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1.
ACS Omega ; 9(21): 23001-23012, 2024 May 28.
Article in English | MEDLINE | ID: mdl-38826538

ABSTRACT

The literature does not provide any "high-performance thin-layer chromatographic (HPTLC)" techniques for the determination of a novel antidiabetic medicine, ertugliflozin (ERZ). Additionally, there are not many environmentally friendly analytical methods for ERZ measurement in the literature. A rapid, sensitive, and eco-friendly reversed-phase-HPTLC (RP-HPTLC) method was designed and validated in an attempt to analyze ERZ in marketed pharmaceutical tablets more precisely, accurately, and sustainably over the traditional normal-phase HPTLC (NP-HPTLC) method. The stationary phases used in the NP- and RP-HPTLC procedures were silica gel 60 NP-18F254S and 60 RP-18F254S plates, respectively. For NP-HPTLC, a chloroform/methanol (85:15 v/v) mobile phase was used. However, ethanol-water (80:20 v/v) was the preferred method for RP-HPTLC. Four distinct methodologies, including the National Environmental Method Index (NEMI), Analytical Eco-Scale (AES), ChlorTox, and Analytical GREEnness (AGREE) approaches, were used to evaluate the greenness of both procedures. For both approaches, ERZ detection was carried out at 199 nm. Using the NP- and RP-HPTLC techniques, the ERZ measurement was linear in the 50-600 and 25-1200 ng/band ranges. The RP-HPTLC method was found to be more robust, accurate, precise, linear, sensitive, and eco-friendly compared to the NP-HPTLC approach. The results of four greenness tools demonstrated that the RP strategy was greener than the NP strategy and all other reported HPLC techniques. The fact that both techniques can assess ERZ when its degradation products are present implies that they both have characteristics that point to stability-indicating features. 87.41 and 99.28%, respectively, were the assay results for ERZ in commercial tablets when utilizing the NP and RP procedures. Based on several validation and greenness metrics, it was determined that the RP-HPTLC approach was better than the NP-HPTLC method. As a result, it is possible to determine ERZ in pharmaceutical products using the RP-HPTLC approach.

2.
Saudi Pharm J ; 32(6): 102072, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38726227

ABSTRACT

Silymarin (SLR) is a poorly water-soluble bioactive compound with a wide range of therapeutic activities. Nanosized silymarin vesicles (F1-F6) were prepared by the solvent evaporation rehydration method. The silymarin vesicles were evaluated for vesicle size, surface charge, entrapment efficiency, and drug release studies. The optimized SLR lipid vesicle (F3) was further modified with the addition of the cationic polymer chitosan. After that, the modified vesicle (F3C1) was assessed for permeation flux, antimicrobial activity, cell viability, and molecular docking studies. The silymarin vesicles showed nanometric size (<250 nm), low polydispersibility index (<0.05), negative surface charge, and high SLR entrapment (85-95 %). The drug release study result demonstrated a maximum drug release of 91.2 ± 2.8 %. After adding chitosan to the surface, there was a significant change in the size, polydispersibility index, surface charge (positive), and encapsulation efficiency. The drug release was found to be prolonged, and the permeation flux was also increased in comparison to free SLR. A comparative antimicrobial result was observed in comparison to the free SLR and standard drug. The cell viability assay also demonstrated a low IC50 value for F3C1 against the cell line.

3.
Luminescence ; 39(5): e4752, 2024 May.
Article in English | MEDLINE | ID: mdl-38697778

ABSTRACT

Prucalopride (PCD), is a modern medication approved by the United States in 2018 to alleviate constipation caused by motility issues. PCD demonstrates a strong affinity and selectivity toward the 5-HT4 receptor. The study here introduces a feasible, direct, non-extractive, and affordable pathway for PCD analytical tracking. The fluorimetric study is based on the on-off effect on the emission amplitude of fluorone-based dye (pyrosin B). In a one-pot experiment, the complex between PCD and pyrosin B is formed instantly in an acidic medium. Correlation between decreased pyrosin B emission and PCD concentrations provides a linear calibration plot from 50 to 900 ng/mL. PCD-dye complex system affecting variables were meticulously tuned. The values of the estimated limit of quantitation and limit of detection for the current methodology were 47.5 and 15.7 ng/mL, respectively. Conformity of the strategy validity was achieved by a comprehensive study of the International Council for Harmonization of Technical Requirements for Pharmaceuticals for Human Use criteria. The method was convincingly applied for PCD assay in tablets and content uniformity investigation. Furthermore, PCD tracking in the spiked biological fluid was applied. Finally, the method uses distilled water as dispersing medium which rise accommodation with the green chemistry principle.


Subject(s)
Benzofurans , Fluorescent Dyes , Benzofurans/chemistry , Benzofurans/analysis , Fluorescent Dyes/chemistry , Humans , Spectrometry, Fluorescence , Molecular Structure , Limit of Detection
4.
Front Public Health ; 12: 1383078, 2024.
Article in English | MEDLINE | ID: mdl-38779421

ABSTRACT

Individuals with disabilities are more vulnerable to depression development than the general population. This study sought to map the evidence on current knowledge of depression, intervention strategies, and assessment tools among people with disabilities. This review was conducted following Arksey and O'Malley's scoping review methodology framework. An electronic search was performed on four English databases: PubMed, Cochrane Library, PsycINFO, and Web of Science. The original search returned 1802 results, with 1,116 from Web of Science, 626 from PubMed, 25 from Cochrane, and 35 from PsycINFO. After removing duplicates, 786 articles were chosen for the title and abstract screening processes. Finally, 112 full-text publications were deemed eligible, with 41 papers being included in this scoping review for analysis. A large proportion (32; 78.04%) of the studies chosen were cross-sectional, 14 (34.14%) of them reported general disability, 12 (29.26%) used a patient health questionnaire (PHQ-9) to measure depression, and 14 (34.14%) had interventions, including cognitive behavioral therapy, psychological counseling, social support, and physical activity. All interventions successfully reduced the severity of the depression. Cognitive behavioral therapies and psychological counseling were widely used interventions that had a significant impact on reducing depression. More randomized controlled trials are required, and they should focus on individuals with specific disabilities to provide disability-specific care that can improve the quality of life for disabled individuals.


Subject(s)
Depression , Disabled Persons , Humans , Disabled Persons/psychology , Social Support , Cognitive Behavioral Therapy
5.
Spectrochim Acta A Mol Biomol Spectrosc ; 319: 124532, 2024 May 25.
Article in English | MEDLINE | ID: mdl-38820815

ABSTRACT

Letrozole is an anticancer medication prescribed for the management of estrogen receptor-positive breast cancer in postmenopausal women. Chronic pain is prevalent in patients receiving chemotherapy, leading to the use of adjuvant analgesics such as tramadol. This work introduces the first analytical approach for the concurrent quantification of letrozole and tramadol, two co-administered drugs, employing a rapid, highly sensitive, eco-friendly, and cost-effective first derivative synchronous spectrofluorimetric technique. The fluorescence of tramadol and letrozole was measured at wavelengths of 235.9 nm and 241.9 nm, respectively using a wavelength difference (Δλ) of 60.0 nm. The developed approach demonstrated exceptional linearity (r ˃ 0.999) within the specified concentration ranges for tramadol (10.0-1200.0 ng/mL) and letrozole (1.0-140.0 ng/mL). The results demonstrated that the proposed technique exhibits a high level of sensitivity, with detection limits of 0.569 and 0.143 ng/mL for tramadol and letrozole, respectively, indicating the good bioanalytical applicability. The within-run precisions, both intra-day and inter-day, for both analytes, were less than 0.71 % RSD. The developed approach was effectively applied to simultaneously estimate the mentioned drugs in their tablets and human plasma samples, achieving high percentage recoveries and low % RSD values. In order to assess the environmental sustainability of the developed approach, Analytical GREEnnessNNESS (AGREE) and the Green Analytical Procedure Index (GAPI) metric tools were employed. Both tools revealed that the developed approach is excellent green, suggesting its usage as an environmentally-friendly alternative for the routine assayof the investigated pharmaceuticals. The developed approach was validated according to the ICHQ2 (R1) requirements.

7.
Spectrochim Acta A Mol Biomol Spectrosc ; 317: 124400, 2024 Sep 05.
Article in English | MEDLINE | ID: mdl-38710139

ABSTRACT

Eletriptan (ETR), a selective pharmaceutical agent agonist of the 5-hydroxytryptamine1 receptor subtype, are primarily used to treat acute migraine attacks. ETR is a triptan-class medication that works by narrowing cerebral blood vessels and reducing chemicals that produce headache pain, light and sound sensitivity, and nausea. Due to its effectiveness in reducing migraine symptoms, it is a worthwhile choice for those looking for quick and efficient treatment. A green, raid, one-pot and straightforward fluorescence spectrometric method was employed to evaluate ETR in tablets and biological samples. By introducing the ETR drug and the fluorescent ligand, Acid red 87, in an acidic buffer, a quenching of the ligand native fluorescent was promptly produced. The quenching action was simply attributed to the selective ion-pair complex generation between the cationic target and the selected ligand. An increase in ETR concentration was linearly proportional to the quenching response in the 50.0 - 500.0 ng/mL range. The optimal configurations for adjusting the system's variable parameters were determined by examining the ETR-Acid red 87 system's response. Additionally, the sensor that was developed met the standards set by the International Council for Harmonisation of Technical Requirements of Pharmaceuticals for Human Use. The sensitivity thresholds of the approach were 13.8 and 42.0 ng/mL for the detection and quantification parameters, respectively, LOD and LOQ. This approach proficiently evaluated the pharmaceutical and biological samples of ETR. Finally, the proposed approach not only simplifies the analysis process but also limits the badimpact on the environment, making it a promising technique for analytical applications.


Subject(s)
Pyrrolidines , Spectrometry, Fluorescence , Tryptamines , Tryptamines/analysis , Tryptamines/blood , Tryptamines/chemistry , Spectrometry, Fluorescence/methods , Humans , Pyrrolidines/chemistry , Green Chemistry Technology/methods , Migraine Disorders/drug therapy , Tablets , Limit of Detection , Hydrogen-Ion Concentration
8.
Saudi Pharm J ; 32(6): 102070, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38645413

ABSTRACT

Cancer is the leading cause of mortality worldwide. In patients with metastatic non-small cell lung cancer, epidermal growth factor receptor (EGFR) is often overexpressed. Gefitinib (GEF), an inhibitor of EGFR, is approved for the treatment of patients with metastatic non-small cell lung cancer (NSCLC). However, the low solubility and dissolution of GEF limits its bioavailability. Numerous methods, including solid dispersion (SD) and complexation, have been reported to enhance the dissolution of poorly soluble drugs. In this study, GEF complexes were prepared using methyl-ß-cyclodextrin (MßCD) and hydroxypropyl-ß-cyclodextrin (HPßCD) in two molar ratios (1:1 and 1:2), furthermore, GEF SDs were prepared using polyvinylpyrrolidone (PVP), polyethylene glycol (PEG), and poloxamer-188(PXM) in three different ratios (1:2, 1:4 and 1:6 w/w). Dissolution studies were conducted on the prepared formulations. Dissolution results showed a 1.22-2.17-fold enhancement in drug dissolution after one hour compared to untreated GEF. Two formulations that showed higher dissolution enhancement were subsequently evaluated for in-vitro cytotoxicity and were formulated into tablets. The selected PVP-GEF (1:4 w/w) and MßCD-GEF (1:1M) formulas displayed improved cytotoxicity compared to untreated GEF. The IC50 values of the PVP-GEF and MßCD-GEF were 4.33 ± 0.66 and 4.84 ± 0.38 µM, respectively which are significantly lower (p < 0.05) than free GEF. In addition, the formulated tablets exhibited enhanced dissolution compared to pure GEF tablets. PVP-GEF SD tablets released (35.1 %±0.4) of GEF after one hour, while GEF-MßCD tablets released (42.2 % ± 0.7) after one hour. In the meantime, tablets containing pure GEF showed only 15 % ± 0.5 release at the same time. The findings of this study offer valuable insights for optimizing the dissolution and hence therapeutic capabilities of GEF while mitigating its limitations.

9.
Mult Scler Relat Disord ; 85: 105558, 2024 May.
Article in English | MEDLINE | ID: mdl-38569381

ABSTRACT

BACKGROUND: Neuro-Behçet's disease (NBD) is defined as primary neurological involvement in patients with systemic symptoms of BD. The variety of clinical presentations seen in NBD and the long list of similar conditions make diagnosis challenging. This retrospective study aimed to estimate the prevalence and describe neurological involvement in patients with Behçet's disease who presented to King Abdulaziz Medical Cities in Jeddah and Riyadh, Saudi Arabia. METHODS: This was a retrospective, cohort study which utilized a non-probability consecutive sampling technique to include all patients diagnosed with NBD patients. All patients with BD (215) were screened for neurological symptoms. Thirty-five patients were found to be diagnosed with NBD. Outcomes were estimated using the modified Rankin scale (mRS). RESULTS: In our cohort, one in six patients with BD was diagnosed with NBD. A total of 35 patients were diagnosed with NBD (mean age 27.56 ± 10.36 years; [2.88:1; Male: Female]). The main clinical features of NBD were headaches, weakness, unsteadiness, and dysarthria. The most commonly involved sites on imaging were the brainstem, diencephalon, cerebellum and basal ganglia. Oligocolonal bands were negative in all patients. Maintenance therapy most commonly included oral corticosteroids, azathioprine, and/or infliximab. Most patients received pulse corticosteroids alone when presenting with acute relapse. Half of our cohort was asymptomatic and three in four had favorable outcomes. CONCLUSION: NBD is common among patients with BD in our population with most patients having favorable outcomes. Patients might have a wide array of symptoms which might make the diagnosis challenging.


Subject(s)
Behcet Syndrome , Humans , Behcet Syndrome/epidemiology , Behcet Syndrome/diagnostic imaging , Behcet Syndrome/complications , Male , Female , Saudi Arabia/epidemiology , Adult , Retrospective Studies , Prevalence , Young Adult , Adolescent , Magnetic Resonance Imaging
10.
J Infect Public Health ; 17(6): 1013-1022, 2024 Jun.
Article in English | MEDLINE | ID: mdl-38636312

ABSTRACT

BACKGROUND: Disability is a serious health issue that can have a significant impact on both physical and mental health. This study attempted to investigate the relationship between depression, quality of life (QOL), and COVID-19 challenges faced by people with disabilities (PwD) from Saudi Arabia. METHODS: A structured interview questionnaire to measure QOL (WHOQOL-BREF) and depression (PHQ-9) was used to conduct a cross-sectional study among PwDs in Saudi Arabia. Binary regression analysis was done using SPSS-IBM and predictors for depression, quality of life and COVID-19 challenges were determined. RESULTS: Of the 111 study samples, two-thirds were male (67.6%), with only one-third employed (34.2%). Most of them (70%) reported moderate to severe disability-related difficulties. Only 28.8% of the samples were satisfied with the physical health domain of the quality of life, whereas 31.5%, 44.1%, and 50.5% were satisfied with the psychological, social, and environmental health domains, respectively. Approximately 62% of the participants had been diagnosed with depression. A significantly higher percentage of participants who had not received COVID-19 vaccination were depressed (P = 0.011), whereas the depression rate was lower among those who received three or four doses of vaccination (P = 0.006). Depression is 4.1 times more likely in people with comorbidities, and disability with increased difficulty (OR: 4.266). Furthermore, vaccinated people had a 5.3-fold higher chance of developing satisfactory QOL. CONCLUSION: Regardless of the type, cause, or duration of disability, the degree of difficulty is a strong predictor of depression and a decrease in quality of life. A multidisciplinary approach is needed to improve the well-being of people with disabilities.


Subject(s)
COVID-19 , Depression , Disabled Persons , Quality of Life , Humans , Quality of Life/psychology , Saudi Arabia/epidemiology , Male , COVID-19/psychology , COVID-19/epidemiology , Female , Cross-Sectional Studies , Disabled Persons/psychology , Disabled Persons/statistics & numerical data , Adult , Depression/epidemiology , Middle Aged , Surveys and Questionnaires , Young Adult , SARS-CoV-2 , Aged , Adolescent
11.
Spectrochim Acta A Mol Biomol Spectrosc ; 313: 124107, 2024 May 15.
Article in English | MEDLINE | ID: mdl-38452459

ABSTRACT

The proposed research adheres to a certain methodology to ensure that the technique used for analyzing the centrophenoxine drug is sustainable and green. It is important to highlight that several tools that have been recently developed were utilized as potential indicators of environmental sustainability and applicability. The present research presents a novel and entirely innovative method utilizing ultrasensitive spectrofluorimetry for the detection of centrophenoxine (CPX) drug. The employed methodology in this study involved the utilization of one-step, one-pot, and direct spectrofluorimetric technique, which was found to be both efficient and environmentally sustainable in the validation and assessment of the drug. Simply, when CPX and erythrosine B reagent were combined in an acidic environment, the highly resonance Rayleigh scattering product was immediately produced. The sensitivity limits were observed to be within the range of 15-47 ng mL-1, whereas the linearity was assessed to be in the range of 50-2000 ng mL-1. The optimal settings for all modifiable parameters of the system were ascertained through an analysis of centrophenoxine-erythrosine B complexes. Moreover, the system demonstrated compliance with International Council for Harmonization (ICH) specifications without encountering any issues. The suggested process was then rated on different recent environmental safety measuring metrics to see how good it was for the environment. Fortunately, the WAC standards that combine ecological and functional elements utilizing the Green/Red/Blue (RGB 12) design also acclaimed the current analytical technique as a white one. Additionally, a new applicability evaluation tool (BAGI) was employed to estimate the practicability of the planned method in the analytical chemistry field.


Subject(s)
Erythrosine , Nootropic Agents , Erythrosine/chemistry , Meclofenoxate , Antioxidants , Scattering, Radiation , Spectrometry, Fluorescence/methods
12.
Spectrochim Acta A Mol Biomol Spectrosc ; 313: 124168, 2024 May 15.
Article in English | MEDLINE | ID: mdl-38513420

ABSTRACT

A typical drug used to treat Parkinson's disease is called rasagiline. It belongs to an assortment of drugs known as monoamine oxidase inhibitors, which function by raising dopamine levels in the brain. This work created a unique spectrofluorimetric method for the analytical assay of rasagiline for the first time. The approach utilized the synergistic utility of the fluorogenic properties of benzofurazan and salting-out assisted liquid-liquid extraction. By combining these techniques an ultrasensitive, and highly selective methodology for the assay of rasagiline was established. Measurements were made of the resultant yellow fluorescent product at 533 nm by applying an excitation wavelength of 475.3 nm. The calibration graph was examined to assess its linearity across a range of 30-600 ng/ml. Through estimation, the limit of detection was discovered to be 8.9 ng/ml, while the quantitation limit was estimated to be 27 ng/ml. All relevant parameters influencing the fulfillment of the developed method were thoroughly examined and tuned. Following the directives set by the (ICH) the suggested approach was confirmed and demonstrated its capability for the accurate determination of rasagiline in tablets, as well as for testing content uniformity. The incorporation of salting-out assisted liquid-liquid extraction technology enables effective tracking of rasagiline in plasma samples, providing a novel and innovative approach for its analysis in biological matrices.


Subject(s)
4-Chloro-7-nitrobenzofurazan , Monoamine Oxidase Inhibitors , Sodium Chloride , Monoamine Oxidase Inhibitors/pharmacology , Monoamine Oxidase Inhibitors/therapeutic use , Indans , Liquid-Liquid Extraction/methods
13.
Int J Biol Macromol ; 264(Pt 2): 130634, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38460624

ABSTRACT

The nature of nano molecules as a self-assembled nanocomposite surface depends on the nanoparticles of sodium butyrate, cellulose, and pycnogenol; the synthesis is achieved via precipitation and grinding methods. The excellent functionalized surface of nanocomposite (NCP) enables the loading of the selected drugs, where the efficiency of the NCP surface arrived at 92.2 %. The electrochemical behavior emphasized the success of a functionalized NCP surface for incorporation with drugs for the drug delivery system, the results of cytotoxicity detect the effect of NCP on the mouse normal liver (BNL) cells, where the high and low concentrations on the BNL cells have a safe dose. Cell viability with BNL cells was reported at 101.8 % with10 µL and 100.12 % with 100 µL, the interaction between the NCP and the human serum albumin (HSA) at room temperature. The low interaction rate with the glutamate and increased binding with the oxidized glutathione disulfide (GSSG) and reduced glutathione (SGH) reflect the antioxidant activity of NCP. The strong binding of NCP with biomolecules such as glucose is referred to as the biosensor property. The results recommend that NCP is an excellent nanocarrier for drug delivery and glucose biosensors for diabetes.


Subject(s)
Biosensing Techniques , Nanocomposites , Humans , Animals , Mice , Glucose , Antioxidants/pharmacology , Glutathione , Nanocomposites/chemistry , Glutathione Disulfide , Biosensing Techniques/methods
14.
Environ Sci Pollut Res Int ; 31(18): 26452-26479, 2024 Apr.
Article in English | MEDLINE | ID: mdl-38546921

ABSTRACT

The advanced oxidation process (AOP) is an efficient method to treat recalcitrance pollutants such as pharmaceutical compounds. The essential physicochemical factors in AOP experiments significantly influence the efficiency, speed, cost, and safety of byproducts of the treatment process. In this review, we collected recent articles that investigated the elimination of pharmaceutical compounds by various AOP systems in a water medium, and then we provide an overview of AOP systems, the formation mechanisms of active radicals or reactive oxygen species (ROS), and their detection methods. Then, we discussed the role of the main physicochemical parameters (pH, chemical interference, temperature, catalyst, pollutant concentration, and oxidant concentration) in a critical way. We gained insight into the most frequent scenarios for the proper and improper physicochemical parameters for the degradation of pharmaceutical compounds. Also, we mentioned the main factors that restrict the application of AOP systems in a commercial way. We demonstrated that a proper adjustment of AOP experimental parameters resulted in promoting the treatment performance, decreasing the treatment cost and the treatment operation time, increasing the safeness of the system products, and improving the reaction stoichiometric efficiency. The outcomes of this review will be beneficial for future AOP applicants to improve the pharmaceutical compound treatment by providing a deeper understanding of the role of the parameters. In addition, the proper application of physicochemical parameters in AOP systems acts to track the sustainable development goals (SDGs).


Subject(s)
Oxidation-Reduction , Pharmaceutical Preparations/chemistry , Reactive Oxygen Species , Water Pollutants, Chemical/chemistry
15.
ACS Omega ; 9(3): 3980-3987, 2024 Jan 23.
Article in English | MEDLINE | ID: mdl-38284045

ABSTRACT

Keeping in mind the health scenario in Kingdom of Saudi Arabia with respect to vitamin D3 (VD3) deficiency and its significant role in calcium homeostasis and human metabolism, this research is exploring the combination of eggshell (as a source of calcium) and VD3 as a very economical solution for this problem. Eggshells from local restaurant were collected, washed, ground, sieved, and characterized by Fourier transforms infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and Brunauer-Emmett-Teller (BET) techniques. The results of FTIR, SEM, DSC, XRD, and BET indicate that eggshell powder (ESP) was properly processed. Directly compressed tablets containing 2.5 mg of VD3 (equivalent to 50,000 IU), that are based on the use of ESP as tablet filler, were manufactured based on mixing Avicel PH 101 with ESP in different ratios (9:1, 1:1, and 1:9) in addition to the use of both Avicel PH 101 and ESP alone as tablet filler. Tablets properties were evaluated according to USP30-NF25 pharmacopoeia tests in terms of weight variation test, drug content uniformity, tablet hardness, tablet friability, tablet disintegration, and in vitro dissolution profile. The VD3 contents were found to be 98.77-102.35% in all formulations. After 90 min of study, all formulations showed in vitro drug release content in the range of 99.29-101.05%. All of the tested parameters of ESP tablets were similar to those of commercial Avicel PH 101. All of the tested properties of tablets with ESP as a filler were found to be within the acceptable limits of the pharmacopeia recommendations. Therefore, ESP could be exploited for its use as a filler in direct compression tablets.

16.
Heliyon ; 10(1): e23221, 2024 Jan 15.
Article in English | MEDLINE | ID: mdl-38163135

ABSTRACT

Silymarin (SL) is a water-insoluble flavonoid used in the treatment of different diseases, but its therapeutic activity is limited due to its low solubility. So, in the present study, SL solid dispersions (SDs) were developed using different carriers like Kollidone VA64 (KL), Soluplus (SP), and Poloxamer 188 (PL) by solvent evaporation (SE), microwave irradiation (MI), and freeze-drying (FD) methods. The phase solubility and saturation solubility studies were assessed to estimate the stability constant as well as the carrier effect. The dissolution studies were performed for prepared SL-SDs (binary and ternary) to select the optimum SL-SDs. The selected SL-SDs (F5, F9) were further characterized for infrared spectroscopy (IR), nuclear magnetic resonance (NMR), differential scanning calorimeter (DSC), scanning electron microscope (SEM), and X-ray diffraction (XRD). Finally, the comparative cell viability assay (lung cancer cell line) was performed to evaluate the change in activity after the formulation of SDs. The phase solubility and solubility study results displayed marked enhancements in solubility. The dissolution study findings showed significant enhancement in drug release from ternary solid dispersions (F7-F9) > ternary physical mixture (PM3) > binary solid dispersions (F1-F6) > binary physical mixture (PM1, PM2) in comparison to free SL. A greater release was observed from ternary SDs due to the addition of PL in the formulation, which had a synergistic effect on increasing the solubility. IR and NMR spectra revealed no chemical interaction between SL, KL, and PL. DSC, XRD, and SEM all confirmed the transformation of crystalline SL into amorphous SL. The cell viability assay demonstrated significantly enhanced results from ternary solid dispersion (F9) compared to free SL. Based on the study results, it can be said that SL-SDs are an alternative way to deliver drugs orally that can improve solubility and have anti-cancer activity.

17.
AAPS PharmSciTech ; 25(1): 18, 2024 Jan 23.
Article in English | MEDLINE | ID: mdl-38263347

ABSTRACT

Due to tenoxicam (TX)'s poor aqueous solubility (0.072 mg/ml), it is poorly absorbable in the GIT, and the long-term oral administration of TX may cause severe GIT disturbances. Topical administration of TX can help in bypassing the GIT adverse effects. Therefore, in the present work, we constructed different pluronic/lecithin organogels (PLOs) for topical delivery of TX. PLO was constructed simply via direct mixing of an aqueous pluronic solution with lecithin solution. The prepared PLO formulations were characterized for their physicochemical properties including pH, drug content, visual inspection, viscosity, and spreadability. Also, the in vitro release and kinetic studies were carried out to investigate the mechanism of drug release. Moreover, the in vivo studies were carried out by investigating the anti-inflammatory and analgesic activities using albino male rats. The results showed that the modified PLOs have good physicochemical properties. The viscosity of the modified gels is a direct proportionality with both lecithin and pluronic concentrations. Also, subsequently, the drug release rate is directly proportional to gel viscosity. Moreover, the in vivo studies showed that the modified PLOs (F19) showed a significant ( < 0.05%) paw edema inhibition and pain analgesia compared with other investigated groups. Also, the results indicated that the increase in dose is accompanied by higher activity and a longer duration of action which extended to 12 h. Hence, the modified PLOs are promising safe candidates or vehicles for effective TX loading with sustained delivery behavior.


Subject(s)
Lecithins , Piroxicam/analogs & derivatives , Poloxamer , Animals , Rats , Kinetics , Inflammation , Pain
18.
Spectrochim Acta A Mol Biomol Spectrosc ; 308: 123744, 2024 Mar 05.
Article in English | MEDLINE | ID: mdl-38157690

ABSTRACT

This study introduces the first and unique Molecular-mass-Related Fluorescence Sensor as the first fluorimetric strategy for determining amlodipine. An environmentally friendly, single-step, and direct spectrofluorimetric approach was utilized to evaluate the analyte. In an acidic setting, combining the amlodipine medication and the fluorescent dye Cilefa Pink B generated an instantaneous ultra-fluorescent product. An increase in dye response after adding amlodipine was proportional to the molecular weight of the generated complex, as measured at 329 nm. was the idea ofthe applied fluorimetric analysis. The complexing process increased the molecular mass from 879.86 to 1288.739 g mol-1. The medication's range of 0.050-1.00 µg mL-1 is directly correlated with this molecular massenlargement. The ideal settings for the changeable parameters of the system were established through an analysis of the response of the amlodipine-Cilefa Pink B system. Furthermore, the developed sensor complied with ICH (International Council for Harmonization) standards. The sensitivity limits were 0.0139 µg mL-1 (for the detection limit, LOD) and 0.042 µg mL-1 (for the quantification limit, LOQ). Additionally, this method effectively recovered the drug in its original and therapeutic dosage forms. Finally, the proposed process's environmental impact was also assessed through different modern greenness evaluation tools.


Subject(s)
Amlodipine , Amlodipine/analysis , Molecular Weight , Spectrometry, Fluorescence/methods , Tablets/chemistry , Fluorometry
19.
Molecules ; 28(23)2023 Nov 27.
Article in English | MEDLINE | ID: mdl-38067534

ABSTRACT

Cabozantinib malate (CBZM), a new anticancer medication, has been studied for its solubility and thermodynamic properties in a variety of {dimethyl sulfoxide (DMSO) + water (H2O)} mixtures at 298.2-318.2 K and 101.1 kPa. Using the shake flask technique, the solubility of CBZM was assessed and the results were correlated to the van't Hoff, Apelblat, Buchowski-Ksiazczak λh, Yalkowsky-Roseman, Jouyban-Acree, and Jouyban-Acree-van't Hoff models. There was a significant correlation between the experimental CBZM solubility data and all computational models, as evidenced by the error values for all computational models being less than 5.0%. Temperature and DMSO mass percentage improved the CBZM mole fraction solubility in the cosolvent solutions of {DMSO + H2O}. At 318.2 K, pure DMSO had the highest mole fraction solubility of CBZM (4.38 × 10-2), whereas pure H2O had the lowest mole fraction solubility (2.24 × 10-7 at 298.2 K). The positive values of computed thermodynamic parameters indicated that the dissolution of CBZM was endothermic and entropy-driven in all of the {DMSO + H2O} solutions investigated. It was found that the CBZM solvation in {DMSO + H2O} solutions is governed by enthalpy. When compared to CBZM-H2O, CBZM-DMSO showed the highest molecular interactions. The findings of this investigation demonstrated that DMSO has a great deal of potential for CBZM solubilization in H2O.

20.
Luminescence ; 2023 Dec 03.
Article in English | MEDLINE | ID: mdl-38044037

ABSTRACT

In this study, the simultaneous determination of bilastine and montelukast, two recently approved co-formulated antihistaminic medications, was accomplished using a quick, sensitive, environmentally friendly, and reasonably priced synchronous fluorescence spectroscopic approach for the first time. Enhancement of the method's sensitivity down to nanogram levels was achieved by the addition of sodium dodecyl sulfate (1.0% w/v) as a micellar system. According to the results, bilastine and montelukast's fluorescence was measured at 255.3 and 355.3 nm, respectively, using Δλ of 40.0 nm and distilled water as a green diluting solvent. With respect to the concentration ranges of bilastine (5.0-300.0 ng/ml) and montelukast (50.0-1000.0 ng/ml), the method showed excellent linearity (r ≥ 0.9998). The results showed that the suggested method is highly sensitive, with detection limits of 1.42 and 13.74 ng/ml for bilastine and montelukast, respectively. Within-run precisions (intra- and interday) per cent relative standard deviations (RSD) for both analytes were <0.59%. With high percentage recoveries and low percentage RSD values, the designed approach was successfully applied for the simultaneous estimation of the cited medications in their dosage form and human plasma samples. To evaluate the green profile of the suggested method, an analytical GREENNESS metric approach (AGREE) and green analytical procedure index (GAPI) metric tools were used. These two methods for evaluating greenness confirmed that the developed method met the highest number of green requirements, recommending its use as a green substitute for the routine analysis of the studied drugs. The proposed approach was validated according to ICHQ2 (R1) guidelines.

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