Diglyceride prodrug strategy for enhancing the bioavailability of norfloxacin

Dhaneshwar, Suneela; Tewari, Kunal; Joshi, Sonali; Godbole, Dhanashree; Ghosh, Pinaki

doi:10.1016/j.chemphyslip.2011.03.006

Cited by 19 publications

(15 citation statements)

References 27 publications

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“…The 50% growth inhibition (IC 50 ) values against Clone 1‐5c‐4 cells in case of FK506 or FK506 prodrugs showed 336.6 μg/mL for FK506, 337.9 μg /mL for FK506‐G, or 480.1 μg /mL for FK506‐S, suggesting that FK506‐S was less toxic than FK506 or FK506‐G (Figure ). The finding that the lipophilic drug was more cytotoxic than hydrophilic prodrugs was consistent …”

Section: Resultsmentioning

confidence: 99%

Preformulation of FK506 Prodrugs for Improving Solubility

Jun

Kim³

et al. 2016

Bulletin Korean Chem Soc

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In order to improve water solubility of a lipophilic drug, tacrolimus (FK506), two prodrugs (FK506-G or FK506-S) such as FK506-M32-LS-G (FK506-G) and FK506-M32-LS-SL (FK506-S) were synthesized. Two prodrugs (FK506-G or FK506-S), including FK506, were characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), scanning electron microscopy (SEM), enzymatic kinetics, and cytotoxicity. A phase solubility test was conducted in distilled water, and the solubility of two prodrugs (FK506-G or FK506-S) was measured in various pH values for pH solubility profiles. Most interesting was that FK506-S showed the highest solubility, 866 μg/mL in water. In vitro enzymatic kinetics of two prodrugs (FK506-G or FK506-S) in human plasma was evaluated by measuring the decrease of FK506-G or FK506-S as well as the increase of FK506 by HPLC, and FK506-G or FK506-S was metabolized in 1 h in human plasma. Two prodrugs (FK506-G or FK506-S) including FK506 showed an IC 50 of 336.6 μg/mL for FK506, 337.9 μg/mL for FK506-G, or 480.1 μg/mL for FK506-S against a conjunctive cell line, Clone 1-5c-4 cells. Taken together, FK506-S could be the most optimal prodrug for aqueous preparations based on preformulation data.

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Section: Resultsmentioning

confidence: 99%

Preformulation of FK506 Prodrugs for Improving Solubility

Jun

Kim³

et al. 2016

Bulletin Korean Chem Soc

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“…The release kinetics was examined in vivo in blood, faeces, and urine in Wistar rats’ model. The studies indicated improved pharmacological profile [104]. …”

Section: Prodrugs With Enhanced Lipophilicitymentioning

confidence: 99%

Modifications of quinolones and fluoroquinolones: hybrid compounds and dual-action molecules

Fedorowicz

Sączewski

2018

Monatsh Chem

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This review is aimed to provide extensive survey of quinolones and fluoroquinolones for a variety of applications ranging from metal complexes and nanoparticle development to hybrid conjugates with therapeutic uses. The review covers the literature from the past 10 years with emphasis placed on new applications and mechanisms of pharmacological action of quinolone derivatives. The following are considered: metal complexes, nanoparticles and nanodrugs, polymers, proteins and peptides, NO donors and analogs, anionic compounds, siderophores, phosphonates, and prodrugs with enhanced lipophilicity, phototherapeutics, fluorescent compounds, triazoles, hybrid drugs, bis-quinolones, and other modifications. This review provides a comprehensive resource, summarizing a broad range of important quinolone applications with great utility as a resource concerning both chemical modifications and also novel hybrid bifunctional therapeutic agents.Graphical abstract

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“…In spite of a great and considerable advancements as well as huge requirement in the antibacterial therapy, these drugs have been found to possess various limitations such as poor hydrophilicity, less oral bioavailability, narrow spectrum of activity, short half life, poor systemic distribution, unpleasant taste and less lipophilicity [4], [5], [6], [7], [8], [9], [10]. To get rid of these problems associated with fluoroquinolone drugs, two main approaches can be adopted; the synthesis of some novel therapeutic substances or a more efficient utilization of already accessible pharmaceutical agents through various means.…”

Section: Introductionmentioning

confidence: 99%