Editor(s)
Dr. Rafik Karaman
Professor,
Bioorganic Chemistry College of Pharmacy, Al-Quds University, Jerusalem Palestine.

 

ISBN 978-93-5547-352-3 (Print)
ISBN 978-93-5547-356-1 (eBook)
DOI: 10.9734/bpi/capr/v1

 

This book covers key areas of  Pharmaceutical Research. The contributions by the authors include emulsifier, surface tension, hydrophilic and lipophilic properties, multivariate calibration technique, pharmaceutical formulation, anti-quorum sensing, antibacterial activity, prodrug approach, azo prodrugs, anti-cancer drug, colon directed drug transport, Ramos-1 cells, lymphoma, high performance liquid chromatographic method, Cardiovascular diseases, lipid profile, fish consumption, atherogenic indices, : bioavailability, micronization, microorganisms, phlobatannin, cardiac glycosides, pharmaceutical and pharmacological formulations. This book contains various materials suitable for students, researchers and academicians in the field of  Pharmaceutical Research.

 

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Chapters


Surfactants: Role in Pharmaceutical Formulation

Amiyakanta Mishra, Biswaranjan Ray

Challenges and Advances in Pharmaceutical Research Vol. 1, 14 March 2022, Page 1-8
https://doi.org/10.9734/bpi/capr/v1/1942A

Surfactants are compounds that lower the Surface tension of a liquid, allowing easier spreading, and lowering the Interfacial tension between two liquids or between a liquid and Solid. Surfactants are amphiphilic in nature. Possessing both hydrophilic and lipophilic properties. Surfactants act as foaming agents, Emulsifiers and dispersants for Suspending Immiscible liquids or Solids, respectively, in water or Some other Liquid. The present review deal with suitable surfactants in different pharmaceutical doses form with their merits and demerits. The article also highlights Compatibility of Surfactants in different formulation with application of the Surfactants.

Objective: The current abstract employs a multivariate calibration technique to quantify ivermectin in pharmaceutical dosage form.

Methods: The multivariate calibration technique relies on linear regression equations to correlate the relationship between concentration and absorbance at seven different wavelengths.  The \(\lambda_{max}\) of ivermectin was found to be 254 nm. The findings were statistically analysed. This statistical approach yields the best results by eliminating fluctuations caused by instrumental or experimental conditions.

Results: The developed method was validated in accordance with ICH guidelines and was found to be simple, linear, accurate, precise, and reproducible. The method was found to be linear over a concentration range of \(5-15 \mu\\g/mL\) with a correlation coefficient \((r^2)\) value of about 0.9998. The limit of detection and quantification were found to be 0.029 and \(0.087 \mu\\g/mL\), respectively. Intraday and interday precision were found to have percentage relative standard deviations of 0.473-1.373 and 0.301-1.617, respectively. The percentage recovery was found within the range of \(97.60-101.80\%w/w\).

Conclusion: The findings show that a simple, linear, precise, accurate, sensitive, and reproducible multivariate calibration technique for the quantification of ivermectin in bulk and pharmaceutical formulation has been devised and validated.

Antiquorum-Sensing and Antibacterial Activity of Green Synthesized Silver Nanoparticles against Methicillin-Resistant Staphylococcus aureus (MRSA)

M. Arunkumar, M. Safana Farjeen, S. K. Divya, T. Jeyadoss

Challenges and Advances in Pharmaceutical Research Vol. 1, 14 March 2022, Page 24-33
https://doi.org/10.9734/bpi/capr/v1/2776C

The development of efficient methods for the green synthesis of silver nanoparticles using plant extracts has emerged as a major area of focus in nanotechnology. Bactericidal nanomaterials are becoming increasingly important as bacteria develop resistance to even the most potent antibiotics. The discovery of a bacterial communication system (Quorum-sensing system), which orchestrates important temporal events during the infection process, has provided a novel opportunity to treat bacterial infection by means other than growth inhibition. This has promoted research in the well-known bactericidal activity of Ag+ ions and Ag-based compounds, including silver nanoparticles (AgNPs). In the present study, the extracellular biosynthesis of silver nanoparticles was carried out using aqueous extracts of nine different herbal plant leaves for the reduction of aqueous silver ions. Among the nine selected medicinal plants, the leaf extracts of Aerva lanata showed rapid reduction (2 min) of silver ions in the solution. Transmission electron microscopy, UV-visible spectroscopy, and X-ray diffraction were used to examine the nanoparticles' morphology and structures. SEM and X-ray diffraction (XRD) analysis revealed the nanocrystalline phase of silver with average particle sizes ranging from 37 to 47 nm and found to be spherical. Moreover, the synthesized AgNPs demonstrated potent antibacterial activity against Methicillin Resistant Staphylococcus aureus (MRSA). Furthermore, the stable silver nanoparticles inhibited violacein production, which is a quorum-sensing regulated behaviour in Chromobacterium violaceum CV026.

Colon Directed Drug Transport by Way of AZO Prodrugs

Sanmati K. Jain, Sanjay K. Lanjhiyana, Bharti Ahirwar, Ajay Gupta, B. G. V. S. Jagan, Ioannis S. Vourdoubas

Challenges and Advances in Pharmaceutical Research Vol. 1, 14 March 2022, Page 34-48
https://doi.org/10.9734/bpi/capr/v1/15696D

Transport of drugs by oral route to colon becomes important in the treatment of colonic diseases like inflammatory bowel disease, ulcerative colitis, Chron’s disease, chronic pancreatic and colonic carcinomas. Metabolic reactions like hydrolysis, redox, deamination etc. and several biological features affecting oral drug delivery include the time spent in gastrointestinal tract (GIT), GI environment, microbial flora and enzymatic degradation and cumulatively all of which are obstructing drug delivery. Prodrug approach is one of the invaluable techniques for transportation of drugs by oral route to colon. In the present work azo prodrugs of 5-Amino Salicylic Acid (5-ASA), 4-ASA, anticancer drugs and newer leads useful in colonic diseases has been reviewed for the colon directed drug transport due to the selective cleavage of the azo bond by azoreductases discharged by the gut microflora.

Determination of Phytochemical Profile and Anti-Oxidation Activity of Annona Fruit and its Effect on Lymphoma Cell Proliferation

Huda Mohammed Al-Shaya, Haiwen Li, Obaid U. Beg, Anwar A. Hamama, Sarah Melissa Witiak, Paul Kaseloo, Rafat A. Siddiqui

Challenges and Advances in Pharmaceutical Research Vol. 1, 14 March 2022, Page 49-65
https://doi.org/10.9734/bpi/capr/v1/15604D

High intake of certain vegetables and fruits is associated with a reduced risk of cancer development. We hypothesized that Annona fruit, which is rich in fibers and phytochemicals that are known to possess anti-cancer properties, can be effective in inhibiting lymphoma growth. The objective of this study was to extract the anticancer activity with a suitable solvent and determine their phenolic content and antioxidation activity. The Annona fruit’s fractions were extracted with water, methanol or chloroform solvents. Each fraction was then assayed for total phenolic, flavonoids, and tannin content, anti-oxidation activities, and inhibition of in vitro cell proliferation using the Ramos-1 lymphoma cells. The methanol fractions contained the highest phenolics, flavonoids, tannins content, and anti-oxidation activity. Although the methanol extracts of skin, pulp, and seeds had a moderate effect, the chloroform extracts of pulp and seeds had strong effects on Ramos-1 cell proliferation. Our findings suggest that Annona fruits may be effective in the prevention or treatment of lymphoma.

Assessment of Related Substances in Pioglitazone Hydrochloride by HPLC Method

N. Balaji, Sayeeda Sultana

Challenges and Advances in Pharmaceutical Research Vol. 1, 14 March 2022, Page 66-80
https://doi.org/10.9734/bpi/capr/v1/2684C

Objective: An efficient, high performance liquid chromatographic method has been developed and validated for the quantification of related substances in pioglitazone hydrochloride drug substance.

Methods: This method includes the determination of three related substances in pioglitazone hydrochloride. The mobile phase A is 0.1% w/v triethylamine in water with pH 2.5 adjusted by dilute phosphoric acid. The mobile phase B is premixed and degassed mixtures of acetonitrile and methanol. The flow rate was 1 ml/min. The elution used was gradient mode. The HPLC column used for the analysis was symmetry C18 with a length of 250 mm, internal diameter of 4.6 mm and particle size of 5.0 microns.

Results: The developed method was found to be linear with the range of 0.006-250% with a coefficient of correlation 0.99. The precision study revealed that the percentage relative standard deviation was within the acceptable limit. The limit of detection and limit of quantitation of the impurities was less than 0.002%and 0.006% with respect to pioglitazone hydrochloride test concentration of 2000 µg/ml respectively. This method has been validated as per ICH guidelines Q2 (R1). The specificity, solution stability and robustness of the method show that the impurity PGR-II and PIO-II were process related impurities and N-oxide was degradation impurity. This indicates that the equipment was suitable, accurate, precise, sensitive and fit for study.

Conclusion: A reliable, economical HPLC method was magnificently established for quantitative analysis of related substances of pioglitazone hydrochloride drug substance.

Determination of Lipid Profile and Atherogenic Indices for Cardiovascular Disease Risk Based on Different Fish Consumption Habits

Chandravathani Devadawson, Chamila Jayasinghe, Sivakanesan Ramiah, Arulnithy Kanagasingam

Challenges and Advances in Pharmaceutical Research Vol. 1, 14 March 2022, Page 81-89
https://doi.org/10.9734/bpi/capr/v1/15611D

Objective: Habitual consumption of moderate amounts of fish is associated with reduced mortality from cardiovascular disease (CVD). However, the beneficial effects of fish-enriched diet seem contradictory due to the oxidation susceptibility of the polyunsaturated fatty acids in them. The atherogenic index is an important tool to identify people with CVD risk. Lipid profile levels are favorably affected by certain fish consumption habits, thereby decreasing the risk of coronary heart diseases. The aim of this study was to evaluate the plasma lipid profile of healthy people with different fish consumption habits and to assess CVD risk using atherogenic indices.

Methods: Fasting blood samples were collected from healthy people for lipid profile estimations with an automated analyzer. Detailed information regarding physical and atherogenic parameters was collected from each participant.

Results: The CVD risk profiles showed varying level with the type of fish consumption. Total cholesterol, triglyceride (TG), and non-high-density lipoprotein (Non-HDL-C) varied significantly among the types of consumers (p<0.05), whereas the high-density lipoprotein cholesterol showed variation (p<0.001). TG/HDL showed the greater level in inland fish consumers. However, atherogenic coefficient and Castelli risk index-2 did not show significant variation among type of fish eating. Atherogenic indices were borderline “high risk” among all fish eaters including beef eating habits.

Conclusion: Fish and beef eaters had high risk among other inland and sea fish eaters. Non-HDL-cholesterol could be a marker for a serum lipid pattern associated with increased risk of heart diseases. All fish including beef eaters had a non- HDL-C level that was borderline high risk for CVD. TC and lipid-protein fractions had age- and sex-related differences. Women had higher TC and LDL-C levels than men. The values of non-HDL-C and TG/HDL-C can be used as improved diagnostic factors for CVD risk.

Bioavailability is the rate and extent (amount) of absorption of an unchanged drug from its dosage form. This is considered as a primary parameter for a drug to show maximum pharmacological response. The poor aqueous-soluble drug can exhibit poor dissolution rates and incomplete absorption resulting in poor bioavailability. The dissolution and solubility parameters of the drug are very important in developing formulation. So, different methods are employed to improve the drugs solubility such as pH adjustment, micronization, solid dispersion, Supercritical fluid recrystallization, complexation, use of surfactants, co-solvency, Precipitation and nanotechnology etc. The main objective of this study is to give an overview of methods to enhance solubility, dissolution, and bioavailability of low aqueous soluble drugs and the importance of Green chemistry in nanotechnology to produce various nanosized formulations.

Imparting Yashtimadhu Antimicrobial Coating on Organic Cotton Fabric for Skincare Protective Applications

V. Krishnaveni, G. Rajkumar

Challenges and Advances in Pharmaceutical Research Vol. 1, 14 March 2022, Page 139-145
https://doi.org/10.9734/bpi/capr/v1/15712D

Protective textiles are one of the hastily increasing sectors within the technical fabric market. In the current years, comfort has grown to be obligatory in skin-care- protective textiles. Textiles with antimicrobial finishes are provided give comfort to humans. The herb yashtimadhu is used to improve the antimicrobial coated material and the impact of the end result. The herb is extracted using a direct extraction method with ethanol as the chosen solvent. Other solvents such as methanol, ethanol, chloroform, acetone, and distilled water are used primarily based entirely on distinct polarity stages and are applied directly to the cotton material via a pad-dry-remedy method in an optimised manner situation. The optimized parameters are Temperature-35oC, Time-3hrs, pH-6 and Concentration-25%. The coated and uncoated samples are examined in popular antimicrobial exams particularly AATCC 100, AATCC 147, AATCC 30 Agar Diffusion and Broth Dilution exams against disease causing micro-organisms. The major objective of the study is very much suitable for curing the skin care protective applications against various skin irritations, rashes and eczema.

Determination of Antibacterial Evaluation, Phytochemical Screening and Ascorbic Acid Assay of Turmeric (Curcuma longa)

Michael Oghenejobo, O. A. Opajobi, U. S. Oghenejobo Bethel, U. E. Uzuegbu

Challenges and Advances in Pharmaceutical Research Vol. 1, 14 March 2022, Page 146-161
https://doi.org/10.9734/bpi/capr/v1/15376D

Using the agar well diffusion method, the microbial susceptibility of an ethanolic extract of Turmeric (Curcuma longa) was tested. The extract was found to be active against the bacteria used as it inhibited all the organisms with the highest inhibition zone of 13.7mm recorded against Shigella flexnerri and the least inhibition of 2.3mm recorded against Staphylococcus epidermis. Minimum Inhibitory Concentration (MIC) values range from 6.25mg/ml to 200mg/ml. Shigella flexnerri gave MIC of 6.25mg/ml, S. aureus and K. Pneumonia, 25mg/ml, E. coli, 50mg/ml, S. epidermis, Lactobacillus and P. aeruginosa, 100mg/ml and V. cholera and S. typhi 200mg/ml respectively. Secondary metabolites were also screened using phytochemistry. Fourteen (14) secondary metabolites were screened from the ethanolic extract. The presence of these phytochemicals like tannins, alkaloids, phenols, steroids, flavonoids, phlobatannin, cardiac glycosides, terpenoids, triterpenes, saponin, etc; is indicative of the antimicrobial activity of Turmeric. The extract was found to contain 66.749mg/100ml ascorbic acid which is relatively comparable to many fruits recommended by dieticians. The value of curcumin present (Rf value 0.436) is also relatively close to that of pure curcumin. The results so far obtained are indicative of the good medicinal value of Turmeric in both pharmaceutical and pharmacological formulations. It is recommended therefore that further research should be done on it for its use as a plant medicinal especially in this period that herbal drugs are becoming significant as antimicrobials.