Universal Journal of Pharmaceutical Research
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    INNOVATIVE DRUG DELIVERY SYSTEMS FOR INFECTIOUS DISEASES OF THE SKIN

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    Introduction: Skin is the organ of the body that is exposed mostly to the microorganisms. Bacteria, fungi, and viruses are usually responsible for the infection of the skin. Due to lack of penetration through the stratum corneum of conventional systems used in infectious diseases of the skin leads to a decrease in bioavailability. For this reason, nanoscale drug delivery systems that could be used in infectious diseases of the skin are currently being investigated. Areas covered: In this review, innovative studies conducted over the years are presented. New topical formulations such as nanoparticles, microemulsions, liposomes, nanofibers and micelles etc are widely used and topic of research for many researchers. Conclusion:  Studies have shown that the smaller size and control of these delivery systems provide more effective treatment by increasing drug penetration into the skin. It has been found that drug delivery systems provide a better antimicrobial effect, especially in resistant infections caused by MRSA. Keywords: drug delivery systems, modified release dosage forms, skin infectious diseases, topical.                        Peer Review History: Received: 1 June 2022; Revised: 9 July; Accepted: 18 August; Available online: 15 September 2022 Academic Editor: Dr. Rola Jadallah, Arab American University, Palestine, [email protected] Reviewers: Prof. Dr. Hassan A.H. Al-Shamahy, Sana'a University, Yemen, [email protected] Dr. Nuray Arı, Ankara University, Turkiye, [email protected]

    COMPUTATIONAL DRUG REPROPOSING TO IDENTIFY SARS-COV-2 MPRO INHIBITORS: MOLECULAR DOCKING, ADMET ANALYSIS, AND IN-SILICO/IN-VITRO TOXICITY STUDY

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    Aim and Objective: After the COVID-19 outbreak, drug repurposing has emerged as an effective and fast approach for combating the SARS-CoV-2 crisis. in this work, computational drug repurposing has been utilized to identify new SARS-CoV-2Mpro inhibitors. Methods: Comparative molecular docking studies were used to evaluate the activity of the commercially available oral antiviral drug simeprevir and its degradation products (compounds 1–5) against the main protease (Mpro)of SARS-CoV-2 (PDB ID: 6lu7; resolution: 2.16 Å). Moreover, the ADMET and in-silico toxicity properties of the acidic (compounds 1–3) and oxidative (compounds 4 and 5) degradation products of simeprevir were predicted. Results: Docking studies revealed good binding affinities for compounds (1–5) against Mpro of SARS-CoV-2, with binding free energies ranging from −6.23 to −7.65 kcal/mol. The acidic degradant 2 exhibited the best affinity and was superior to simeprevir and a natural ligand. All compounds were expected to be safe to the CNS. Conclusion: Compounds 1, 4, and 5 were expected to possess good human intestinal absorption, whereas compounds 2 and 3 appeared to have moderate intestinal absorption.                          Peer Review History: Received: 5 August 2022; Revised: 9 September; Accepted: 20 October; Available online: 15 November 2022 Academic Editor: Dr. DANIYAN Oluwatoyin Michael, Obafemi Awolowo University, ILE-IFE, Nigeria, [email protected] Reviewers: Dr. Gehan Fawzy Abdel Raoof Kandeel, Pharmacognosy Department, National Research Centre, Dokki, 12622,  Giza, Egypt, [email protected]  Dr. Nicola Micale, University of Messina, Italy,  [email protected] Prof. Cyprian Ogbonna ONYEJI, Obafemi Awolowo University, Ile-Ife, Nigeria, [email protected]

    ANALYSIS OF THE ANTIBIOGRAM PROFILES OF BIOFILM FORMING STAPHYLOCOCCUS AUREUS AND ESCHERICHIA COLI

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    Background and Objectives: Bacteria that attach to the surfaces and produce polymeric matrix resulting in the biofilms formation are involved in a wider range of human infections. Biofilms forming Staphylococcus aureus and Escherichia coli are considered to be highly antibiotics resistant. This study aimed to analysis the antibiogram profile of biofilm forming S. aureus and E. coli in Mukalla city, Hadhramaut,Yemen. Methods: Sixty clinical isolates of S. aureus and E. coli were isolated from different clinical samples, and identified by standard bacteriological methods, then subjected to biofilm formation detection by tissue culture plate (TCP) method. The antibiotics susceptibility test was performed by disc diffusion (Kirby-Bauer) method. Chi-square test was used to analyze the data and p value< 0.05 was taken as significant. Results: Among the total isolates S. aureus and E. coli, TCP method detected 55% of isolates as strong, 25% as moderate and 25% as weak/non-biofilm producers. Biofilm forming of S. aureus developed significantly higher degrees of antibiotic resistance of amoxicillin/clavulanic acid100%, ceftazidime 95.8%, cefotaxime62.5%, cefadroxil 45.8%, ciprofloxacin 41.7% and ceftriaxone 25% with significant statistics correlation the resistance of amoxicillin/clavulanic acid and ceftazidime and bacterial biofilm production (p-value< 0.05). The rates of antibiotics resistance biofilm E. coli were 100%, 91.7%, 75%, 70.8%, 66.7%, 62.5% and 33.3%for amoxicillin/clavulanic acid, cefadroxil, cefotaxime, ceftazidime, ceftriaxone, ciprofloxacin and co-trimoxazole respectively with statistically significant correlation of cefadroxil resistance (p-value < 0.05). Conclusion: TCP method showed that S. aureus and E. coli isolates have high degree of biofilm forming ability. A high antibiotics resistance found in biofilm producers isolates than non-biofilm producers.                     Peer Review History: Received: 3 October 2021; Revised: 9 November; Accepted: 12 December; Available online: 15 January 2022 Academic Editor: Dr. Nuray Arı, Ankara University, Turkiye, [email protected] Reviewers: Dr. Wadhah Hassan Ali Edrees, Hajja University, Yemen, [email protected] Dr. Tamer Elhabibi, Suez Canal University, Egypt, [email protected] Dr. Rawaa Souhil Al-Kayali, Aleppo University, Syria, [email protected] Rola Jadallah, Arab American University, Palestine, [email protected]

    BLADDER CANCER: DIFFERENTIATION OF TYPES, AGE, SEX DISTRIBUTION AND ASSOCIATED VARIANTS WITH GRADATION

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     Background:  Urinary bladder cancer (UBC) is the ninth most common cancer in the world, and the third most common cancer among men in West Asian countries, including Arab countries. Despite the increasing prevalence of UBC in developing countries, many places, including Yemen, do not have representative studies showing the true impact of these tumors on the population. Aims: To describe the different types of bladder cancers, and their distributions with age, and sex and to correlated different types with gradation, invasion muscles; and schistosomiasis in the last ten years in a single Yemini institute. Materials and methods:  An observational descriptive study was performed on UBC patients who were subsequently diagnosed selectively by histopathological study in the Department of Pathology at the National Center for Public Health Laboratories (NCPHL) Sana'a, Yemen, over a period of about 10 years from January 1, 2012 to October 31, 2021. The study variables were cancer histological type, sex, grades and age. Types, grading and histological diagnoses were formed in line with the World Health Organization classification of bladder cancer. Results: Most of the cases were in the age group 60-69 years (32%), followed by 70 years (22.3%), and 50-59 years (20%).  The most common UBCs were urothelial neoplasms (UNs) (71.5%), followed by squamous neoplasms (SNs) (24.4%) while other types were less frequent. There was a cytologically high grade with a significance rate (64.2%) with UNs. There was a significance rate of:  schistosomiasis (43.8%) with SNs as OR=19.5 (p < 0.001), and invasion of muscle fibers  (66.4%) with SNs as OR=3.3,  UNs (37.1%) as OR=11.2 (p < 0.001). Also there was a significance rate of GII grade (46.1%) with SNs as OR=64.1 (p<0.001) and GNs (33.3%) as  OR=3.8 (p =0.02).  Conclusion:  The present study verification data congruence with those in the international literature and reports of neighboring countries, with some minor differences. This study documents a high incidence of urothelial neoplasms, with a male predominance and a peak incidence in the sixth decade of life. Imminent studies are needed to identify risk factors that increase cystitis in more detail and to study genetic susceptibility to inflammation and inflammatory markers before cancer is diagnosed.              Peer Review History: Received: 12 October 2021; Revised: 9 November; Accepted: 13 December; Available online: 15 January 2022 Academic Editor: Dr. Nuray Arı, Ankara University, Turkiye, [email protected] Reviewers: Dr. Bilge Ahsen KARA, Ankara Gazi Mustafa Kemal Hospital, Turkey, [email protected] Dr. Eyassu Mathewos, School of public health, college of health sciences and medicine, Wolaita Soddo university- P.O. Box 158, Wolaita Soddo, Ethiopia.    Md. Monirul Islam, Department of Pharmacy, Faculty of Health Sciences, Northern University Bangladesh, Dhaka, Bangladesh.  [email protected] Dr. Rawaa Souhil Al-Kayali, Aleppo University, Syria, [email protected]

    ANTIMICROBIAL ACTIVITY OF SODIUM HYPOCHLORITE, NANO SILVER AND CHLORHEXIDINE AGAINST MONO-SPECIES BIOFILMS OF SELECTED MICROORGANISMS OF ORAL SOURCES

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    Background: Among the measures involved in the control of endodontic infection, irrigation is an important factor in the elimination of microorganisms present in the open root canal. It is known that mechanical debridement alone does not result in a complete or permanent reduction of bacteria, therefore antimicrobial agents are used as an aid to mechanical cleaning to completely kill or reduce the number of microorganisms. Aim:  To investigate the antimicrobial activity of 2.5%, 5.25% sodium hypochlorite and 2.0% chlorhexidine liquid and as the first new study of 60 mg/L silver nanoparticles as an endodontic-irrigating substances against single-species biofilms. Methods: Biofilms of Enterococcus faecalis, Staphylococcus aureus, Pseudomonas aeruginosa and Candida albicans oral sources were produced on a cellulose nitrate membrane placed on agar medium. Membrane filters were transferred to tubes containing 2 mL of fresh broth medium plus neutralizers. Microorganisms were suspended using a vortex, and the inoculum was serially diluted 10-fold. Aliquots of the dilutions were placed on 5% blood agar medium and incubated under appropriate gaseous conditions. Colony forming units were calculated. Results:  The antimicrobial agents in liquid presentation, especially 5.25% NaOCl, 2% chlorhexidine, and 2% nano-silver liquid killed the tested microorganisms more rapidly with mean rank equal to 1.4, 1.9, and 1.6, respectively. Saline did not inhibit the growth of any of the tested microorganisms, as it was statistically (p < 0.05) different for NaOCl, Nano-silver and chlorhexidine. Conclusions:  Preferring agents in liquid supply to get rid of biofilm microorganisms, especially 5.25% NaOCl and 60mg/L nanosilver liquid.                         Peer Review History: Received: 4 December 2021; Revised: 9 January 2022; Accepted: 11 February, Available online: 15 March 2022 Academic Editor: Dr. Nuray Arı, Ankara University, Turkiye, [email protected] Reviewers: Prof. Dr. Gorkem Dulger, Duzce University, Turkey, [email protected] Dr. Rawaa Souhil Al-Kayali, Aleppo University, Syria, [email protected] Dr. Wadhah Hassan Ali Edrees, Hajja University, Yemen, [email protected]

    SYNTHESIS AND ANTICANCER ACTIVITY TOWARDS HEPG-2 AND MCF-7 OF NEW 2-AMINO-1,3,4-THIADIAZOLE AND THEIR SUGAR DERIVATIVES

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    Background: In recent papers, it was found that 1,3,4-oxadiazole, 1,3,4-thiadiazoleand 1,2,4-triazole pharmacophores are present in several drugs, tiodazosin and nesapidil (antihypertensive), raltegravir (antiretroviral), Furamizole, cefazolin and ceftezole (antibiotics), acetazolamide and methazolamide (carbonic anhydrase inhibitors), sulfamethizole (antibacterial), fluconazole, ravuconazole, voriconazole, itraconazole, posaconazole, and tebuconazole (antifungal). Methods: Thiosemicarbazide was reacted with ethyl p-substituted-phenyl glycinate; namely, ethyl p-tolylglycinate (1), ethyl p-methoxyphenylglycinate (2) or ethyl p-bromophenylglycinate (3), respectively to give compounds 4-6, which then kept with conc. H2SO4 overnight to yield 1,3,4-thiadiazol-2-amine derivatives 7-9. Compounds 10-18 were yielded by reaction of compounds 7-9 with D-sugars namely, D-galactose, D-glucose and/ or D-xylose in ethanol and catalytic amount of acetic acid. Compounds (10-18) were then acetylated with acetic anhydride to form compounds (19-21). Finely compound 7 was reacted with chloroacetyl chloride and/or acetic anhydride to afford compounds 22 and/or 23 respectively. Results: Six compounds were evaluated in vitro for their cytotoxic activity on the HepG-2 and MCF-7 human cancer cell lines. Conclusion: Among the tested compounds, compounds 6 and 13 were found to be the more potent for their cytotoxic activity on the two cancer cell lines.                            Peer Review History: Received: 5 February 2022; Revised: 7 March; Accepted: 13 April; Available online: 15 May 2022 Academic Editor: Dr. Asia Selman Abdullah, Pharmacy institute, University of Basrah, Iraq, [email protected] Reviewers: Dr. Andrzej Szymański, Poznan University of Technology, Poland, [email protected] Dr. Bilge Ahsen KARA, Ankara Gazi Mustafa Kemal Hospital, Turkey, [email protected]

    NIGELLA SATIVA L.: A GOLDEN REMEDY: SIGNIFICANCE WORLDWIDE HIGHLIGHTING THEIR POSSIBLE USE FOR COVID-19

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    Nigella sativa L. is a therapeutic natural herb that cures several serious ailments, so can be considered a Golden remedy. It has been used for centuries and has a long history in different cultures. This review article has surveyed nearly all the relevant literature on Nigella sativa L. from 1960-2020, offering a broad range of data including the origin, taxonomy, botany, history of traditional uses in different regions then passing through their phytochemistry, pharmacology, and consumed natural pharmaceutical preparations till recent findings and their possible use in COVID-19 therapy. The main aim of this review is to focus on the importance of Nigella sativa L. as a medicinal herb used widely in therapy and to correlate its phytochemical constituents with their pharmacological effects. The biological importance was attributed to Thymoquinone in the first-place present in the volatile oil of the seeds and other classes such as sterols, triterpenes, tannins, flavonoids, and cardiac glycosides, alkaloids, saponins, coumarins, volatile bases, glucosinolates, and anthraquinones. Moreover, several studies confirmed its benefits in Alzheimer’s disease, as a potent antioxidant, cytotoxic, antiallergic, antimicrobial, etc. In addition to other studies which documented the use of this plant mainly the seeds and the extracted essential oil, in the production of cosmeceutical preparations, and its role as a nutritive spice in the food industry due to its very low toxicity, besides their use as fodder for farm animals.                    Peer Review History: Received: 3 April 2022; Revised: 12 May; Accepted: 13 June; Available online: 15 July 2022 Academic Editor: Ahmad Najib, Universitas Muslim Indonesia,  Indonesia, [email protected] Reviewers: Ahmad Najib, Universitas Muslim Indonesia, Makassar, Indonesia, [email protected] Prof. Dr. Ali Gamal Ahmed Al-kaf, Sana'a university, Yemen, [email protected] Prof. Dr. Hüsniye Kayalar, Ege University, Turkey, [email protected]

    ANTIBIOTIC RESISTANCE PROFILE OF ISOLATED BACTERIA AT THE SANGMELIMA REFERENCE HOSPITAL, SOUTH CAMEROON REGION: A RETROSPECTIVE STUDY

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    Background and objective: Bacterial resistance to antibiotics is now one of the most serious threats to global health. Knowledge of the main bacterial species responsible for bacteremia and their antibiotic resistance profile makes possible to provide an objective basis for effective antibiotic therapy. However, in the South Cameroon region, microbiological documentation is not always available. The objective of our study was to determine the resistance profile of bacteria isolated at the Sangmélima Reference Hospital. Methods: It was a retroprospective study on biological samples collected from interned and ambulatory patients seen at the Sangmélima Reference Hospital during the period from January 2021 to October 2021.The samples were cultured on specific media and the susceptibility was carried out on agar media using Kirby-Bauertechnique and interpretation according to the 2020 CASFM Guidelines. Results: For the retrospective part, GNB were most represented (15/26; 57.7%,) with the E. coli (n=12/15) and only Staphylococcus spp for GPB (n=11/26). Staphylococcus resistance was particularly relevant with 81.81% to erythromycin, 63.63% to cefoxitin and 72.72% to Cotrimoxazole. E. coli showed a resistance of 66.66% for augmentin and 83.33% for cefuroxime. In the prospective part, GPB were only represented by Staphylococcus epidermidis (7/7 ; 50%), and GNB included E. coli (3/7 ; 21.42%), K. pneumoniae (2/7; 14.29%) and A baumannii (2/7; 14.29%). For all isolated bacteria strains, a high resistance to the majority of betalactams and penicillin was observed. However, bacteria with greater antibiotic resistance were Staphylococcus strains, highly resistant to beta-lactams, while A. baumannii strains showed higher resistance, and E. coli especially to penicillins and fluoroquinolones. Conclusion: E. coli and Staphylococcus spp were predominant isolated bacteria with high rate of resistance to antibiotics frequently used in hospital. Strict adherence to infection prevention practices and judicious use of antibiotics are recommended to slow te spread of antimicrobial resistance (AMR).                   Peer Review History: Received: 6 April 2022; Revised: 11 May; Accepted: 14 June; Available online: 15 July 2022 Academic Editor: Dr. Emmanuel O. Olorunsola, Department of Pharmaceutics & Pharmaceutical Technology, University of Uyo, Nigeria, [email protected] Reviewers: Prof. Dr. Hassan A.H. Al-Shamahy, Sana'a University, Yemen, [email protected] Dr. Wadhah Hassan Ali Edrees, Hajja University, Yemen, [email protected]

    CARDIOVASCULAR RISK AND HIV INFECTION IN PATIENTS AGED 50 YEARS AND OLDER AT THE AHALA DISTRICT MEDICAL CENTER, CAMEROON

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    Aim and objectives: Older people living with HIV (P50+) are living longer and longer and are therefore prone to age-related comorbidities. The objective of this study was to investigate the cardiovascular risk of P50+ followed in an HIV care unit in Cameroon. Methods: Cardiovascular risk factors (CVRF) were assessed through clinical examination and the following paraclinical exams fasting blood glucose, lipid profile, creatinine level with calculation of glomerular filtration rate according to the Cockcroft and Gault formula and resting electrocardiogram. Results: The proportion of P50+ was 13.9% and 80 patients were included in the study. The following prevalence of CVRF were found sedentary lifestyle (77.5%), chronic smoking (5%). Fifteen percent reported having hypertension and 25% of the P50+ had high blood pressure during physical examination. Similarly, 2.5% of the patients reported diabetes and 7.5% of the P50+ had high blood sugar levels. The examinations performed revealed 2.5% of LDL-cholesterol dyslipidemia, 23.1% of glomerular filtration rate abnormalities, 5.7% of left ventricular hypertrophy (LVH), and 22.9% of electrocardiographic signs of myocardial ischemia. The study of the interdependence between CVRF and the characteristics of the population revealed a relationship of dependence between physical activity and age (p=0.002), diabetes and age (p=0.004), diabetes and duration of HIV (p=0.007), LVH and duration of HIV (p=0.001). Conclusion: Cardiovascular risk is high in P50+ which could make them vulnerable to cardiovascular events. It is therefore necessary or even essential that cardiovascular risk assessment be integrated into the continuum of care of PLWH in general and P50+ particularly in HIV care units.                    Peer Review History: Received: 2 April 2022; Revised: 10 May; Accepted: 13 June; Available online: 15 July 2022 Academic Editor:  Dr. A.A. Mgbahurike, University of Port Harcourt, Nigeria, [email protected] Reviewers: Dr. Peter Juma Ochieng, Biotech Research Center (BRC), Obuda University, Hungary, [email protected] Dr. Esther Marguerite Chase DJANGA, Faculty of Medicine and Biomedical Sciences. Department of Public Health. University of Yaoundé I, Cameroon. [email protected]

    PHYTOCHEMICAL SCREENING OF AQUEOUS, ETHANOL AND METHANOL EXTRACTS OF FLACOURTIA INDICA LEAF AND RIPE FRUIT

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    Aim and Objective: Plants have been exploited over the years for their therapeutic benefits, because they contain a lot of bioactive compounds that have potentials and ability to treat or manage diseases. Thus, this study investigated the qualitative and quantitative phytochemicals in Flacourtia indica (F. indica) aqueous, ethanol and methanol leaf and ripe fruit extracts. Methods: F. indica leaf and ripe fruit were harvested from a fruiting tree in Emene, Enugu state, Nigeria, and the analyses were done following standard methods. Results: Qualitative screening revealed that tested extracts contained saponin, tannin, flavonoids, alkaloids, glycosides and phenol. While proteins and steroids were not detectable in aqueous and ethanol leaf and ripe fruit extracts, they were present in moderately high (++) amount and in trace amount (+) in methanol leaf extract of f. Indica. The quantitative screening comparatively revealed that concentrations of glycosides (mg/ml), flavonoids (mg/ml), alkaloids (mg/ml) and tannins (mg/ml) were higher and phenol (mg/ml) lower in ethanol leaf extract, while in the aqueous leaf extract, phenol (mg/ml) was higher; in the ethanol fruit extract, flavonoids (mg/ml) and alkaloids (mg/ml) were higher, and in the aqueous fruit extract, phenol (mg/ml) and tannin (mg/ml) were higher. Conclusion: In conclusion, quantitatively, ethanol was a better solvent of extraction than water and methanol and f. indica leaf and ripe fruit are rich sources of secondary bioactive phyto-molecules, which could be consumed for their health and therapeutic benefits.                           Peer Review History: Received: 8 August 2022; Revised: 11 September; Accepted: 22 October; Available online: 15 November 2022 Academic Editor: Dr. Asia Selman Abdullah, Pharmacy institute, University of Basrah, Iraq, [email protected] Reviewers: Dr. Sangeetha Arullappan, Universiti Tunku Abdul Rahman, Malaysia, [email protected] Prof. Ali Gamal Ahmed Al-kaf, Sana'a university, Yemen, [email protected] Dr. Gehan Fawzy Abdel Raoof Kandeel, Pharmacognosy Department, National Research Centre, Dokki, 12622,  Giza, Egypt, [email protected]

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