Pharmaceutical Sciences

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https://hdl.handle.net/20.500.11888/3211

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DEVELOPMENT AND EVALUATION OF THE ANTICANCER, ANTIOXIDANT, AND ANTIMICROBIAL ACTIVITIES OF CYPRESS OIL NANOEMULGEL
(An-Najah National University, 2024-07-01) Shahin, Ayah
Cypress oil is a potent essential oil known for its wide range of therapeutic activities. This study aimed to incorporate cypress oil into nanoemulgels to overcome their low solubility and high volatility. Gas chromatography-mass spectrometry identified the chemical composition. The cypress oil nanoemulsion was optimized, and then it was incorporated with Carbopol hydrogel to produce cypress oil nanoemulgel. DPPH scavenger technique measured the cypress oil and its nanoemulgel antioxidant activity. Then, the droplet size, PDI, zeta potential, rheology, antimicrobial, anticancer, and anti-inflammatory activities were evaluated utilizing reference methods. The chemical composition of cypress oil is predominantly composed of monoterpene hydrocarbons, with α-pinene as the major component (50.72%), followed by 3-b-carene (27.57%). The ternary phase diagram revealed that the nanoemulsion containing 40% Tween, 10% Span, and 50% cypress oil had an optimized droplet size of 105.28 ±2.12 nm and a PDI of 0.112 ±0.016 nm. The cypress nanoemulgel formulation showed no significant change in droplet size or PDI, while it has a zeta potential of -33 mV. Moreover, the antioxidant efficiency of cypress oil was IC50 = 14.7 ±0.3 μg/mL, while it was reduced to more than half for nanoemulgel with IC50=6.6 ±0.13 µg/ml. Potent antibacterial activity was reported against several gram-positive and gram-negative bacteria, with inhibition zones in the 11–36 mm range. Also, effective antifungal activity was noticed against different species of Candida albicans in the range of 16–24 mm. The formulated nanoemulgel had better activity compared to the oil alone. Furthermore, it was more potent than the oil as an anticancer agent against Hep-G2 cells, with an IC50 of 39.81 µg/ml, followed by 58.88 and 61.65 µg/ml for MCF-7 and HeLa cell line. It also demonstrated an anti-fibrotic effect with an IC50 of 63.09 µg/ml against LX-2 cell line. The cypress oil nanoemulgel was more selective for COX-2 than COX-1. In addition, the IC50 of the nanoemulgel toward COX-2 (13.96 µg/ml) was almost half the value for the oil (28.78 µg/ml). The overall findings suggest that cypress oil nanoemulgel holds promise to counteract several skin infections and cancer cell lines. However, further in vivo studies are needed.
SYNTHESIS AND CHARACTERIZATION OF SILVER NANOPARTICLES USING PALESTINIAN THYMUS CAPITATUS, WITH EVALUATION OF ITS POTENTIAL ANTI-OXIDANT, ANTIMICROBIAL, AND ANTICANCER ACTIVITIES
(An Najah National University, 2025-03-06) Asmar, Lara
Introduction: Nowadays, the demand for thyme oil is growing because of the wide variety of its applications. Thymus capitatus, or Thymbra capitat, belongs to the Lamiaceae family and was the main herbal plant in this research that aimed to study the potential synthesis of silver nanoparticles utilizing Thymus capitatus essential oil as a reducing and stabilizing agent and to assess its antioxidant, anticancer, antimicrobial, and anti-inflammatory properties for potential biomedical applications in medicine. Methodology: The essential oil of T. capitatus was obtained through hydrodistillation. The chemical composition of the essential oil was identified and characterized using GC/MS spectrometry. The green synthesis of AgNPs was accomplished by dropwise adding diluted T. capitatus oil to a 0.1 M aqueous solution of AgNO3. Characterization of synthesized AgNPs was accomplished by several techniques, including UV-visible spectrometry, dynamic light scattering, atomic force microscopy, and zeta potential analyzer. An antimicrobial assay for both synthesized AgNPs was performed against six different types of the most common bacteria in addition to the fungi Candida albicans. Also, the cytotoxicity of synthesized AgNPs and T. capitatus EO was studied on many different cell types, including, Hep3B, B16F1, 3T3, MCF-7, HeLa, and HEK293 cell lines. The evaluation of antioxidant activity was conducted using a DPPH test. The effectiveness of the synthesized AgNPs and T. capitatus EO in reducing inflammation was assessed through the COX (human) inhibitor screening assay kit. Results: The EO yield of extraction was 1.16 %W/W, the major chemical components of the EOs were carvacrol with the highest percentage (37.47%), P-cymene (27.96%), and γ-terpinene (26.3%). The green synthesis of T. capitatus AgNPs was accomplished after several trials to determine the optimal synthesis parameter. Finally, we had a dark-brown colloidal sample of AgNPs. The UV-visible spectral peak was obtained at 425 nm wavelength. The AFM image shows a mostly spherical shape of the synthesized AgNPs with a diameter range between 40 and 80 nm. In contrast, the average effective diameter obtained by DSL analysis was 119.80 ±1.7 nm, and the zeta potential value was -43.86 ±2.2. Both synthesized AgNPS and T. capitatus EO have good antioxidant activity compared to the reference Trolox. However, the potency of synthesized AgNPs was 5-fold greater than T. capitatus EO, with IC50 values of 2.27 ±0.91, 10.47 ±1.11, and 48.97 ±1.20μg/ml for Trolox, synthesized AgNPs, and T. capitatus oil, respectively. The synthesized AgNPs had antimicrobial activity about 5-folds greater than T. capitatus pure oil against all bacterial strains that were used in addition to candida albicans, with MIC values ranging between (0.016 _ 0.290 μg/ml) for AgNPs, and (0.078 and 1.562 μg/ml) for pure T. capitatus EO. Both T. capitatus EO and synthesized AgNPs showed promising results against HeLa, MCF-7, NIH3T3, HEK293, Hep3B, and B16F1 cell lines. Synthesized AgNPs have an average percent inhibition of 80% at 200 μg/ml concentration. Finally, results indicate a great anti-inflammatory activity for synthesized AgNPs and the pure oil, also, both of them were more selective for COX-2 than COX-1, especially the synthesized NPs, whose IC50 value (2.83 µg/ml) toward COX-2 was almost 14% of the IC50 value (19.42 µg/ml) for the oil. Conclusion: The green synthesis of AgNPs can be performed by using Palestinian T. capitatus EOs as a reducing agent. Furthermore, these AgNPs can be used to develop a new treatment line for cancer therapy due to their anticancer activities
DESIGN, SYNTHESIS, AND BIOLOGICAL EVALUATION OF THIAZOLE-CARBOXAMIDE DERIVATIVES AS COX INHIBITORS
(2022-12-26) Rozan Ghassan Sabobeh
ABSTRACT Non-Steroidal anti-inflammatory drugs (NSAIDs) are often employed to alleviate swelling and discomfort and lower high temperatures. They inhibit the cyclooxygenase enzyme (COX) required to convert arachidonic acid to Prostaglandins that are inflammatory. In this master's thesis, new thiazole derivatives with aniline derivatives were synthesized, specified, and estimated for their selectivity and potency at COX-1 and COX-2 by an in vitro COX inhibition assay kit. The synthesized compounds' cytotoxicity was estimated using an MTS assay against human hepatic stellate (LX-2) and the normal cell line (Hek293T). HRMS, 1H-NMR, and 13C-NMR techniques characterized all newly synthesized chemicals. The results demonstrated that the most effective compound against the COX-1 enzyme was 2b with an IC50 =0.239 µM. It also showed potent activity against COX-2 with IC50=0.191 µM with a selectivity ratio of 1.251. The highest selectivity ratio was (2.766) for 2a compound against COX-2 with an IC50 = 0.958 µM relating to celecoxib ratio (23.8) and its IC50 against COX-2 =0.002 µM. The 2j compound also showed good selectivity towards COX-2 (1.507) with an IC50 of 0.957 µM. All compounds showed negligible cytotoxic activity against the evaluated normal cell lines, and the IC50 values were more than 300 µM, except compound 2b, whose IC50 values were 203.711.89 and 116.96±2.05 µM against LX-2 and Hek293t cell lines, respectively. Keywords: Anti-inflammatory; Cyclooxygenase enzyme; COX inhibitors; Docking studies; Heterocyclic; Thiazole-carboxamide; NSAIDs.
BIOLOGICAL EVALUATION OF 2-OXO-BENZOXAZOLE DERIVATIVES
(2023-09-07) Haneen Marwan Abu Katab
Benzoxazole derivatives are essential building blocks for innovative drugs due to their wide range of biological activities in medicinal chemistry, particularly their pharmacological effects (such as analgesic, antibacterial, antifungal, anti-inflammatory, and anticancer properties). The importance of benzoxazole derivatives in drug development is emphasized by this work, which also highlights their potential as therapeutic targets with a variety of pharmacological actions and structural flexibility. This study investigates the 1,3-oxazole nucleus, which is a very effective molecule with antibacterial, anticancer, analgesic, and anti-inflammatory characteristics. These substances are created both naturally and artificially by several organisms, including bacteria and marine life. Pharmaceutical compounds belonging to the 1,3-oxazole family can be used to synthesize a wide range of molecules with various therapeutic applications, such as antiviral and anticancer effects. The fascinating possibility of benzoxazole derivatives inhibiting anaerobic choline metabolism and their possible anticancer effects is examined in this work. Certain compounds based on benzoxazoles exhibit enhanced cytotoxicity, especially towards particular cancer cell lines, suggesting that they may be useful in stopping the spread of cancer cells. The promise of benzoxazole derivatives in pharmaceutical research is highly praised, and more investigation into the benzoxazole scaffold and its functionalization is encouraged to find more powerful and selective molecules with enhanced activity and decreased toxicity. The study's findings on sixteen artificial chemicals tested against seven cancer cell lines are presented in the article. The compounds BNZ-2, BNZ-4, BNZ-7, BNZ-9, and BNZ-10 show promise as anticancer agents. Key moieties, such as chlorobenzoyl, piperazine, piperidine, morpholinomethyl, and 4-methylpiperidin-1-yl, that are responsible for their actions against different cell lines are identified by a structural analysis using Structure-Activity Relationship (SAR) study. BNZ-10 has a lower IC50 value than other well-known anticancer medications, which suggests that it may be a more effective treatment against particular cancer cell types. It's important to remember, nevertheless, that doxorubicin (DOX) has far lower IC50 values than the majority of BNZ-1-16 drugs and is nonetheless a powerful anticancer agent. The study concludes by highlighting the tremendous promise of benzoxazole derivatives in drug development, particularly in the treatment of cancer, and the significance of particular structural motifs in controlling their biological activity. Novel treatment approaches in hepG2-associated malignancies require further research on molecular interactions and processes, especially those that affect hepG2 cells. The research advances the hunt for new medicines and helps to rationally develop anticancer drugs. Keywords: Benzoxazole Derivatives; Anticancer Efficacy; Structure-Activity Relationship (SAR); IC50 Values
INFLUENCE OF FOOD INDUCED VISCOSITY ON DISSOLUTION AND DISINTEGRATION OF TABLETS: EFFECT OF FORMULATION AND PROCESS PARAMETERS ON TABLET MANUFACTURED BY WET GRANULATION
(2023-06-05) Zain Alabedin Zanoon
Abstract Postprandial elevation in gastric viscosity may retard tablet disintegration and delay drug dissolution from solid dosage forms, resulting in a significant decrease in drug bioavailability thereby affecting the therapeutic efficacy. This may be critical especially for medication where rapid onset of action is required. Deep understanding of the critical processing parameters on tablet disintegration and drug dissolution under fed conditions will help in designing a formulation with minimum viscosity mediated negative food effects. The current research aims to study the impact of formulation and processing factors on tablet disintegration and release of Active Pharmaceutical ingredient (API) under both fasting state and fed states. The effect of different types of fillers was investigated in different formulations: Lactose monohydrate, corn starch and Microcrystalline cellulose (MCC), as well as, Di-calcium phosphate dehydrate. Wet granulation is a critical manufacturing step for oral solid dosage forms. Wet granulation method was applied in the preparation of ten immediate release formulations with Paracetamol serving as the model drug. The effects of wet granulation parameters such as: the mode of incorporation of disintegrant and the type of the granulating solvent were highlighted. The study concluded that filler type is found to affect tablet disintegration: MCC based formulations gave the quickest drug disintegration in simulated fasted state, but they were the worst under viscous media. Lactose and Dicalcium Phosphate (DCP) based formulations provide rapid disintegration under fed state. Formulations prepared by using alcohol as solvent of granulation had shorter disintegration times compared to formulations using water in both fasting and fed states. The addition of Sodium Starch Glyclolate (SSG) intra-granularly results in shorter disintegration time compared to the extra-granular counterparts under fed condition. The study recommends that: the obtained results highlight the importance of formulation excipients (filler type) and manufacturing parameters on tablet disintegration. This study will provide guidance that help in design and development of formulation with minimal food effect. Keywords: Behaviour; Disintegration; Dissolution; Even Formula; Fasting State; Fed State; Odd Formula.

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