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1.
Ther Deliv ; 15(4): 267-278, 2024 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-38449422

RESUMEN

Background: Thymoquinone (TQ) and vitamin C (Vit C) have demonstrated individual anticancer effects in various studies. TQ exhibits inhibitory properties against tumor growth, induces apoptosis, while Vit C protects against DNA damage and oxidative stress. Aim: Formulation of TQ and Vit C combination into liposomes using two methods and investigate the synergistic anticancer. Method: Liposomal preparations were characterized, and the purity of drug components was confirmed using encapsulation efficiency (EE %). Results: In vitro cell viability studies demonstrated the inhibitory effect of TQ and Vit C against colorectal (HT29, 5.5 ± 0.9 µM) and lung cancer (A549, 6.25 ± 0.9 µM) cell lines with combination index <1. Conclusion: The formulation of TQ and Vit C displayed synergistic anticancer activity.


Asunto(s)
Liposomas , Neoplasias Pulmonares , Humanos , Ácido Ascórbico/farmacología , Benzoquinonas/farmacología , Neoplasias Pulmonares/tratamiento farmacológico , Línea Celular Tumoral
2.
Ther Deliv ; 2024 Mar 12.
Artículo en Inglés | MEDLINE | ID: mdl-38469691

RESUMEN

Aim: In this study, we prepared, characterized and in vitro evaluated a 5-fluorouracil (5-FU)-loaded chitosan-acacia gum nanoparticles. Methods: Nanoparticles were characterized for their size, charge, morphology and encapsulation efficiency (EE%) followed by cellular investigations against HT-29 colon cancer cell line. Results: The nanoparticles exhibited a spherical morphological size with 94.42% EE%. Free 5-FU showed a fast and fully cumulative release after 6 h while 5-FU loaded into CS-AG NPs showed good entrapment and slow, prolonged 5-FU release even after 24 h. Enhanced IC50 for the 5-FU loaded NPs compared with free 5-FU against HT-29 colon cancer cell line was reported with high selectivity compared with normal fibroblast cells. Conclusion: 5-FU loaded NPs is promising nano-therapy against colon cancer.

3.
J Liposome Res ; 34(1): 178-202, 2024 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-37378553

RESUMEN

Liposomes are spherical lipidic nanocarriers composed of natural or synthetic phospholipids with a hydrophobic bilayer and aqueous core, which are arranged into a polar head and a long hydrophobic tail, forming an amphipathic nano/micro-particle. Despite numerous liposomal applications, their use encounters many challenges related to the physicochemical properties strongly affected by their constituents, colloidal stability, and interactions with the biological environment. This review aims to provide a perspective and a clear idea about the main factors that regulate the liposomes' colloidal and bilayer stability, emphasising the roles of cholesterol and its possible alternatives. Moreover, this review will analyse strategies that offer possible approaches to provide more stable in vitro and in vivo liposomes with enhanced drug release and encapsulation efficiencies.


Asunto(s)
Liposomas , Fosfolípidos , Liposomas/química , Fosfolípidos/química , Colesterol/química , Estabilidad de Medicamentos
4.
Chem Biodivers ; 21(2): e202301470, 2024 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-38161147

RESUMEN

Doxorubicin (DOX) is widely used against solid tumors. Niosomes are self-assembled nanocarriers of non-ionic surfactants. DOX loaded into cationic niosomes (DOX-Nio) was prepared via thin film hydration method. DOX-Nio was then decorated with a hyaluronic acid (DOX-HA-Nio) via electrostatic interaction. DOX-Nio and DOX-HA-Nio displayed a particle size of 120.0±1.02 and 182.9±2.3 nm, and charge of + 35.5±0.15 and -15.6±0.25 mV, respectively, with PDI < 0.3. DOX-HA-Nio showed a good stability regarding size and charge over 4 weeks at 4 °C and maintain their integrity after lyophilization. HPLC results showed a 94.1±4.2 % encapsulation efficiency of DOX with good entrapment and slow, prolonged DOX release even after 48 hrs. Cell viability assay showed an IC50 of 14.26 nM for the DOX-HA-Nio against MCF-7 cell line with micromolar IC50 results against CD-44 negative cell lines (NIH/3T3). DOX-HA-Nio was proven to be an effective, targeted nanocarrier for DOX against MCF-7 cell line.


Asunto(s)
Neoplasias de la Mama , Humanos , Femenino , Neoplasias de la Mama/tratamiento farmacológico , Liposomas , Ácido Hialurónico , Doxorrubicina/farmacología , Células MCF-7
5.
Molecules ; 28(19)2023 Oct 04.
Artículo en Inglés | MEDLINE | ID: mdl-37836770

RESUMEN

The current work was aimed at the development of a topical drug delivery system for azelaic acid (AzA) for acne treatment. The systems tested for this purpose were deep eutectic systems (DESs) prepared from choline chloride (CC), malonic acid (MA), and PEG 400. Three CC to MA and eight different MA: CC: PEG400 ratios were tested. The physical appearance of the tested formulations ranged from solid and liquid to semisolid. Only those that showed liquid formulations of suitable viscosity were considered for further investigations. A eutectic mixture made from MA: CC: PEG400 1:1:6 (MCP 116) showed the best characteristics in terms of viscosity, contact angle, spreadability, partition coefficient, and in vitro diffusion. Moreover, the MCP116 showed close rheological properties to the commercially available market lead acne treatment product (Skinorin®). In addition, the formula showed synergistic antibacterial activity between the MA moiety of the DES and the AzA. In vitro diffusion studies using polyamide membranes demonstrated superior diffusion of MCP116 over the pure drug and the commercial product. No signs of skin irritation and edema were observed when MCP116 was applied to rabbit skin. Additionally, the MCP116 was found to be, physically and chemically, highly stable at 4, 25, and 40 °C for a one-month stability study.


Asunto(s)
Acné Vulgar , Fármacos Dermatológicos , Animales , Conejos , Ácidos Dicarboxílicos/química , Fármacos Dermatológicos/uso terapéutico , Piel , Preparaciones Farmacéuticas , Colina/química , Acné Vulgar/tratamiento farmacológico , Solventes/química
6.
Chem Biodivers ; 20(8): e202300534, 2023 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-37498138

RESUMEN

Olive leaf extract is a valuable source of phenolic compounds; primarily, oleuropein (major component) and rutin. This natural olive leaf extract has potential use as a therapeutic agent for cancer treatment. However, its clinical application is hindered by poor pharmacokinetics and low stability. To overcome these limitations, this study aimed to enhance the anticancer activity and stability of oleuropein and rutin by loading them into PEGylated Nano-phytosomes. The developed PEGylated Nano-phytosomes exhibited favorable characteristics in terms of size, charge, and stability. Notably, the anticolonic cancer activity of the Pegylated Nano-phytosomes loaded with oleuropein (IC50=0.14 µM) and rutin (IC50=0.44 µM) surpassed that of pure oleuropein and rutin alone. This outcome highlights the advantageous impact of Nano-phytosomes to augment the anticancer potential of oleuropein and rutin. These results present a promising pathway for the future development of oleuropein and rutin Nano-phytosomes as effective options for passive tumor-targeted therapy, given their improved stability and efficacy.


Asunto(s)
Neoplasias , Olea , Rutina/farmacología , Antioxidantes , Iridoides/farmacología , Glucósidos Iridoides , Polietilenglicoles , Hojas de la Planta , Extractos Vegetales/farmacología
7.
Int J Anal Chem ; 2015: 862592, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25838825

RESUMEN

A simple, sensitive, inexpensive, and rapid stability indicating high performance liquid chromatographic method has been developed for determination of gemcitabine in injectable dosage forms using theophylline as internal standard. Chromatographic separation was achieved on a Phenomenex Luna C-18 column (250 mm × 4.6 mm; 5µ) with a mobile phase consisting of 90% water and 10% acetonitrile (pH 7.00 ± 0.05). The signals of gemcitabine and theophylline were recorded at 275 nm. Calibration curves were linear in the concentration range of 0.5-50 µg/mL. The correlation coefficient was 0.999 or higher. The limit of detection and limit of quantitation were 0.1498 and 0.4541 µg/mL, respectively. The inter- and intraday precision were less than 2%. Accuracy of the method ranged from 100.2% to 100.4%. Stability studies indicate that the drug was stable to sunlight and UV light. The drug gives 6 different hydrolytic products under alkaline stress and 3 in acidic condition. Aqueous and oxidative stress conditions also degrade the drug. Degradation was higher in the alkaline condition compared to other stress conditions. The robustness of the methods was evaluated using design of experiments. Validation reveals that the proposed method is specific, accurate, precise, reliable, robust, reproducible, and suitable for the quantitative analysis.

8.
Int J Pharm ; 311(1-2): 63-8, 2006 Mar 27.
Artículo en Inglés | MEDLINE | ID: mdl-16455214

RESUMEN

The pharmacokinetic parameters, i.e. peak concentration (c(max)); peak time (t(max)); area under the curve (AUC); elimination rate constant (k); absorption rate constant (k(a)); Drug clearance (cl(t)), and the volume of distribution (v(d)) of sodium salicylate administered in fractionated coconut oil (FCO) have been compared with that from an aqueous and glycerin vehicles using a three-way crossover study in 12 rabbits. The results of the study show that all of the pharmacokinetic parameters tested differ significantly when administered in oily rather than aqueous or glycerin vehicles. No statistically significant difference was found between any of the above mentioned parameters when comparison was made between aqueous and glycerin formulations. The results indicate that sodium salicylate is absorbed at a lower rate but to a greater extent from oily formulation. Possible reasons for these differences are discussed and is suggested, therefore, that the oily formulation might be used as a sustained release preparation.


Asunto(s)
Antiinflamatorios no Esteroideos/farmacocinética , Vehículos Farmacéuticos , Aceites de Plantas/química , Salicilato de Sodio/farmacocinética , Agua/química , Administración Oral , Animales , Antiinflamatorios no Esteroideos/administración & dosificación , Antiinflamatorios no Esteroideos/química , Química Farmacéutica , Aceite de Coco , Vaciamiento Gástrico/efectos de los fármacos , Tránsito Gastrointestinal/efectos de los fármacos , Glicerol/química , Absorción Intestinal/efectos de los fármacos , Masculino , Aceites de Plantas/farmacología , Conejos , Salicilato de Sodio/administración & dosificación , Salicilato de Sodio/química , Viscosidad
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