Volume 18, Issue 2, Summer and Autumn 2021, Page 1-220

Evaluation of cytogenetic damage induced by antihypertensive drug Amlodipine: in vitro

Sayran K. Salih; Rawaa M. Abdo; Dian J. Salih; Asaad A. Alasady

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 1-9
DOI: 10.33899/iphr.2022.170390

Background: Amlodipine is a calcium channel blocker medication used to treat high blood pressure and coronary artery diseases for long term of use. Sufficient studies reporting the cytogenetic effects of this drug have not reporting yet.
Aim of study: This study aimed to assess the frequency of chromosomal aberrations of amlodipine on human blood lymphocytes in vitro.
Material and Methods: In this study, the in vitro genotoxic effects of amlodipine have been determined in human peripheral blood lymphocytes by using chromosomal aberrations: 0; 5; 10; 15; 25 and 50mg/mL concentrations of amlodipine was used. All samples cultured in 37°C incubation for 72 hours. Then treated with Colcemid.
Results: Amlodipine did not appear to have cytogenetic effects in vitro, as no significant increases in the frequency of chromosomal aberrations were found in cultures treated with different concentrations compared to cultures treated with the recommended concentration (10 mg/mL). The highest concentrations (50 mg/mL) of amlodipine increased chromosomal aberrations compared to negative control, but these increases were not statistically significant
Conclusion: Amlodipine is not seemed to be genotoxic active ingredients in human lymphocytes in vitro.

Antibacterial activities of plant extract Cinnamomum zeylanicum bark against multidrug-resistant bacteria

Nishteman F. Mohammad; Shilan S. Saleem; Rand B. Balata; Dian J. Salih

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 10-21
DOI: 10.33899/iphr.2022.170393

Background : Due to the increased occurrence of bacterial resistance to multiple antimicrobial drugs, there is a constant search for novel therapeutic strategies; medicinal plants represent an important source for obtaining such substances. The antimicrobial activity of extracts and essential oils of medicinal plants has been proven in several studies conducted in countries with diverse flora.
Aim : To evaluate the antibacterial activity of cinnamon against multidrug- resistant bacteria.
Material and Method: Bacterial susceptibility testing was conducted by the diffusion method on Mueller-Hinton agar using paper discs impregnated with test substances.
Results: All test strains were sensitive to the essential oil of cinnamon. We observed low synergistic potential between essential oils against the strain of S. aureus.
Conclusion: The essential oil of cinnamon has antibacterial activity against both Gram-positive and Gram-negative strains. Future research should be conducted to define the best concentration and better extraction solution for mastic and cinnamon peels.

Formulation and Evaluation of Rosuvastatin Calcium Polymeric Nanoparticles-Loaded Transdermal Patch

Mais S. Saadallah; Omar A. Hamid

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 22-38
DOI: 10.33899/iphr.2022.170395

Background: Transdermal drug delivery systems (TDDS) have been rapidly developed as a promising alternative to the oral delivery systems to provide controlled drug delivery and avoid the first-pass metabolism of drugs. Recently, various nanocarriers such as liposome and lipid nanoparticles have been used to enhance dermal and transdermal penetration of drugs. The aim of this study is to formulate and evaluate a polymeric nanoparticle (PNPs)-loaded transdermal patch of the antihyperlipidemic drug rosuvastatin.
Materials and Methods: Rosuvastatin PNPs were prepared by nanoprecipitation method, and evaluated for particle size, zeta-potential and polydispersity index. PNPs-loaded patch and PNPs-free patch (control) of rosuvastatin were prepared by solvent casting method using hydroxyl polymethyl cellulose K15 (HPMC K 15) as film-forming polymer and polyethylene glycol 200 (PEG 200) as a plasticizer and evaluated for physical appearance, thickness, folding endurance, surface pH, in-vitro release and ex-vivo permeability.
Results: The particle size, zeta-potential, and polydispersity index of rosuvastatin-loaded PNPs were 68.69 nm, - 7.5 mV, and 0.294, respectively. The prepared transdermal films showed acceptable appearance, thickness, and folding endurance as well as surface pH values. In vitro release study showed 65% and 82% cumulative release after 24 hrs for the polymeric nanoparticle-loaded patch and control patch, respectively. However. ex vivo permeation results showed that a significantly higher amount of rosuvastatin permeated via rat skin from the PNPs-loaded patch in comparison to the control patch (P-value ˂ 0.05).
Conclusion: Rosuvastatin PNPs-loaded transdermal patch was successfully prepared and revealed promising releasing and permeation properties comparing to control patch.

Preparation and Evaluation of Topical Gel Containing Aloe Vera Exudate

Amina M. Al-Nima

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 39-52
DOI: 10.33899/iphr.2022.170396

Background:Aloe vera is known as a miracle plant belonging to the Lily (Liliaceae) family, The exudate of Aloe vera is utilized as a natural drug as it can be used for many medicinal purposes.
Aims: The present work has been undertaken with the aim to prepare a topical gel containing Aloe vera exudate and to evaluate its physical properties in addition to its anti-microbialpotency in light of the orientation towards plant-based treatment for being more acceptable and preferred in the belief that they are safer with fewer side effects than synthetic ones. Aloe vera has been proved its great medicinal and cosmetic benefits.
Materials and Methods: Two sets of gel formulas were prepared; the first set containing carbopol-934 (F1-F4) and the second set containing carboxymethylcellulose (F5-F10) with varied concentrations to achieve the best formula that has been selected according to various physicochemical evaluations; like homogeneity, transparency, appearance, consistency, color, odor, pH, phase separation and others. The selected formula was further subjected to in vitro study for its anti-microbial activity.
Results and Discussion: There was a significant difference (p≤0.05) in physical parameters between the two sets of formulas except in pH. Results showed that (F2) containing 1.5% m/v carbopol-934 is considered the promising formula which showed better physicochemical properties and exhibited good anti-microbial activity against both (E.coli) and (Staphylococcus aureus).
Conclusion and recommendations: The selected formula (F2) of Aloe vera exudate could be considered as a suitable medicinal herbal candidate for treatment of topical bacterial infections. In addition, it is recommended to use higher concentration of antioxidants to preserve the stability of the product, also it is recommended to add water soluble fragrance (perfume) for better odor.

Minoxidil in androgenic alopecia: New formulations with Improved delivery

Alaa Al-taie; Myasar M. Al-kotaji; Hani M. Almukhtar

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 53-63
DOI: 10.33899/iphr.2022.170397

Background: Minoxidil was introduced into the market as a hypotensive agent, however, aftermarketing, the hypertrichosis side effect was reported by almost all users. This adverse effect encourages the repositioning or repurposing the use of minoxidil as a topical preparation for the treatment of hair loss.
Objective: topical minoxidil is contemplated as an effective treatment to reduce hair loss and promote regrowth in conditions like androgenetic alopecia. However, the unerring mode of action of minoxidil remains obscure. In this review, the molecular pharmacology of minoxidil, the response of hair follicles to treatment, and the side effects of the topically applied minoxidil were reviewed. The innovation in the formulation of topical preparation toward enhancing delivery was highlighted focusing on the use of nanoemulsion and nanocarrier systems such as nanoparticles and liposomes that enriched the topical delivery.

Transdermal patch of acetylsalicylic acid as an alternative dosage form: A review

Hayder F. Alhamdany; Mohanad A. Alfahad

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 64-72
DOI: 10.33899/iphr.2022.170398

As a substitute for traditional systemic administration, many topical treatments have lately evolved. Transdermal drug delivery systems (TDDSs) are the most appealing of these methods due to their low rate of failure, simplicity of distribution, superior efficiency and preference amongst users. TDDS has the potential to be useful not just in medicines, but also in the skincare sector, particularly cosmetics. Since this approach means the development of local administration, it can minimize local drug level accumulation and inappropriate drug distribution to regions not primarily tailored by the medication. Aspirin (acetylsalicylic acid) is becoming the preferred choice against which subsequent antiplatelet medicines are measured in terms of lowering the cardiovascular risk while remaining inexpensive. Along with its substantial presystemic metabolism, orally administered acetylsalicylic acid has the potential of gastrointestinal negative impacts albeit at modest dosages and necessitates regular administration. Transdermal administration avoids the gut and would be more practical and healthier for aspirin usage, particularly during repeated doses. The present review highlights general aspects of aspirin primed as a TDDS as an appropriate topical preparation.

Effect of polyphenol secondary metabolites on oxidative stress and inflammatory responses associated with aging diseases

Khadeeja Y. Abid; Maimonah Yahya; Adnan A. Zainal

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 73-83
DOI: 10.33899/iphr.2022.170399

Several mechanisms are responsible for regulating the process of aging. A rise in reactive oxygen species (ROS) and oxidative stress is usually linked to the development of age-related diseases. Evidence indicates that prolonged oxidative stress can predispose to frequent diseases such as chronic inflammation, cancer and heart diseases. Polyphenols are naturally occurring substances found in numerous fruits, vegetables, cereals, etc. They considered as one of the most abundant and widely distributed secondary metabolites of the plant kingdom. Long-term consumption of polyphenol-rich diets was confirmed for protection from as shown by earlier. Additionally, polyphenol-rich foods and beverages offer protection against certain chronic diseases, particularly type 2 diabetes and heart disease. Certain polyphenols, such as quercetin, have anti-inflammatory properties and they were also associated with lower levels of biomarkers of muscle injury and inflammation. Flavonoids were shown to slow memory problems and the progression of Alzheimer’s disease. Antioxidants such as plant polyphenols have been proposed for cancer prevention and/or treatment. Dietary benefits are attributed in part to polyphenols, which have antitumor properties in both animal models and humans. Resveratrol (RV), a polyphenol found in blueberries, cranberries, wine almonds, and red grapes, has anti-inflammatory and anti-cancer properties and was shown to reduce cancer cell glycolytic metabolism and reduce intracellular ROS levels.

Bacteriophage as a Promising Alternative or Complementary Therapy to Antibiotics

Zahraa A. Hashim; Farah H. Omer

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 84-96
DOI: 10.33899/iphr.2022.170408

The global issue of antibiotic resistance and the narrowing down of new antibiotic discoveries besides their cost has led to the reintroduction of bacteriophage as a focus of research projects. Phage therapy is mainly grounded on the discriminating ability of the bacteriophage to destroy the targeted bacterial cells, but not human cells, via lytic phages. Although there has been a number of life-sparing clinical trials and applications, this therapy is still facing challenging issues. This review gives an overview of the microbiology and history of the bacteriophages. It also reviews the past and current studies of phage therapy in humans and it’s commercial production. The aim of this study is to shed the light on the rapidly growing field of phage therapy and the obstacles that appear ahead as antimicrobial science moves away from broad dependence on conventional antibiotics.

Drug Physicochemical Properties Relevant to Powder Flowability in Pharmaceutical Appliance: A Review

Liqaa S. Esmail

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 97-103
DOI: 10.33899/iphr.2022.170401

Background: Studies have shown that the powder flowability rate significantly impacts the content uniformity and weight of the active pharmaceutical ingredients in drug tableting procedures.
The aim was studying the physicochemical properties relevant to the powder flowability in some pharmaceutical instruments.
Powders with good flow characteristics are required to ensure a continuous flow through the die and other compartments of the pharmaceutical appliances used for manufacturing. Several factors, such as size, density, adhesiveness, shape, surface conditions, and electrostatic chargeability of the drug ingredients, tend to influence the flowability of a drug.
Conclusion: The study highlights that particle size is one of the major determinants of powder flowability. Large particles are expected to aid better flowability resulting in a clearer feeder during the manufacturing process. The flowability of the powder could be improved by adding a small number of fine particles and granules as excipients.

A review on coumarin backbone: An attractive scaffold for promising bioactive compounds

Sara F. Jasim; Yasser F. Mustafa

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 104-125
DOI: 10.33899/iphr.2022.170402

Background: Coumarin moiety is found in many naturally occurring products that have been used for many decades in traditional medicine around the world. Coumarin has distinctive physicochemical properties and can be easily transformed into a wide range of functionalized coumarins. As a result, a large number of coumarin derivatives have been designed, synthesized, and evaluated to attack a variety of pharmacological targets selectively. These targets may include various selective enzyme inhibitors and the targets, tagged as multitarget-directed ligands, found in diseases like Parkinson's and Alzheimer's, which are considered as multifactorial diseases.
Objectives: The most widely used synthetic methods leading to coumarins, besides the major biological routes for their metabolic transformations and biosynthesis, are highlighted and reviewed. Also, the focus was concentrated on some pharmacological activities of coumarin derivatives involving those related to the selective inhibition of cholinesterase and monoamine oxidase enzymes and targeting specific ligands of neurodegenerative diseases.
Conclusion: The impacts of substituents pattern/type on the selectivity and potency of the studied coumarins were explained to determine the main structural and molecular factors that may affect the activity and performance of the directed targets.

Synthesis of coumarin-based derivatives from different starting materials: A review of ongoing developments

Sarah A. Waheed; Yasser F. Mustafa

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 126-138
DOI: 10.33899/iphr.2022.170403

Objective: This brief review highlights the recent advances in the synthesis of coumarin-based derivatives from phenols, aldehydes, ketones, and various other functional group-containing starting compounds. Also, the recent developments in the conditions of several original synthetic methods involving Pechmann and Knoevenagel reactions are being revised.
Conclusion: It is critical to decreasing energy consumption, prevent hazardous chemicals, and get pure molecules in high yields during synthesis. Scientists working in this sector will be able to utilize this comparison of reaction conditions and compound yields to create new efficient procedures.

Natural Coumarin-Lead Compounds: A Review of Their Medicinal Potentials

Rahma M. Jebir; Yasser F. Mustafa

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 139-161
DOI: 10.33899/iphr.2022.170404

Background: Natural coumarins group, a principal member of the benzopyrone family, is one of the naturally occurring substances obtained ordinarily from plant origins, with antibacterial, anticoagulant, antihypertensive, anticancer, antioxidant, anti-inflammatory, and many other medicinal potentials. Because coumarins are found in nuts, seeds, fruits, vegetables, tea, coffee, and wine, the average person consumes a significant amount of these substances daily. Given the documented limited toxicity, relatively cheap, availability in foods, and prevalence of coumarins in numerous herbal medicines, it seems reasonable to investigate their characteristics and usage.
Objective: This review discusses naturally occurring coumarin lead substances, their extensive medicinal benefits, and official pharmacopoeia-based detection methods.
Conclusion: The medicinal potential and therapeutic uses of simple coumarins are determined by their structural substitution pattern. Because there is limited research on bioavailability for coumarins, additional research is needed to investigate the bioavailability for various coumarins, which have demonstrated good bioactivity in prior research.

Coumarin-based products: Their biodiversity and pharmacology

Reem N. Ismael; Yasser F. Mustafa; Harith K. Al-Qazaz

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 162-179
DOI: 10.33899/iphr.2022.170405

Background: The plant kingdom generates and releases a wide range of secondary-metabolites, which have several effects on biological, toxicological, and ecological systems that may act in a similar manner to chemically synthesized compounds. One of these secondary-metabolites are coumarins, which are obtained from many plants, fungi, and bacteria. Coumarins are well-known due to their anticancer, antiviral, antifungal, and antibacterial properties.
This study aims to provide a short overview of the biodiversity and pharmacological applications of coumarins, and its natural congeners, as well as an assessment of future medicinal benefits. Also, the study extended to review some of the data related coumarins and their derivatives, particularly those related to pharmaceutical and biological actions.
Conclusion: The implications of coumarins on the health of humans is a multifaceted issue, with many concerns about their safety, toxicity, and medicinal merits. Based on the findings of this review, the authors suggested that different bioactive coumarins for treating a variety of chronic health conditions, including cancer, Alzheimer's disease, HIV, diabetes, and hypertension.

Green synthesis of Schiff bases: a review study

Ahmed A. Mahmood

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 180-193
DOI: 10.33899/iphr.2022.170406

Objectives: Green chemistry is the field that implies instruments and procedures, by which it offers significant environmental and financial benefits above traditional synthetic methods. The modern attention in green chemistry has pretended an additional need for organic synthesis in which different reaction environments must locate, which decreases the use of toxic organic solvents or toxic chemicals.
These green methods must enhance the selectivity, shorten reaction time, and make the products isolation simpler than the ordinary routes. In the 19th century, Hugo Schiff recorded the first synthesis of Schiff bases (imines). A Schiff base is considered as an aldehyde with a C=N group (azomethine group) in steed of the C=O group, It is normally produced by condensation of primary amines with aldehydes. Schiff bases entertain many important biologically and pharmaceutical activities and they are distinguished for their pharmacological action and wide-range applications in the food industry.
This study tries to focus on the green synthetic methods used for Schiff bases synthesis, in order to find the best technique that offers higher yields in shorter time within eco-friendly environment.
Conclusions: The review considered many green synthetics techniques, from which the microwaves irradiation method is considered to be the best followed by the ultrasonic, natural acids utilizing and grinding methods.

Drug Abuse as a Contemporary Social Problem

Zena S. Hamed

Iraqi Journal of Pharmacy, 2021, Volume 18, Issue 2, Pages 194-202
DOI: 10.33899/iphr.2022.170407

Objective: Drug abuse and its repercussions are of the most serious problems in society nowadays. This is because of their enormous influence on the individual, the family, and its social effects like crime, social marginalization, and death from overdose or suicide, as well as on the economy.
The latest reports that are used gave a genuine assessment of the societal problem of drug abuse, and the results of these reports have also been evaluated to see if there are any negative consequences for drug abuse on families and individual and the methods that used to remedy these problems.
Drug abuse has been shown in several studies and publications to have detrimental implications for families and individual members, particularly children. These problems clearly affect a huge number of people, not just the person with the condition; they typically put a strain on the family and its members.
Conclusion: Drug abuse is a big social problem. In most climes, drug abusers will go to any way for getting the drug or substance. The social implications are a clear indication of how drug abuse can be a social problem.