Preparation and study the 1:2 inclusion complex of carvedilol with β-cyclodextrin

Wen, Xianhong; Tan, Fei; Jing, Zhijun; Liu, Ziuyang

doi:10.1016/s0731-7085(03)00576-4

Cited by 141 publications

(70 citation statements)

References 33 publications

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“…The MGL Tools 1.5.4 with AutoGrid 4 and AutoDock 4 27 were used to set up and perform blind docking calculations between molecules and DNA sequence. The DNA sequence (CGCGAATTCGCG) 2 dodecamer (PDB ID: 1BNA) was obtained from the Protein Data Bank.…”

Section: Molecular Modelingmentioning

confidence: 99%

Interaction of β-Carbolines with DNA: Spectroscopic Studies, Correlation with Biological Activity and Molecular Docking

Silva

Savariz

Silva-Júnior

et al. 2016

Journal of the Brazilian Chemical Society

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Quantitative interaction of twelve β-carboline derivatives with calf thymus deoxyribonucleic acid (ctDNA) using spectroscopic techniques was evaluated. The values of the binding constants (K b ) obtained for the complexes formed with the ctDNA ranged from 3.30 × 10 2 to 1.82 × 10 6 mol L −1 , being the β-carbolines with the N,N-dimethylaminophenyl group at position 1 the ones which presented the highest K b values. The binding mode between the β-carbolines evaluated and ctDNA was proposed from the KI assay, competition with ethidium bromide, and DNA thermal denaturation profile (T m ), where it was possible to infer that the evaluated alkaloids interact with ctDNA preferably via intercalation. Additionally, the correlation of K b values obtained with the IC 50 of seven human cancer cell lines was carried out. From this study, it was possible to observe a linear relation among most of the evaluated derivatives, obtaining r 2 values from 0.5360 to 0.9600. In addition, in silico molecular docking was performed to corroborate the experimental results.

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Section: Molecular Modelingmentioning

confidence: 99%

Interaction of β-Carbolines with DNA: Spectroscopic Studies, Correlation with Biological Activity and Molecular Docking

Silva

Savariz

Silva-Júnior

et al. 2016

Journal of the Brazilian Chemical Society

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“…Carvedilol, ((±)-1-(carbazol-4-yloxy)-3-[[2-(omethoxyphenoxy) ethyl] amino]-2-propanol) (Chakraborty et al, 2009), is a drug showing antioxidant properties used in clinical practice for the treatment of cardiovascular diseases (hypertension, congestive heart failure, or myocardial infarction; Wen et al, 2004). The oral bioavailability remains low (e.g.…”

Section: Introductionmentioning

confidence: 99%

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

et al. 2016

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The purpose of this study was to develop Carvedilol nanostructured lipid carriers (CAR-NLCs) using stearic acid and oleic acid as lipid, and to estimate the potential as oral delivery system for poorly water soluble drug. The particle-size analysis revealed that all the developed formulations were within the nanometer range. The EE and loading were found to be between 69.45-88.56% and 9.58-12.56%, respectively. The CAR-NLCopt showed spherical morphology with smooth surface under transmission electron microscope (TEM). The crystallization of the drug in NLC was investigated by powder X-ray diffraction and differential scanning calorimetry (DSC) and revealed that the drug was in an amorphous state in the NLC matrix. The ex vivo gut permeation study showed many folds increment in the permeation of CAR-NLCs compared to Carvedilol suspension (CAR-S). The oral bioavailability study of CAR was carried out using Wistar rats and relative bioavailability of CAR-NLCopt was found to be 3.95 fold increased in comparison with CAR-S. In vivo antihypertensive study in Wistar rats showed significant reduction in mean systolic BP by CAR-NLCopt vis-à-vis CAR-S (p50.05) owing to the drug absorption through lymphatic pathways. In conclusion, the NLC formulation remarkably improved the oral bioavailability of CAR and demonstrated a promising perspective for oral delivery of poorly water-soluble drugs. The promising findings in this investigation suggest the practicability of these systems for the enhancement of bioavailability of CAR.

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“…21,22 The enhancement of the aqueous solubility and the dissolution rate of CAR have been extensively studied. For example, the use of lipophilic solutions, 23 formation of inclusion complex with cyclodextrin, 24 the use of a self-emulsifying system, 25 and preparation of solid dispersions 26 have all been used to improve the solubility and dissolution rate of CAR. However, studies addressing its delivery through the pulmonary route using nanoparticles are rare, and none of these has linked the optimization of formulation to the in vitro simulated pulmonary delivery of the drug.…”

Section: Introductionmentioning

confidence: 99%

Preparation, optimization, and in vitro simulated inhalation delivery of carvedilol nanoparticles loaded on a coarse carrier intended for pulmonary administration

Abdelbary¹,

Al-mahallawi²,

Abdelrahim³

et al. 2015

IJN

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Carvedilol (CAR) is a potent antihypertensive drug but has poor oral bioavailability (24%). A nanosuspension suitable for pulmonary delivery to enhance bioavailability and bypass first-pass metabolism of CAR could be advantageous. Accordingly, the aim of this work was to prepare CAR nanosuspensions and to use artificial neural networks associated with genetic algorithm to model and optimize the formulations. The optimized nanosuspension was lyophilized to obtain dry powder suitable for inhalation. However, respirable particles must have a diameter of 1–5 µm in order to deposit in the lungs. Hence, mannitol was used during lyophilization for cryoprotection and to act as a coarse carrier for nanoparticles in order to deliver them into their desired destination. The bottom-up technique was adopted for nanosuspension formulation using Pluronic stabilizers (F127, F68, and P123) combined with sodium deoxycholate at 1:1 weight ratio, at three levels with two drug loads and two aqueous to organic phase volume ratios. The drug crystallinity was studied using differential scanning calorimetry and powder X-ray diffractometry. The in vitro emitted doses of CAR were evaluated using a dry powder inhaler sampling apparatus and the aerodynamic characteristics were evaluated using an Andersen MKII cascade impactor. The artificial neural networks results showed that Pluronic F127 was the optimum stabilizer based on the desired particle size, polydispersity index, and zeta potential. Results of differential scanning calorimetry combined with powder X-ray diffractometry showed that CAR crystallinity was observed in the lyophilized nanosuspension. The aerodynamic characteristics of the optimized lyophilized nanosuspension demonstrated significantly higher percentage of total emitted dose (89.70%) and smaller mass median aerodynamic diameter (2.80 µm) compared with coarse drug powder (73.60% and 4.20 µm, respectively). In summary, the above strategy confirmed the applicability of formulating CAR in the form of nanoparticles loaded on a coarse carrier suitable for inhalation delivery.

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Preparation and study the 1:2 inclusion complex of carvedilol with β-cyclodextrin

Cited by 141 publications

References 33 publications

Interaction of β-Carbolines with DNA: Spectroscopic Studies, Correlation with Biological Activity and Molecular Docking

Interaction of β-Carbolines with DNA: Spectroscopic Studies, Correlation with Biological Activity and Molecular Docking

Carvedilol nano lipid carriers: formulation, characterization and in-vivo evaluation

Preparation, optimization, and in vitro simulated inhalation delivery of carvedilol nanoparticles loaded on a coarse carrier intended for pulmonary administration

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