In Vitro and In Vivo Study of Poly(ethylene glycol) Conjugated Ibuprofen to Extend the Duration of Action

Nayak, Anjali

doi:10.3797/scipharm.0911-07

Cited by 24 publications

(20 citation statements)

References 30 publications

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“…The process of PEG20K–EPOB releasing free EPOB was similar to the hydrolysis pattern of PEG5K–EPOB with a breakdown of the ester bond between the PEG and EPOB. As the MW of mPEG increased, the conjugates were more stable because the hydrolysis of the conjugates decreased with an increase in the length of PEG . In this study, PEG20K–EPOB was expected to have more stability than PEG5K–EPOB because of the higher MW and longer length.…”

Section: Resultsmentioning

confidence: 80%

“…As the MW of mPEG increased, the conjugates were more stable because the hydrolysis of the conjugates decreased with an increase in the length of PEG. 22,23 In this study, PEG20K-EPOB was expected to have more stability than PEG5K-EPOB because of the higher MW and longer length. However, the higher MW of PEG20K-EPOB made it difficult to be analyzed by UPLC; the exact stability of PEG20K-EPOB was not determined in our study.…”

Section: Stability Of the Peg-epob Conjugates In Plasma And Buffer Somentioning

confidence: 92%

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Synthesis and In vitro cytotoxicity of poly(ethylene glycol)–epothilone B conjugates

Zhang

Wang²,

Cheng³

et al. 2014

J of Applied Polymer Sci

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Natural epothilone B (EPOB) is currently in clinical trials for treatment of advanced cancers. In this study, two poly(ethylene glycol) (PEG)-EPOB conjugates were synthesized with carbodiimide chemistry with linear PEG Methoxy-PEG-Carboxymethy(mPEG-COOH) with different molecular weights (5 and 20 kDa). The products were confirmed by matrix-assisted laser desorption/ionization timeof-flight mass spectroscopy and 1 H-NMR, which showed that PEGylation only took place at the 7-OH site of EPOB. The solubilities of PEG5K-EPOB the conjugate of mPEG-COOH (MW 5,000) and epothilone B and PEG20K-EPOB the conjugate of mPEG-COOH (MW 20,000) and epothilone B were determined to be 4.93 3 10 22 and 1.58 3 10 22 mmol/mL; this showed improvements of 35 and 11 times, respectively, over that of free EPOB (1.4 3 10 23 mmol/mL). Moreover, the conjugates were more stable than that of free EPOB in plasma.The cytotoxicity of conjugates was evaluated on human breast cancer MCF-7 cells with an 3-(4,5)-dimethylthiahiazo (-z-y1)-3,5-di-phenytetrazoliumromide(MTT) based assay. The half maximal inhibitory concentration of a substance(IC50) values of EPOB, PEG5K-EPOB, and PEG20K-EPOB were 6.0 3 10 24, 0.57, and 8.4 3 10 23 lM, respectively.

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Section: Resultsmentioning

confidence: 80%

Section: Stability Of the Peg-epob Conjugates In Plasma And Buffer Somentioning

confidence: 92%

Synthesis and In vitro cytotoxicity of poly(ethylene glycol)–epothilone B conjugates

Zhang

Wang²,

Cheng³

et al. 2014

J of Applied Polymer Sci

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“…The product obtained was dissolved in dichloro methane and dried over anhydrous potassium carbonate and filtered. The filtrate was then treated with Neutral Alumina and then reprecipitated by excess of cold Diethyl ether 30 .…”

Section: Classification Of Polymersmentioning

confidence: 99%

Synthesis and Comparison of Peg-Ibuprofen and Peg-Ketoprofen Prodrugs by in Vitro and in Vivo Evaluation

Kemisetti¹,

Sarangapani

2018

J. Drug Delivery Ther.

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Pain is an unpleasant sensation experienced by all individuals and classified as acute and chronic pain. NSAID's were most widely used for treatment of Analgesia and Inflammation. Ibuprofen, Ketoprofen, Polyethylene glycol 1500 & PEG 6000 were used as drug carriers and Glycine was used as spacer to link the drugs through ester linkage. Ibuprofen and Ketoprofen belong to propionic acid derivatives of Anti-inflammatory drugs and are non-selective COX inhibitors. PEG 1500/PEG6000-Ibuprofen/Ketoprofen and PEG 1500/PEG 6000-Glycine-Ibuprofen/Ketoprofen were synthesized and are subjected to In Vitro dissolution studies which revealed that the drug release was higher at 7.2 pH rather than at 1.2 pH. The results of In Vivo evaluation studies of both synthesized prodrugs revealed that these prodrugs retained their Analgesic activity by hot plate method and acetic acid method, Antiinflammatory activity by paw edema method and cotton pellet method. Both the prodrugs had exhibited good ulcer protective activity when compared to parent drugs.

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“…Therefore, the research was focused on masking the carboxylic acid group of selected NSAID agent oxaprozin by esterification with dextran, a biodegradable carrier . Further, it was aimed to evaluate the prepared prodrug for its physicochemical and pharmacological characters.…”

Section: Introductionmentioning

confidence: 99%

Oxaprozin prodrug as safer nonsteroidal anti‐inflammatory drug: Synthesis and pharmacological evaluation

Peesa

Atmakuri²,

Yalavarthi

et al. 2017

Archiv der Pharmazie

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Oxaprozin is a popular non-steroidal anti-inflammatory drug (NSAID) and its chronic oral use is clinically restricted due to its gastrointestinal (GI) complications. In order to circumvent the GI complications, oxaprozin was amended as a prodrug in a one-pot reaction using N,N-carbonyldiimidazole as an activating agent. Dextran of average molecular weight (60,000-90,000 Da) was exploited as a carrier in the process of oxaprozin prodrug production by esterification. The structural profiles of the synthesized oxaprozin prodrug were characterized by FT-IR and NMR spectroscopy. The oxaprozin prodrug possessed optimal molecular weight, lipophilicity, partition coefficient, protein binding, and degree of substitution of 52.4%. The release of oxaprozin upon hydrolysis of the prodrug in both simulated gastric fluid and simulated intestinal fluid followed first-order kinetics with 55.2 min of half-life. Varied ADME properties of the prodrug resulted upon Schrodinger's QikProp tool application. Oxaprozin prodrug displayed significant analgesic, antipyretic, and anti-inflammatory activities, with a remarkable decrease in the ulcer index and being devoid of antigenicity in experimental animals. Thus, it is evident that oxaprozin prodrug is a safer oral NSAID without causing any ulcerations.

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In Vitro and In Vivo Study of Poly(ethylene glycol) Conjugated Ibuprofen to Extend the Duration of Action

Cited by 24 publications

References 30 publications

Synthesis and In vitro cytotoxicity of poly(ethylene glycol)–epothilone B conjugates

Synthesis and In vitro cytotoxicity of poly(ethylene glycol)–epothilone B conjugates

Synthesis and Comparison of Peg-Ibuprofen and Peg-Ketoprofen Prodrugs by in Vitro and in Vivo Evaluation

Oxaprozin prodrug as safer nonsteroidal anti‐inflammatory drug: Synthesis and pharmacological evaluation

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