Liberação específica de fármacos para administração no cólon por via oral. I - O cólon como local de liberação de fármacos

Freire, Ana Cristina; Podczeck, Fridrun; Sousa, João; Veiga, Francisco José

doi:10.1590/s1516-93322006000300003

Cited by 10 publications

(5 citation statements)

References 53 publications

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“…The oral administration route is the most recommended in developing drugs for tropical diseases, because it is considered easy for patients to adhere to treatment; therefore, it is necessary for the drugs to have good oral bioavailability they can be linked to good solubility and essential permeability to predict the ability of compounds to reach their target at established concentrations [ 65 , 66 ].…”

Section: Resultsmentioning

confidence: 99%

Evaluation of antiplasmodial activity in silico and in vitro of N-acylhydrazone derivatives

et al. 2022

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N-acylhydrazones are considered privileged structures in medicinal chemistry, being part of antimicrobial compounds (for example). In this study we show the activity of N-acylhydrazone compounds, namely AH1, AH2, AH4, AH5 in in vitro tests against the chloroquine-resistant strain of Plasmodium falciparum (W2) and against WI26 VA-4 human cell lines. All compounds showed low cytotoxicity (LC50 > 100 µM). The AH5 compound was the most active against Plasmodium falciparum, with an IC50 value of 0.07 μM. AH4 and AH5 were selected among the tested compounds for molecular docking calculations to elucidate possible targets involved in their mechanism of action and the SwissADME analysis to predict their pharmacokinetic profile. The AH5 compound showed affinity for 12 targets with low selectivity, while the AH4 compound had greater affinity for only one target (3PHC). These compounds met Lipinski's standards in the ADME in silico tests, indicating good bioavailability results. These results demonstrate that these N-acylhydrazone compounds are good candidates for future preclinical studies against malaria. Graphical Abstract

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Section: Resultsmentioning

confidence: 99%

Evaluation of antiplasmodial activity in silico and in vitro of N-acylhydrazone derivatives

et al. 2022

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“…To obtain maximum absorption of the drug in the colon, there should be minimal or null absorption through the gastric mucosa and small intestine and, to this effect, the resistance time in these regions should be considered. Transit of the pharmaceutical form through the stomach ranges from minutes to 2 hours (acidic pH) and, through the small intestine, the transit time is approximately 3-4 hours (Freire et al, 2006;Sanghi and Tiwle, 2016).…”

Section: In Vitro Dissolution Profilementioning

confidence: 99%

Application of zein and chitosan in the development of a colon-specific delivery system

Zara¹,

Stival²,

Shioji³

et al. 2020

J Appl Pharm Sci

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Drug release in the colon is a therapeutic alternative for pathologies that affect this organ, for absorption of peptide drugs and proteins, and in chronopharmacotherapy. Systems for this purpose should be formulated considering the obstacles of the gastrointestinal tract. Strategies used consider characteristics such as pH, enzymatic activity, microflora, and transit time. This work aims to present a system to deliver drugs directly to the colon using the natural polymers zein and chitosan. The biopolymers were prepared with the objective of obtaining effective polymer dispersions to be applied in the coating of tablets and evaluated for in vitro dissolution profile. The polymer films obtained by casting were characterized by Fourier-transform infrared spectroscopy, thermal analysis, mechanical analysis, and water vapor transmission. The results obtained demonstrate that zein can be used as a sealing coat to separate incompatible materials and as a barrier against moisture. They also show that chitosan is specifically degraded by the colonic flora and, when associated with ethyl cellulose, can be applied as support for the colon-specific delivery.

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“…8B) showed distinct amorphous halo and characteristic peaks indicating the semi-crystalline nature of this polymers. The peaks around 171, 231 and 251 (2θ) are characteristic of the B-type polymorphous, while the peak in 19.81 is typical of V polymorph indicating a well-organized crystalline structure of amylose-lipid complexes present in the starch granules (Carbinatto et al, 2012;Freire et al, 2006;Shamai et al, 2003;Soares et al, 2013).…”

Section: X-ray Diffraction (Xrd) Analysismentioning

confidence: 99%

Development and characterization of cross-linked gellan gum and retrograded starch blend hydrogels for drug delivery applications

Cardoso

Cury

Evangelista

et al. 2017

Journal of the Mechanical Behavior of Biomedical Materials

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The retrogradation of high amylose starch (5% or 10%), by isothermal cycles at 4°C (method 1) or by alternating thermal cycles (method 2) was efficient and promoted important structural modifications. Hydrogels of gellan gum and starch retrograded blends, containing or not ketoprofen, were prepared by ionic and dual cross-linking, at different concentrations of polymer and cross-linkers, and characterized by texture and rheological analysis, X-ray diffraction and morphological analysis. The ionic cross-linking and starch retrograded by method 1 contributed to the improvement of hardness and cohesiveness of hydrogels while the dual cross-linking and starch retrograded by method 2 favored the adhesiveness. The rising of polymer concentration lead to the improvement of all mechanical parameters. Rheological data demonstrated that non-cross-linked dispersions showed a behavior of weak gels and the cross-linked hydrogels presented a predominantly elastic behavior (G'≫G″), peculiar of strong gels. X-ray diffraction, rheological data and the scanning electron microscopy (FEG-SEM) revealed that the increase of polymers and cross-linkers concentration and the presence of drug resulted in stronger and more stable tridimensional structures. The suitable adhesiveness and high strength and elasticity of hydrogels H253IC-KT, H255IC-KT, H21053DC-KT and H21055DC-KT make them more promising materials for the design of mucoadhesive drug delivery systems.

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Liberação específica de fármacos para administração no cólon por via oral. I - O cólon como local de liberação de fármacos

Abstract: A liberação específica de fármacos no cólon tem atraído a atenção de investigadores interessados no tratamento de patologias locais e no

Cited by 10 publications

References 53 publications

Evaluation of antiplasmodial activity in silico and in vitro of N-acylhydrazone derivatives

Evaluation of antiplasmodial activity in silico and in vitro of N-acylhydrazone derivatives

Application of zein and chitosan in the development of a colon-specific delivery system

Development and characterization of cross-linked gellan gum and retrograded starch blend hydrogels for drug delivery applications

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