4, 30 June 2022, Page 205-218
https://doi.org/10.9734/bpi/capr/v4/6762F

Perfect precision medications must be rationally designed by accurately characterising the disease's molecular target. This article discusses how the present medication development process should adapt in order to meet this demand. The article uses examples from previous drug development to show what needs to be done to get to the next step, which is the development of precision drugs-drugs that target diseases with no, or very few, adverse effects. To this goal, distinctive molecular structures linked to diseases must be identified, followed by the development of medications that bind to these structures specifically. Finally, this new paradigm must be adopted in future drug development.