Pulsatile: A Tool for Circardian Rhythm - A Review

Modi, Mitesh P.; Prasanth, V V; Mathew, Sam T.

doi:10.22270/jddt.v2i1.68

Cited by 7 publications

(10 citation statements)

References 23 publications

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“…In the majority of conventional oral controlled-release drug delivery systems, the drug is released at constant or variable rates. There is currently growing interest in systems designed to deliver time-specific (delayed, pulsatile) and site-specific drug delivery among modified-release oral dosage forms (Modi et al, 2012). For those diseases whose symptoms tend to return primarily at night or in the early morning, the potential of using the pulsatile release to undertake chronotherapy is particularly alluring, such as bronchial asthma, peptic ulcers, angina pectoris, and rheumatoid arthritis.…”

Section: Pulsatile Drug Delivery Systemmentioning

confidence: 99%

“…The chronotherapeutic oral drug absorption system (CODAS®) is a multi-particular system, dosed at bedtime that delays drug release for 4-5 h. The delay is provided by the non-enteric coating of the drug-loaded beads. The technique has been used in the formulation of Verapamil extendedrelease capsules Verelan® PM (Modi et al, 2012).…”

Section: Codas Technologymentioning

confidence: 99%

“…The drug was sealed inside an insoluble capsule body by an erodible tablet made of insoluble dibasic calcium phosphate and gel-forming HPMC excipient. In brief, by careful selection and combination of polymeric drug carriers of different erosion/degradation kinetic, or by manipulating the interaction energy between the drug and the polymer, it is possible to control drug release according to the requirement of the biological rhythm of the given disease state (Modi et al, 2012).…”

Section: Other Cr Erodible Polymersmentioning

confidence: 99%

See 2 more Smart Citations

A Comprehensive Review on Chronotherapeutics

Kiranmai¹,

Raajitha²

2023

IJPSM

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Chronotherapy refers to the use of circadian, ultradian, infradian & seasonal, or other rhythmic cycles in the application of therapy. There are a number of conditions that show a circadian pattern and advantages could be taken by timing and adjusting the administration of drugs according to the circadian rhythm of the disease. Chronotherapy can be divided into three categories: time-controlled systems, in which the drug release is primarily controlled by the delivery system; stimuli-induced PDDS, in which release is controlled by the stimuli, such as the pH or intestinal enzymes; or externally regulated systems, in which release is programmed by external stimuli such as magnetism, ultrasound, electrical effect, and irradiation. The symptoms of some diseases, such as asthma, arthritis, depression, ulcer, allergic rhinitis, sleep disturbances, etc., are influenced by circadian rhythms. The biological clock of the human body is based on solar and lunar adaptations. The circadian rhythm is the primary rhythm that the biological clock adheres to. The functioning of the brain, behavior, and cognition can all be significantly impacted by circadian rhythm disruption. The use of chronotherapeutics can help with this. The recent interest that has occurred in the field of chronotherapeutics is to match the circadian rhythms of the disease for the successful treatment of the disease.

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Section: Pulsatile Drug Delivery Systemmentioning

confidence: 99%

Section: Codas Technologymentioning

confidence: 99%

Section: Other Cr Erodible Polymersmentioning

confidence: 99%

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A Comprehensive Review on Chronotherapeutics

Kiranmai¹,

Raajitha²

2023

IJPSM

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“…Covalent inhibitors of type III impede the binding of ATP at the binding site by forming a covalent bond with the cysteine amino acid residue. [ 80 ] The key pharmacophoric characteristics that the majority of VEGFR inhibitors have in common are: (i) a flat heterocyclic core, such as a moiety located in the ATP‐binding area that directs the orientation of the backbone donor (NH of Cys919 residue) and an important H‐bond acceptor (a lone pair of nitrogen), (ii) a hydrophobic spacer (central aromatic ring) that fills the linker space between the ATP‐binding domain and the DFG domain, (iii) Glu885 and Asp1046 residues in the DFG out domain (allosteric region) are targeted for interaction with urea or amide moiety acting as H‐bond donor‐acceptor pair; the NH motif makes a hydrogen bond with Glu885 and the CO motif forms a hydrogen bond with Asp1046, (iv) the terminal aryl moiety, which is in the allosteric hydrophobic back pocket and interacts hydrophobically with the hydrophobic side chains of Leu1019, Leu892, and Leu1049. [ 81 ]…”

Section: Pyrazolo[34‐d]pyrimidines As Vegfr Inhibitorsmentioning

confidence: 99%

Pyrazolo[3,4‐d]pyrimidine scaffold: A review on synthetic approaches and EGFR and VEGFR inhibitory activities

Kassab

2022

Archiv der Pharmazie

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The pyrazolo[3,4‐d]pyrimidine core has received a lot of interest from the medicinal chemistry community as a promising framework for drug design and discovery. It is an isostere of the adenine ring of adenosine triphosphate, which allows it to mimic kinase active site hinge region binding contacts. This scaffold has a wide pharmacological and biological value, one of which is as an anticancer agent. Many successful anticancer medicines have been designed and synthesized using pyrazolo[3,4‐d]pyrimidine as a key pharmacophore. The main synthetic routes of pyrazolo[3,4‐d]pyrimidines as well as their recent developments as promising anticancer agents acting as endothelial growth factor receptors and vascular endothelial growth factor receptor inhibitors, published in the time frame from 1999 to 2022, are summarized in this review to set the direction for the design and synthesis of novel pyrazolo[3,4‐d]pyrimidine derivatives for clinical deployment in cancer treatment.

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“…[ 5 ] NSCLC, thyroid, colorectal, ovarian, breast, melanoma, and Hepatocellular carcinoma are among the cancers where VEGFR‐2 is overexpressed. [ 6,7 ] VEGFR‐2 has thus been discovered as a potential ameliorative ambition for the development of innovative anticancer drugs. [ 7 ] According to reports, the heterocyclic thiazolidine‐2,4‐dione (TZD) compounds may typify as a critical scaffold in the remedy of cancer.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and docking of novel thiazolidine‐2,4‐dione multitarget scaffold as new approach for cancer treatment

Hanafy

El‐Hddad

Abdelgawad

et al. 2023

Archiv der Pharmazie

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Novel thiazolidine‐2,4‐diones have been developed and estimated as conjoint inhibitors of EGFRT790M and VEGFR‐2 against HCT‐116, MCF‐7, A549, and HepG2 cells. Compounds 6a, 6b, and 6c were known to be the dominant advantageous congeners against HCT116 (IC50 = 15.22, 8.65, and 8.80 µM), A549 (IC50 = 7.10, 6.55, and 8.11 µM), MCF‐7 (IC50 = 14.56, 6.65, and 7.09 µM) and HepG2 (IC50 = 11.90, 5.35, and 5.60 µM) mass cell lines, correspondingly. Although compounds 6a, 6b, and 6c disclosed poorer effects than sorafenib (IC50 = 4.00, 4.04, 5.58, and 5.05 µM) against the tested cell sets, congeners 6b and 6c demonstrated higher actions than erlotinib (IC50 = 7.73, 5.49, 8.20, and 13.91 µM) against HCT116, MCF‐7 and HepG2 cells, yet lesser performance on A549 cells. The hugely effective derivatives 4e–i and 6a–c were inspected versus VERO normal cell strains. Compounds 6b, 6c, 6a, and 4i were found to be the most effective derivatives, which suppressed VEGFR‐2 by IC50 = 0.85, 0.90, 1.50, and 1.80 µM, respectively. Moreover, compounds 6b, 6a, 6c, and 6i could interfere with the EGFRT790M performing strongest effects with IC50 = 0.30, 0.35, 0.50, and 1.00 µM, respectively. What is more, 6a, 6b, and 6c represented satisfactory in silico computed ADMET profile.

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Pulsatile: A Tool for Circardian Rhythm - A Review

Cited by 7 publications

References 23 publications

A Comprehensive Review on Chronotherapeutics

A Comprehensive Review on Chronotherapeutics

Pyrazolo[3,4‐d]pyrimidine scaffold: A review on synthetic approaches and EGFR and VEGFR inhibitory activities

Design, synthesis, and docking of novel thiazolidine‐2,4‐dione multitarget scaffold as new approach for cancer treatment

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