NO-NSAIDs. Part 3: Nitric Oxide-Releasing Prodrugs of Non-steroidal Anti-inflammatory Drugs

Borhade, Namdev; Pathan, Asif R.; Halder, Somnath; Karwa, Manoj; Dhiman, Mini; Pamidiboina, Venu; Gund, Machhindra; Deshattiwar, Jagannath Janardhan; Mali, Sunil V.; Deshmukh, Nitin; Senthilkumar, S; Gaikwad, Parikshit; Tipparam, Santhosh G.; Mudgal, Jayesh; Dutta, Milan Chandra; Burhan, Aslam; Thakre, Gajanan; Sharma, Ankur; Deshpande, Shubhada; Desai, Dattatraya C.; Dubash, Nauzer P.; Jain, Arun K.; Sharma, Somesh; Nemmani, Kumar V.S.; Satyam, Apparao

doi:10.1248/cpb.60.465

Cited by 33 publications

(16 citation statements)

References 32 publications

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“…Furthermore, NO-naproxene showed superior analgesic, anti-inflammatory, and anti-oxidative actions than parent compounds [28]. Another NSAIDs combined with biogas H 2 S warrant GI safety since sodium hydrogen sulfide prevents the reduction of mucosal blood flow, counteracted increased expression of TNF-a and ICAM-1, improved PGE 2 synthesis all impaired by NSAIDs [29 ,30 ,31].…”

Section: Pharmacological Development To Overcome Classical Mechanismsmentioning

confidence: 99%

Development of GI-safe NSAID; progression from the bark of willow tree to modern pharmacology

Kangwan

Park

Hahm

2014

Current Opinion in Pharmacology

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Section: Pharmacological Development To Overcome Classical Mechanismsmentioning

confidence: 99%

Development of GI-safe NSAID; progression from the bark of willow tree to modern pharmacology

Kangwan

Park

Hahm

2014

Current Opinion in Pharmacology

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“…Various strategies have been explored to avoid NSAIDs-related toxicity, including concomitant administration of gastric protectors (as free-drugs or coupled) [7], use of rectal drug delivery systems [8], or modified release formulations [9]. The development of oral controlled and sustained release offers a potential benefit for NSAIDs.…”

Section: Introductionmentioning

confidence: 99%

Ibuprofen Nanoparticles for Oral Delivery: Proof of Concept

Figueiredo¹

2014

J Nanomedine Biotherapeutic Discov

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Background: Using nanoparticles to improve non-steroidal anti-inflammatory drugs therapeutic profile is an interesting approach, especially concerning their gastric toxicity.Objective: The aim of this work was to present a proof of concept for a nanoparticulate formulation composed of a biodegradable polymer poly (DL-lactic acid) (PLA) meant for oral delivery of ibuprofen (IBU) to systemic circulation with reduced gastric toxicity. Materials and methods:IBU-loaded nanoparticles composed of PLA and poloxamer 188 were prepared by an emulsion/solvent diffusion method. The particles obtained were characterized for size, zeta potential and morphology, as well as encapsulation efficiency. Nanoparticles were given to Wistar rats at an equivalent dose of 12 mg/kg (t.i.d.) of ibuprofen for a period of 10 days. Both concentration of IBU in the plasma and toxicity in different tissues were evaluated.Results: Nanoparticles displayed a size of 281.1 ± 66.7 nm with a zeta potential of -4.3 mV. Scanning electron microscopic images showed spherical shape particles with low polydispersity index. IBU concentration in blood samples indicated that nanoparticles were able to deliver IBU to systemic circulation. A significant reduction in toxicity was observed for nanoparticles in gastric mucosa compared to free ibuprofen. This may be due to controlled release of IBU from the nanoparticles, which decreases the mucosal contact to IBU. In summary, we designed a proof of concept for PLA nanoparticles as suitable carrier for IBU allowing reduced gastric toxicity of the drugs. This strategy can eventually be applied to other non-steroidal anti-inflammatory drugs.

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“…Increasing data suggest a considerable "modulating" effect of nitric oxide as a pleiotropic agent, acting on several body parts. [4][5][6] There is important evidence that NO is involved in several inflammatory disorders. Indeed, every cell and many immunological parameters are virtually modulated by NO.…”

Section: Introductionmentioning

confidence: 99%

The synthesis, characterization and biological evaluation of a new nitric oxide donor agent

Profire

Apotrosoaei

Oprea

et al. 2014

JSCS

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The synthesis of a new xanthine nitric oxide donor (TSP-81) is discussed. The designed compound included two structural moieties, i.e., theophylline (1,3-dimethylxanthine) and acetaminophen (4-hydroxyacetanilide), linked by the nitric oxide donor alkyl chain as a spacer. The compound was characterized by microanalysis (CHN), 1 H-NMR, 13 C-NMR, FT-IR and UV--Vis spectroscopy and thermogravimetric analysis. The thermal behaviour showed that TSP-81 melts with decomposition in four steps, the most important ones being the 2 nd one (the registered weight loss being 17.6 %) and the 3 rd one (with a registered weight loss of 30.4 %). The toxicity degree, the anti--inflammatory effect and the ability of releasing nitric oxide of TSP-81 was also evaluated. The biological assays established that TSP-81 exhibits enhanced biological properties, such as lower toxicity and higher anti-inflammatory effect, compared to theophylline and acetaminophen, the drugs used as the parent molecules. Thus, TSP-81 is approximately 2 times more active than theophylline and 4 times more active than acetaminophen in reducing cotton pellet granuloma formation. Furthermore, the release of nitric oxide (NO) appears to play an important role in enhancing the anti-inflammatory effect.

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NO-NSAIDs. Part 3: Nitric Oxide-Releasing Prodrugs of Non-steroidal Anti-inflammatory Drugs

Cited by 33 publications

References 32 publications

Development of GI-safe NSAID; progression from the bark of willow tree to modern pharmacology

Development of GI-safe NSAID; progression from the bark of willow tree to modern pharmacology

Ibuprofen Nanoparticles for Oral Delivery: Proof of Concept

The synthesis, characterization and biological evaluation of a new nitric oxide donor agent

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