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2.
J Cancer Res Clin Oncol ; 150(4): 212, 2024 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-38662247

RESUMEN

BACKGROUND AND AIM: Morinda citrifolia fruit juice (noni) is an herbal remedy documented to have antioxidant properties. It has been suggested that prevention of carcinogen-DNA adduct formation and the antioxidant activity of NJ may contribute to the cancer preventive effect. In the present study, the antitumor activity of noni was investigated in the presence of cyclophosphamide (CYL) in vitro and in vivo. METHODS: In vitro breast cancer cells (MDA-MB-468) were used to measure the percentage of inhibition and the IC50. The in vivo antitumor activity of noni was studied by monitoring the mean survival time (MST), percentage increase in life span (%ILS), viable and non-viable cell count, tumor volume, body weight, and hematological and serum biochemical parameters in mice. Treatment with noni and CYL exhibited dose- and time-dependent cytotoxicity toward breast cancer cells. RESULTS: Individual treatment of noni and CYL exhibited dose- and time-dependent cytotoxicity on breast cancer cell lines, while in combination therapy of noni and CYL, noni enhances cytotoxic effect of CYL at 48 h than that at 24 h. Similar result was found in in vivo studies, the results of which revealed that alone treatment of CYL and noni suppressed tumor growth. However, combination treatment with CYL and noni presented better tumor inhibition than that of alone treatment of CYL and noni. On the contrary, CYL alone drastically attenuated hematological parameters, i.e., RBC, WBC, and Hb compared to normal and control groups, and this change was reversed and normalized by noni when given as combination therapy with CYL. Moreover, the levels of serum biochemical markers, i.e., AST, ALP, and ALT, were significantly increased in the control and CYL-treated groups than those in the normal group. In the combination treatment of noni and CYL, the above biochemical marker levels significantly decreased compared to CYL alone-treated group. CONCLUSIONS: The present study suggested that CYL treatment can cause serious myelotoxicity and hepatic injury in cancer patients. In conclusion, the combined use of noni with CYL potentially enhances the antitumor activity of CYL and suppresses myelotoxicity and hepatotoxicity induced by CYL in tumor-bearing mice.


Asunto(s)
Neoplasias de la Mama , Ciclofosfamida , Morinda , Animales , Ciclofosfamida/farmacología , Ciclofosfamida/efectos adversos , Ratones , Humanos , Femenino , Morinda/química , Neoplasias de la Mama/tratamiento farmacológico , Neoplasias de la Mama/patología , Línea Celular Tumoral , Jugos de Frutas y Vegetales , Ensayos Antitumor por Modelo de Xenoinjerto , Sinergismo Farmacológico , Extractos Vegetales/farmacología , Protocolos de Quimioterapia Combinada Antineoplásica/farmacología , Antineoplásicos Alquilantes/farmacología , Antineoplásicos Alquilantes/efectos adversos , Ratones Endogámicos BALB C , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Enfermedad Hepática Inducida por Sustancias y Drogas/etiología
3.
Environ Sci Pollut Res Int ; 31(18): 26452-26479, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38546921

RESUMEN

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).


Asunto(s)
Oxidación-Reducción , Preparaciones Farmacéuticas/química , Especies Reactivas de Oxígeno , Contaminantes Químicos del Agua/química
4.
J Pharm Health Care Sci ; 10(1): 7, 2024 Jan 24.
Artículo en Inglés | MEDLINE | ID: mdl-38268049

RESUMEN

BACKGROUND: Multidrug-resistant bacterial strains cause several serious infections that can be fatal, such as Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumonia, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacteriaceae (often referred to as ESKAPE pathogens). Since ancient times, several indigenous medical systems in India have utilized diverse medicinal plants (approximately 80,000 species) as conventional treatments for a variety of illnesses. A member of the Fabaceae family, also referred to as "Himalayan indigo," Indigofera heterantha Wall, is well known for its therapeutic properties. METHODS: The present study investigated the antibacterial, antifungal and antihelmintic properties of the roots, bark, leaves, and flowers of I. heterantha from the Kashmir Himalayas. The effectiveness of the extracts against bacteria, fungi, and earthworms. Three of the tested organisms for bacteria were ESKAPE pathogens, as they are responsible for creating fatal bacterial infections. The antifungal potency of I. heterantha aqueous and methanolic extracts was evaluated using the Agar Well Diffusion Assay. The antihelmintic activity was carried out on an adult Pheretima posthuma Indian earth worm, which shares physiological and anatomical similarities with human intestinal roundworm parasites. RESULTS: The methanolic extracts of root and bark have shown prominent activity against all bacterial strains, whereas aqueous extracts of flower, root, and leaves have shown promising activity against Staphylococcus aureus. The aqueous extract demonstrated good activity against S. cerevisiae at a concentration of 200 mg/ml with a zone of inhibition of 16 mm, while the methanolic extract displayed comparable activity against the fungal strains. The remaining two strains, P. crysogenum and A. fumigatus, were only moderately active in response to the extracts. All the extracts have shown anthelmintic activity except aqueous flower. CONCLUSION: These results will pave the way for the bioassay-guided isolation of bioactive constituents that may act as hits for further development as potential antibacterial agents against drug-resistant microbial and helminthic infections.

5.
ACS Omega ; 9(3): 3980-3987, 2024 Jan 23.
Artículo en Inglés | MEDLINE | ID: mdl-38284045

RESUMEN

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.

6.
Molecules ; 28(23)2023 Nov 27.
Artículo en Inglés | MEDLINE | ID: mdl-38067534

RESUMEN

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.

7.
Brain Sci ; 13(12)2023 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-38137115

RESUMEN

Depression is a low-energy condition that has an impact on a person's thoughts, actions, propensities, emotional state, and sense of wellbeing. According to the World Health Organization (WHO), 5% of adults are depressed. Individuals who are depressed are commonly prescribed antidepressants, and sometimes, individuals may have other psychiatric conditions that share overlapping symptoms with depression. These cooccurring conditions can complicate the diagnostic process, leading to a misdiagnosis and the prescription of antidepressants. Capsaicin (CAP) is a known antidepressant. Hence, this study aimed to assess the antidepressant activity of CAP nanoemulsion in nicotine (NC) withdrawal-induced depression in mice. Mice treated with CAP (3 mg/kg) showed reduced immobility in the forced swimming test (FST), tail-suspension test (TST), and open field test (OFT). During the OFT, the animals treated with nanoemulsion (CAP 3 mg/kg) spent less time in the corners than the control animals. Biochemical parameters, such as superoxide dismutase (SOD) and glutathione (GSH), were observed in reduced quantities in the NC withdrawal model (NWM), where they were slightly increased in the high-dose nanoemulsion (CAP 3 mg/kg) compared to the low-dose nanoemulsion (CAP 1 mg/kg). These results suggest that CAP caused antidepressant activity in the NWM via the nanoemulsion.

8.
ACS Omega ; 8(44): 41755-41764, 2023 Nov 07.
Artículo en Inglés | MEDLINE | ID: mdl-37970055

RESUMEN

A nanoemulsion-based polyherbal mouthwash (PHFX) of Curcuma longa hydroalcoholic extract was developed and evaluated for its antibacterial effects against a variety of Gram-positive and Gram-negative oral pathogens in comparison to standard chlorhexidine acetate (CHD-A) (positive control). Various nanoemulsion-based mouthwashes of C. longa extract were produced using an aqueous phase titration approach via construction of pseudoternary phase diagrams. The developed nanoemulsion-based PHFX was studied for thermodynamic stability tests. Selected formulations (PHFX1-PHFX5) were characterized physicochemically for droplet diameter, polydispersity index (PDI), refractive index (RI), transmittance, and pH. The drug release studies were performed using the dialysis method. Based on the minimum droplet diameter (26.34 nm), least PDI (0.132), optimal RI (1.337), maximum %T (99.13), optimal pH (6.45), and maximum cumulative drug release (98.2%), formulation PHFX1 (containing 0.5% w/w of C. longa extract, 1.5% w/w of clove oil, 7.0% w/w of Tween-80, 7.0% w/w of Transcutol-HP, and 84.0% w/w of water) was selected for antimicrobial studies in comparison to standard CHD-A. The antibacterial effects and minimum inhibitory concentration were studied against various Gram-positive oral pathogens such as Streptococcus mutans, Staphylococcus aureus, Streptococcus pneumoniae, and Bacillus subtilis and Gram-negative oral pathogens such as Escherichia coli and Klebsiella pneumoniae. The antibacterial effects of PHFX1 were found to be significant over standard CHD-A against most Gram-positive and Gram-negative oral pathogens. The antimicrobial studies showed that the formulation PHFX1 was effective against all oral pathogens even at 3- to 4-fold lower working concentrations. These findings indicated the potential of nanoemulsion-based mouthwash in the treatment of a variety of oral pathogen infections.

9.
Molecules ; 28(20)2023 Oct 16.
Artículo en Inglés | MEDLINE | ID: mdl-37894589

RESUMEN

The solubility and solution thermodynamics of isotretinoin (ITN) (3) in numerous {dimethyl sulfoxide (DMSO) (1) + water (H2O) (2)} combinations were studied at 298.2-318.2 K under fixed atmospheric pressure of 101.1 kPa. A shake flask methodology was used to determine ITN solubility, and correlations were made using the "van't Hoff, Apelblat, Buchowski-Ksiazczak λh, Yalkowsky-Roseman, Jouyban-Acree, and Jouyban-Acree-van't Hoff models". In mixtures of {(DMSO (1) + H2O (2)}, the solubility of ITN in mole fractions was enhanced with the temperature and DMSO mass fraction. The mole fraction solubility of ITN was highest in neat DMSO (1.02 × 10-1 at 318.2 K) and lowest in pure H2O (3.14 × 10-7 at 298.2 K). The output of computational models revealed good relationships between the solubility data from the experiments. The dissolution of ITN was "endothermic and entropy-driven" in all of the {(DMSO (1) + H2O (2)} mixtures examined, according to the positive values of measured thermodynamic parameters. Enthalpy was discovered to be the driving force behind ITN solvation in {(DMSO (1) + H2O (2)} combinations. ITN-DMSO displayed the highest molecular interactions when compared to ITN-H2O. The outcomes of this study suggest that DMSO has a great potential for solubilizing ITN in H2O.

10.
ACS Omega ; 8(42): 39936-39944, 2023 Oct 24.
Artículo en Inglés | MEDLINE | ID: mdl-37901554

RESUMEN

There is a dearth of information in the literature regarding environmentally benign high-performance thin-layer chromatography (HPTLC) methods to determine tenoxicam (TNX). Therefore, designing and validating an HPTLC method to detect TNX in commercial tablets and capsules was the goal of this investigation. The green mobile phase utilized was the combination of ethanol/water/ammonia solution (50:45:5 v/v/v). The TNX was quantified at a wavelength of 375 nm. The proposed method's greenness profile was established using the Analytical GREEnness (AGREE) approach. The proposed methodology for determining TNX was linear in the range of 25-1400 ng/band. The proposed methodology for measuring TNX was accurate (% recoveries = 98.24-101.48), precise (% RSD = 0.87-1.02), robust (% RSD = 0.87-0.94), sensitive (LOD = 0.98 ng/band and LOQ = 2.94 ng/band), and environmentally friendly. The AGREE scale for the present methodology was derived to be 0.75, indicating an outstanding greenness profile. TNX was found to be highly stable under acidic, base, and thermal stress conditions. However, it completely decomposed under oxidative stress conditions. Commercial tablets and capsules were found to have 98.46 and 101.24% TNX, respectively. This finding supports the validity of the current methodology for measuring TNX in commercial formulations. The outcomes of this work showed that the proposed eco-friendly HPTLC methodology can be used for the routine analysis of TNX in commercial formulations.

11.
ACS Omega ; 8(42): 39928-39935, 2023 Oct 24.
Artículo en Inglés | MEDLINE | ID: mdl-37901579

RESUMEN

Suvorexant (SUV) is a new sedative/hypnotic medicine that is recommended to treat insomnia. It is an important medicine from a forensic point of view due to its sedative/hypnotic and depressant effects. To the best of our knowledge, high-performance thin-layer chromatography (HPTLC) bioanalytical methods have not been published to measure SUV in human urine and pharmaceutical samples. Accordingly, this study was designed and validated a sensitive and rapid bioanalytical HPTLC method to determine SUV in human urine samples for the very first time. The densitometric measurement of SUV and the internal standard (IS; sildenafil) was performed on glass-coated silica gel normal-phase-60F254S TLC plates using a mixture of chloroform and methanol (97.5:2.5 v/v) as the eluent system. Both the SUV and IS were detected at a wavelength of 254 nm. Both analytes were extracted using the protein precipitation technique utilizing methanol as the solvent. For the IS and SUV, the Rf values were 0.09 and 0.45, respectively. The proposed bioanalytical method for SUV was linear in the 50-1600 ng/band range. The current bioanalytical technique was linear, precise (% RSD = 3.28-4.20), accurate (% recovery = 97.58-103.80), robust (% recovery = 95.31-102.34 and % RSD = 2.81-3.15), rapid, and sensitive (LOD = 3.73 ng/band and LOQ = 11.20 ng/band). These findings suggested that the current bioanalytical method can be regularly used to determine SUV in wide varieties of urine samples.

12.
Heliyon ; 9(8): e18405, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-37576265

RESUMEN

In this study, an environmentally friendly "high-performance liquid chromatography (HPLC)" assay to quantify isotretinoin (ITN) in commercial products and solubility samples is designed and verified. A Nucleodur reverse-phase C18 column was used as the stationary phase to identify ITN. The ecologically friendly mobile phase was composed of ethyl acetate and ethanol (50:50 v/v), and it was delivered at a flow rate of 1.0 mL/min. ITN was measured at 354 nm in wavelength. The current HPLC method had a determination coefficient of 0.9994 and was linear in the 0.2-80 µg/g range. The current protocol for ITN measurement was also rapid (retention time = 2.78 min), accurate (%recoveries = 98.60-101.52), precise (% uncertainties = 0.71-0.98), and sensitive. According to the AGREE methodology, the current procedure received an outstanding greenness profile with an AGREE score of 0.76. By determining ITN in commercial products and solubility samples, the applicability of the current approach was proven. ITN was discovered to be present in 98.43% and 100.84%, respectively, of commercial capsule brands A and B. The ITN's solubility in numerous eco-friendly solvents was successfully measured. Under different stress conditions, the current approach was able to distinguish between its degradation products, demonstrating its stability-indicating characteristics. These findings indicated that ITN in procured capsules and solubility samples might be regularly tested by the suggested approach.

13.
ACS Omega ; 8(33): 30655-30664, 2023 Aug 22.
Artículo en Inglés | MEDLINE | ID: mdl-37636909

RESUMEN

High-performance thin-layer chromatographic (HPTLC) assays for pomalidomide (PMD) measurement are lacking in the published database. Furthermore, eco-friendly stability-indicating analytical assays for PMD measurement are also lacking in the published database. In order to detect PMD in commercial products more accurately and sustainably than the conventional normal-phase HPTLC (NP-HPTLC) assay, an effort was made to design and verify a sensitive and eco-friendly reversed-phase HPTLC (RP-HPTLC) assay. The silica gel 60 NP-18F254S and 60 RP-18F254S plates were used as the stationary phases for NP-HPTLC and RP-HPTLC methods, respectively. The solvent system for NP-HPTLC was chloroform-methanol (90:10 v/v). However, the solvent system for RP-HPTLC was ethanol-water (75:25 v/v). The greenness scores for both assays were measured by AGREE approach. PMD measurement was performed for both assays at 372 nm. In the 50-600 and 20-1000 ng/band ranges, the NP-HPTLC and RP-HPTLC methods were linear for PMD measurement. The RP-HPTLC assay was superior to the NP-HPTLC method for measuring PMD in terms of sensitivity, accuracy, precision, and robustness. The ability of both methods to identify PMD in the presence of its degradation products suggests that both methods have stability-indicating features. When employing the NP-HPTLC and RP-HPTLC assays, respectively, the assay for PMD in commercial capsules was 88.68 and 98.83%. The AGREE scores for NP-HPTLC and RP-HPTLC assays were calculated to be 0.44 and 0.82, respectively, suggesting an outstanding greenness characteristic of the RP-HPTLC method than the NP-HPTLC method. The RP-HPTLC method was found to be superior to the NP-HPTLC method based on these findings. Therefore, the RP-HPTLC method could be successfully applied for the determination of PMD in pharmaceutical products.

14.
Molecules ; 28(15)2023 Aug 03.
Artículo en Inglés | MEDLINE | ID: mdl-37570832

RESUMEN

This article sheds light on the various scaffolds that can be used in the designing and development of novel synthetic compounds to create DPP-4 inhibitors for the treatment of type 2 diabetes mellitus (T2DM). This review highlights a variety of scaffolds with high DPP-4 inhibition activity, such as pyrazolopyrimidine, tetrahydro pyridopyrimidine, uracil-based benzoic acid and esters, triazole-based, fluorophenyl-based, glycinamide, glycolamide, ß-carbonyl 1,2,4-triazole, and quinazoline motifs. The article further explains that the potential of the compounds can be increased by substituting atoms such as fluorine, chlorine, and bromine. Docking of existing drugs like sitagliptin, saxagliptin, and vildagliptin was done using Maestro 12.5, and the interaction with specific residues was studied to gain a better understanding of the active sites of DPP-4. The structural activities of the various scaffolds against DPP-4 were further illustrated by their inhibitory concentration (IC50) values. Additionally, various synthesis schemes were developed to make several commercially available DPP4 inhibitors such as vildagliptin, sitagliptin and omarigliptin. In conclusion, the use of halogenated scaffolds for the development of DPP-4 inhibitors is likely to be an area of increasing interest in the future.


Asunto(s)
Diabetes Mellitus Tipo 2 , Inhibidores de la Dipeptidil-Peptidasa IV , Humanos , Inhibidores de la Dipeptidil-Peptidasa IV/química , Hipoglucemiantes/química , Vildagliptina , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Fosfato de Sitagliptina , Relación Estructura-Actividad
15.
Int J Biol Macromol ; 248: 125875, 2023 Sep 01.
Artículo en Inglés | MEDLINE | ID: mdl-37473899

RESUMEN

Natural polymers, like chitosan and alginate have potential of appearance, as well as the changes and handling necessary to make it acceptable vehicle for the controlled release of medicines and biomolecules. Microcapsules are characterized as micrometer-sized particulate that can be employed to store chemicals within them. In the present review, we have discussed various advantages, components of microcapsules, release mechanisms, preparation methods, and their applications in drug delivery systems. The preparation methods exhibited strong encapsulation effectiveness and may be used in a wide range of pharmaceutical and biomedical applications. The major advantages of using the microencapsulation technique are, sustained and controlled delivery of drugs, drug targeting, improvement of shelf life, stabilization, immobilization of enzymes and microorganisms. As new biomaterials are developed for the body, they are better suited to the development of pharmaceutical systems than traditional pharmaceuticals because they are more reliable, biocompatible, biodegradable, and nontoxic. Furthermore, the designed microcapsules had been capable of shielding the essential components from hostile environments. More advanced techniques could be developed in the future to facilitate the formulation and applications of microcapsules and working with the pharmaceutical and medical industries.


Asunto(s)
Quitosano , Quitosano/química , Cápsulas/química , Alginatos/química , Sistemas de Liberación de Medicamentos , Materiales Biocompatibles/química
16.
ACS Omega ; 8(26): 23812-23824, 2023 Jul 04.
Artículo en Inglés | MEDLINE | ID: mdl-37426214

RESUMEN

In order to increase bioavailability and intranasal absorbance, the current work set out to create azelastine nasal spray based on nanosuspension. Chondroitin was utilized as a polymer to prepare azelastine nanosuspension through the precipitation procedure. A size of 500 nm and a polydispersity index of 0.276 with a negative potential (-20 mV) were achieved. X-ray diffraction, scanning electron microscopy, Fourier transform infrared spectroscopy, thermal analysis including differential scanning calorimetry and thermogravimetric analysis, in vitro release, and diffusion studies were used to characterize the optimized nanosuspension. MTT assay was used to assess the viability of the cells, and hemolysis assay was used to assess the blood compatibility. Using RNA extraction and reverse transcription polymerase chain reaction, the levels of the anti-inflammatory cytokine IL-4, which is most closely related to cytokines in allergic rhinitis, were measured in mouse lungs. The drug dissolution and diffusion study indicated 2.0-fold increase compared to pure reference sample. Therefore, the azelastine nanosuspension could be suggested as a practical and simple nanosystem for intranasal delivery with improved permeability and bioavailability. The outcome obtained in this study indicated that azelastine nanosuspension has great potential to treat allergic rhinitis as intranasal treatment.

17.
Molecules ; 28(13)2023 Jun 29.
Artículo en Inglés | MEDLINE | ID: mdl-37446763

RESUMEN

Eco-friendly liquid chromatographic methods for measuring ergotamine (EGT) are scant in the published database. Accordingly, the goal of the current study was to develop a high-performance thin-layer chromatography (HPTLC) method for fluorescence detection of EGT in commercially available tablets. This approach was based on the application of ethyl alcohol-water (80:20 v/v) as the eco-friendly eluent mixture. The fluorescence detection of EGT was carried out at 322 nm. The greenness score of the present approach was evaluated by "Analytical GREENness (AGREE)" technology. The present approach for measuring EGT in the 25-1000 ng band-1 range was linear. The present assay for fluorescence detection of EGT was validated successfully by ICH guidelines for various parameters. The method was found to be rapid, sensitive, eco-friendly, and stability-indicating. The computed AGREE index for the current strategy was 0.84, displaying outstanding greenness features. The present methodology successfully separated the EGT degradation products under forced-degradation circumstances, exhibiting its stability-indicating qualities and selectivity. An amount of 99.33% of EGT was found in commercial formulations, indicating the validity of the current method for pharmaceutical analysis of EGT in commercial products. The results showed that EGT in commercial products might be regularly measured by the existing method.


Asunto(s)
Ergotaminas , Cromatografía en Capa Delgada/métodos , Cromatografía Líquida de Alta Presión/métodos , Reproducibilidad de los Resultados , Comprimidos
18.
Molecules ; 28(9)2023 May 08.
Artículo en Inglés | MEDLINE | ID: mdl-37175381

RESUMEN

Lung cancer is the main cause of cancer-related mortality globally. Erlotinib is a tyrosine kinase inhibitor, affecting both cancerous cell proliferation and survival. The emergence of oncological nanotechnology has provided a novel drug delivery system for erlotinib. The aims of this current investigation were to formulate two different polyamidoamine (PAMAM) dendrimer generations-generation 4 (G4) and generation 5 (G5) PAMAM dendrimer-to study the impact of two different PAMAM dendrimer formulations on entrapment by drug loading and encapsulation efficiency tests; to assess various characterizations, including particle size distribution, polydispersity index, and zeta potential; and to evaluate in vitro drug release along with assessing in situ human lung adenocarcinoma cell culture. The results showed that the average particle size of G4 and G5 nanocomposites were 200 nm and 224.8 nm, with polydispersity index values of 0.05 and 0.300, zeta potential values of 11.54 and 4.26 mV of G4 and G5 PAMAM dendrimer, respectively. Comparative in situ study showed that cationic G4 erlotinib-loaded dendrimer was more selective and had higher antiproliferation activity against A549 lung cells compared to neutral G5 erlotinib-loaded dendrimers and erlotinib alone. These conclusions highlight the potential effect of cationic G4 dendrimer as a targeting-sustained-release carrier for erlotinib.


Asunto(s)
Dendrímeros , Neoplasias Pulmonares , Humanos , Clorhidrato de Erlotinib/farmacología , Sistemas de Liberación de Medicamentos/métodos , Neoplasias Pulmonares/tratamiento farmacológico , Pulmón
19.
Molecules ; 28(10)2023 May 17.
Artículo en Inglés | MEDLINE | ID: mdl-37241879

RESUMEN

Since the discovery of nanomedicine-based drug delivery carriers such as nanoparticles, liposomes, and self-nanoemulsifying drug delivery systems (SNEDDS), enormous progress has been achieved in the field of innovative active biomolecule drug delivery systems [...].


Asunto(s)
Nanomedicina , Nanopartículas , Solubilidad , Sistemas de Liberación de Medicamentos , Portadores de Fármacos , Liposomas
20.
Saudi Pharm J ; 31(4): 605-616, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-37063446

RESUMEN

This observational descriptive study that was carried out with the objective of exploring the contribution of the local pharmaceutical industry to the Saudi drug security. Using a drug formulary provided from the Saudi Food and Drug Authority, containing all registered pharmaceutical products available in Saudi Arabia, we extracted information about drug class, drug type, country and place of manufacturing, shelf-life and price. Results showed that the majority of drugs in the market are manufactured in Europe (43.86%), followed by Saudi Arabia (22.55%), China and India (20.47%), Americas (10.24%), and other nations (2.61%). Most of the manufactured drugs were prescription drugs (90.62%). In this work, the local pharmaceutical industry with the highest percentage of contribution to local drug security was Pharmaceutical Solution Industries (PSI), representing the 5% of the items available in the Saudi market. The second highest percentage was 4% by TABUK Pharmaceutical Manufacturing CO., followed by SPIMACO (3%), JAMJOOM pharmaceutical company (2%), Riyadh pharma (2%), and Jazeera pharmaceutical industries (2%). In addition, results from this study provide information about the most essential pharmaceutical products that needs to be nationally manufactured or increased in production in order to rise the contribution of local pharmaceutical industries in Saudi drug security. Unfortunately, the small contribution of the Saudi pharmaceutical industry in local drug security increases the burden on the Kingdom's annual budget due to the over-reliance on international pharmaceuticals.

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