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- FORMULATION AND CHARACTERIZATIONS OF ROSUVASTATIN LOADED NANOSUSPENSION
Abstract: Nanosuspensions (NS) are novel means of delivering drugs in controlled manner used to enhance bioavailability and get controlled therapeutic effect. Thus, the aim of the current study was to develop and optimize the preparation and characterization methods of Nanosuspensions for poorly water-soluble drug compound Rosuvastatin Ca (ROS) using Box Behnken Design (BBD). Pre formulation studies included differential scanning Calorimetry (DSC), Infra-Red (FTIR) spectroscopy and X-Ray diffraction (XRD) analysis were carried out to check compatibility of ROS and other excipient before starting optimization modeling by Box Behnken Design. The designed fifteen formulae of Nanosuspension were prepared and monitored for different responses to determine optimum formula and its expected characterization parameters. Then testing the efficiency of optimum formula against selected responses. Rosuvastatin Ca (ROS) nano suspension formulating was prepared using thin film hydration method using Box Behnken Design modeling include three independent variables (cholesterol (X1), Soy lecithin (X2), and span 60 (X3)), The responses were coded Y1 to Y6 respectively (particle size (PS), zeta potential (ZP), entrapment efficiency percent (EE%), as well as in vitro drug release after four hours, eight hours, and twelve hours. After obtaining optimum formula it was monitored for responses Y1 to Y6. The values of studied responses were particle size (408.6 nm), zeta potential (-53 mv), entrapment efficiency (79.2 %), cumulative drug release at 4 hr (53.2 %), cumulative drug release at 8 hr (67.1 %) and cumulative drug release at 12 hr (86.8 %). The results demonstrated that BBD optimization technique succeeded in prediction of an optimized ROS NS formula which when prepared and investigated, it met the demands of the desired responses comparing with free Rosuvastatin.
- PREPARATION AND EVALUATION OF SUSTAINED RELEASE MATRIX FORMULATIONS OF
VORICONAZOLE
Abstract: Voriconazole is a triazole antifungal with a half-life of 1.7 hours and 96% oral bioavailability. The oral route is the most popular of drug delivery routes. However, there are a few limitations to the traditional dosage form, for instance, fluctuations in plasma drug level. Sustained drug delivery system overcomes these limitations; it helps to maintain stable plasma drug concentrations by decreasing drug r elease and extending the duration of the effect. The main purpose of this study was to formulate voriconazole sustained release dosage form to enhance efficacy, decrease dose frequency, decrease its side effects, and improve patient compliance. The study explored various formulations for producing the sustained-release (S.R) dosage form, as well as assessed the drug's release kinetics and its stability.
Methodology: Fourier-transform Infrared Spectroscopy was used to investigate drug-polymer compatibility. The micromeritics of voriconazole powder and its blends were evaluated. Different sustained release tablets were formulated utilizing a wet granulation process and acrylic polymers (Eudragit) i.e., Eudragit RL100 and RS100 alone and as mixtures with different ratios, in different concentrations. In-vitro drug release of formulae was performed for 24 hours. The formula with desired control of drug release and complied with dissolution specifications for SR dosage forms was further evaluated for its stability by storage for 3 months at 30o C and 40o C and 75% relative humidity.
Results: no interaction was observed between voriconazole and polymers using FTIR. The powder blends micromeritics were found to be in accordance with the specification. Tablets showed release from 37.29 to 76 % up to 24 hr using USP type I technique. It was found that as polymer concentration increased, the drug release from tablet decreased. The selected formulation F13 which containing 5% of Eudragit RL100:RS100 at a ratio of (10:1) was found to be stable.
Conclusion: The obtained data concluded that the F13 formula gave more prominent S.R effect than using Eudragit RL100 or RS 100 alone.
- REVIEW ON THE SIGNIFICANCE OF PYRIMIDINE DERIVATIVES AS POTENT
ANTI-ANGIOGENIC VEGFR-2 INHIBITORS
Abstract: Cancer is a disease in which human cells grow uncontrollably and spread to other body parts. Cancer is the second leading cause of death globally and accounted for 9.6 million deaths in 2022 according to the statistics of the World Health Organization. Cancer can begin in any part of the human organs when the normal cell loses the ability to control the division cycle, which may inhibit apoptosis. Cancer cells grow and multiply by activating the angiogenetic factors to build new capillaries that can supply tumor tissue with nutrients. Cancerous tumors spread into or invade nearby tissues and can travel to other organs in the body to form new carcinogenic tissue by metastasis. The goal of treatment is control growth of cancer cells, and induction the programmed cell death. Pyrimidines and its derivatives have been found as effective and valuable pharmacophoric units in medicinal chemistry to design and develop a wide range of bioactive compounds. The present review summarizes the advances in lead compounds of pyrimidines hybrids and their related heterocycles in the treatment of cancer. Moreover, the review also helps to intensify the drug development process by providing an understanding of the potential role of these hybridized pharmacophoric features as VEGFR-2 inhibitors.
Abbreviations
Abbreviation
Meaning
FGFR1
Fibroblast growth factor receptor 1
VEGFR
Vascular Endothelial Growth Factor
CSF-1R
Colony stimulating factor 1 receptor
NETs
Neuroendocrine tumors
AKT
Protein kinase B (PKB), also known as Akt
A549
Human lung adenocarcinoma cell line
MCF-7
Human breast cancer cell line
HepG2
Human liver cancer cell line
Ovcar-3
High-grade serous ovarian adenocarcinoma cell line
Objectives
The aim of this study is to highlight the role of Pyrimidines containing compounds in inhibiting VEGFR-2 as well as to suggest some new aspects of treatment of cancer using pyrimidines scaffold soon.
- RECENT ADVANCES ON PYRIMIDINE DERIVATIVES AS ANTICANCER AGENTS.
Abstract: Cancer is a global health challenge; it impacts the quality of life and its treatment is associated with several side effects. Resistance of the cancer cells to the existing drugs has led to search for novel anticancer agents. Pyrimidine, a privileged scaffold, is part of living organisms and plays vital role in various biological procedures as well as in cancer pathogenesis. Due to resemblance in structure with the nucleotide base pair of DNA and RNA, it is recognized as valuable compound in the treatment of cancer.
Objectives
Many novel pyrimidine derivatives have been designed and developed for their anticancer activity in the last few years. The present review aims to focus on the structure of pyrimidine derivatives as anticancer agent from the last decade.
Results
In summary, the development of more potent and efficacious anticancer drugs with pyrimidine scaffold will continue to be a promising scaffold over the next 20 years.
- PIM KINASES INHIBITORS AND PYRIMIDINE-BASED ANTICANCER AGENTS
Abstract: Human phosphatidyl inositol mannoside kinases (Pim kinases) are important biological target for discovery of new anticancer agents. In addition, Pyrimidines have a good contribution as building blocks of many anticancer agents. Hence, a literature survey about Pim kinases inhibitors and pyrimidine-based anticancer agents have been achieved. In this survey, we introduced Pim kinase inhibitors under clinical assessment including imidazo[1,2-b]pyridazines, isatins, thiazolidine-2,4-diones, pyridinamines, and diaminopyrazoles. In addition, Pim kinase inhibitors under development were presented. These compounds include pyridine-quinolines, benzimidazoles indoles, cyano pyridines, pyridothieno[3,2-d]pyrimidin-4-ones, oxadiazole, and 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-ones. Furthermore, different pyrimidine-based anticancer agents have been discussed.
- GREEN CHEMOMETRIC ASSISTED SPECTROPHOTOMETRIC METHODS FOR DETERMINATION OF
CIPROFLOXACIN, METRONIDAZOLE, AND INDOMETHACIN RESIDUES IN PHARMACEUTICAL
INDUSTERIAL WASTEWATER EFFLUENTS
Abstract: Development and validation of three simple, eco-friendly, accurate and precise chemometric models have been presented for the spectrophotometric determination of ciprofloxacin (CIP), indomethacin (IND), and metronidazole (MET) residues in production wastewater samples. These methods are classical least square (CLS), principal component regression (PCR) and partial least square (PLS-1). A 3-factor 5-level experimental design was built leading to 25 mixtures containing different ratios of CIP, MET, and IND. Thirteen mixtures were used as a training set, and the other twelve were used as a validation set. Using of multi-wavelengths instead of the single wavelength spectrophotometry has greatly improved the precision and predictive abilities of these multivariate calibrations. The proposed methods have been found to be accurate, precise and can be used for determination of the drugs in pure form and industrial wastewater samples without preliminary separation steps. The methods described were used to accurately assess the drug residues in laboratory-prepared mixtures and actual industrial wastewater samples to confirm that it is free from these drug residues so it can be recycled and used for irrigation and other purposes.
- CHEMOMETRIC ASSISTED SPECTROPHOTOMETRIC METHODS FOR SIMULTANEOUS
DETERMINATION OF AMLODIPINE /CANDESARTAN MIXTURE IN THEIR PURE FORMS AND
THEIR PHARMACEUTICAL PREPARATIONS
Abstract: Three simple, accurate and precise multivariate calibration models, including classical least square (CLS), principal component regression (PCR) and partial least square (PLS-1), have been used for simultaneous determination of the components of recently approved fixed – dose combination tablet containing amlodipine / candesartan mixture in their pure forms and their pharmaceutical preparations, using spectral data in the range of (220nm-400nm). The CLS, PCR and PLS-1 models are useful in spectral analysis because the simultaneous employment of many spectral wavelengths instead of the single wavelength used in derivative spectrophotometry, which greatly improves the precision and predictive abilities of these multivariate calibrations. The developed methods were statistically compared with the reported spectrophotometric method and no significant differences were observed regarding both accuracy and precision, all the developed methods have been validated using external validation set. Moreover, the proposed models were successfully applied to the spectrophotometric determination of amolodipine besylate and candesartane cilexetil in Unisia® tablets.
- COMPARATIVE STUDY AMONG FOUR SPECTROPHOTOMETRIC METHODS FOR THE
SIMULTANEOUS DETERMINATION OF BINARY MIXTURE OF CHLORZOXAZONE AND
DICLOFENAC POTASSIUM
Abstract: Four simple, fast, accurate, reproducible, and non-sophisticated spectrophotometric methods were developed and validated for the simultaneous determination of chlorzoxazone and diclofenac potassium without preliminary separation in pure powder form and in their capsule formulation. Method A, is a dual wavelength spectrophotometric method in which the wavelengths selected for determination of chlorzoxazone were 259 nm and 294 nm, whereas the wavelengths selected for determination of diclofenac potassium were 294 nm and 242 nm. while method B, is a ratio difference spectrophotometric method in which the wavelengths selected for determination of chlorzoxazone were 280 nm and 230 nm, whereas the wavelengths selected for determination of diclofenac potassium were 246 nm and 284 nm. while method C, is the first derivative of the ratio spectra measured at 290 nm and 301 nm for chlorzoxazone and diclofenac potassium, respectively. While method D, is the constant center spectrophotometric method in which more measured at 280 nm and 277 nm for chlorzoxazone and diclofenac potassium, respectively. Regression analysis of Beer-Lambert’s plots showed good correlation in concentration range of 2.5 – 20 μg/mL for both drugs with LOD 0.308 μg/mL and 0.932 μg/mL, LOQ 0.458 μg/mL and 1.388 μg/mL, RSD 1.325 and 1.666 and % recovery 98.99 and 101.23 for chlorzoxazone and diclofenac potassium, respectively in method A. Furthermore, LOD 0.307 μg/mL and 0.373 μg/mL, LOQ 0.929 μg/mL and 1.123 μg/mL, RSD 1.065 and 1.371 and % recovery 99.94 and 101.53 for chlorzoxazone and diclofenac potassium, respectively in method B. Furthermore, LOD 0.287 μg/mL and 0.301 μg/mL, LOQ 0.871 μg/mL and 0.911 μg/mL, RSD 1.214 and 1.596 and % recovery 99.73 and 100.26 for chlorzoxazone and diclofenac potassium, respectively in method C. Furthermore, LOD 0.221 μg/mL and 0.331 μg/mL, LOQ 0.521 μg/mL and 0.825 μg/mL, RSD 0.914 and 1.412 and % recovery 101.22 and 98.59 for chlorzoxazone and diclofenac potassium, respectively in method D. The suggested methods were validated in compliance with the ICH guidelines and were successfully applied for determination of chlorzoxazone and diclofenac potassium in their laboratory prepared mixtures and commercial capsule formulation.
- THE PREVALENCE OF DERMATOPHYTOSIS, ITS RELATIONSHIP TO BLOOD TYPE AND
DISEASE MANAGEMENT HOSPITAL BASED STUDY IN EGYPT
Abstract: The aim of this study was to investigate the common dermatophytosis and dermatophyte(s) in Cairo hospitals, examining age, gender, blood groups, and dermatophyte incidence. It explores natural extracts like plant oils and fungal extracts as alternatives to commercial antifungal drugs and their synergistic effects. In this study, the prevalence of distinct types of dermatophytosis was investigated in 128 patients who were referred to the dermatology departments of different hospitals, including EL-Houd El-Marsoud, El Zahraa Medical Hospital, and El-Sahel Teaching Hospital in Cairo, Egypt.
Descriptive data for the tested patients was collected, including age, gender, the source of infection, and blood group type. The results showed that Tinea capitis was the most prevalent dermatophytosis, mostly in children. Investigating the correlation between blood group types and the incidence of the disease revealed that patients with blood groups B and O were the most sensitive ones. The most prevalent dermatophyte within the studied cases was identified and submitted to GenBank as Microsporum canis ON564613. To investigate the effectiveness of antifungal agents against M. canis, different common antifungal drugs, including terbinafine, ketoconazole, clotrimazole, fluconazole, and betadine, were evaluated using the agar disc diffusion test. In addition, natural alternatives were used including essential oils and an ethanolic fungal extract from Fusarium chlamydosporium. The minimum inhibitory concentration (MIC) of the potent agents was detected, including terbinafine, ketoconazole, clotrimazole, clove oil, and F. chlamydosporium extract. The effective antifungal agents against M. canis were clove oil and F. chlamydosporium extract, as well as commercial drugs. According to the MIC, a synergy between combinations of different concentrations of clove oil with terbinafine, ketoconazole, and the F. chlamydosporium extract showed a synergetic effect. These results show the promising potency of these combinations in disease control compared to their use individually.
- COMPARATIVE EVALUATION OF ANTICANCER AND ANTIBACTERIAL ACTIVITIES OF
ENDOPHYTIC FUNGUS-DERIVED ZNO NANOPARTICLES AND CHEMICALLY SYNTHESIZED ZNO
NANOPARTICLES
Abstract: Depending to the WHO, antibiotic resistance and limited anticancer and antimicrobial therapies continue to be serious worldwide health challenges. Current medicines' efficacy suffers by issues such as insufficient solubility, stability, and side effects. To create effective and dependable therapies against antibiotic resistance and robust illnesses, new techniques and strategies are required. Several metal nanoparticles synthesised via green synthesis or chemical synthesise, such as gold (Au), zine (ZnO), and others, have shown promising biological effects against malignancies and a wide spectrum of microbial illnesses caused by multi-drug resistant bacteria.
An eco-friendly biosynthetic technique was used to create zinc oxide nanoparticles (ZnO NPs), as well as their antibacterial and anticarcinogenic activities. Extracellular synthesis of nanoparticles made of zinc oxide ZnO nanoparticles was achieved in the current work using the cell filtrate of the endophytic fungus Fusarium chlamydosporum MW341592.1 isolated from healthy leaves of Eucalyptus sideroxylon plant. The nanoparticles were characterised by UV-VIS spectroscopy, X-ray diffraction (XRD), dynamic light scattering (DLS), transition electron microscopy (TEM), and energy-dispersive X-ray spectroscopy (EDX). The UV-Vis absorption spectra of the produced ZnO NPs showed bands in the UV area at (305) nm. Transmission electron microscopy TEM revealed average sizes of 19.3 nm, while shape revealed spherical like shape. The distinctive pattern of crystalline ZnO NPs was revealed by XRD diffract grams. Furthermore, Biological assay has shown that raising the nanoparticle concentration lowers the number of HCT-116 human colon cancer cells and CACO2 human intestinal cancer cells, as well as antibacterial pathogens Escherichia coli and Pseudomonas aeruginosa.
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