Syntheses, chemical and enzymatic stability of new poly(ethylene glycol)–acyclovir prodrugs

Zacchigna, Marina; Luca, Gabriella Di; Maurich, V.; Boccù, E

doi:10.1016/s0014-827x(01)01193-4

Cited by 36 publications

(24 citation statements)

References 6 publications

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“…We have already reported our investigation of the effect of PLLA addition on the thermomechanical properties of PCL/NA blends [11]; here we report on the effect of PEG on the mechanical and thermal properties of PCL/NA blends as prepared by hot melt extrusion. PEG is approved by FDA for use in medical devices, it is commonly used for PEGylation and it can transfer its properties to other molecules by covalent bonding, which can result in toxic molecules becoming non-toxic and hydrophobic molecules becoming soluble at certain ratios [13,14]. The PEG was chosen in this study as the blended material in order to reduce the stiffness of the PCL and to increase thermal degradation rates with the overall goal of aiding the release of drugs from the PCL matrix.…”

Section: Introductionmentioning

confidence: 99%

Effect of poly ethylene glycol on the mechanical and thermal properties of bioactive poly(ε-caprolactone) melt extrudates for pharmaceutical applications

Douglas

Albadarin²,

Sajjia

et al. 2016

International Journal of Pharmaceutics

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Section: Introductionmentioning

confidence: 99%

Effect of poly ethylene glycol on the mechanical and thermal properties of bioactive poly(ε-caprolactone) melt extrudates for pharmaceutical applications

Douglas

Albadarin²,

Sajjia

et al. 2016

International Journal of Pharmaceutics

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“…However, due to ACV's poor water solubility and ensuing low bioavailability, alternative delivery approaches are required to increase the therapeutic potential of ACV. Several methods reported are to couple ACV to biocompatible hydrophilic polymers [20-22] or encapsulation into drug carriers [23-25]. Although these processes increase the bioavailability of ACV as well as offer a practical treatment for patients, they are labor-intensive and cost- ineffective.…”

Section: Introductionmentioning

confidence: 99%

Polymeric micelles for acyclovir drug delivery

Sawdon

Peng

2014

Colloids and Surfaces B: Biointerfaces

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Polymeric prodrug micelles for delivery of acyclovir (ACV) were synthesized. First, ACV was used directly to initiate ring-opening polymerization of ε-caprolactone to form ACV-polycaprolactone (ACV-PCL). Through conjugation of hydrophobic ACV-PCL with hydrophilic methoxy poly(ethylene glycol) (MPEG) or chitosan, polymeric micelles for drug delivery were formed. 1H NMR, FTIR, and gel permeation chromatography were employed to show successful conjugation of MPEG or chitosan to hydrophobic ACV-PCL. Through dynamic light scattering, zeta potential analysis, transmission electron microscopy, and critical micelle concentration (CMC), the synthesized ACV-tagged polymeric micelles were characterized. It was found that the average size of the polymeric micelles was under 200 nm and the CMCs of ACV-PCLMPEG and ACV-PCL-chitosan were 2.0 mg L−1 and 6.6 mg L−1, respectively. The drug release kinetics of ACV was investigated and cytotoxicity assay demonstrates that ACV-tagged polymeric micelles were non-toxic.

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“…These latter systems, in which drugs are delivered by chemically or biologically induced cleavage of the covalent bonds, allow one to achieve a more constant release of the drug for long periods of time. The use of polymers as prodrugs of bioactive agents can thus decrease the required dose, and then the toxicity of the drug, making its solubility and therapeutic efficiency better [7]. In modern era, some NSAIDs such as Ibuprofen, Indomethacin, Ketoprofen and Diclofenac were covalently attached to various polymer backbones and their hydrolysis studied.…”

Section: Introductionmentioning

confidence: 99%

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

Nayak

2011

Sci. Pharm.

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Ibuprofen–polyethylene glycol (PEG) conjugates (PEG-Ibu) were prepared and their potential as a prolonged release system was investigated. Two PEG-Ibu conjugates were synthesized from Ibuprofen and PEG with two different molecular weights by esterification in the presence of DCC and DMAP. The PEG-Ibu conjugates were characterized by FT-IR, 1H NMR, Mass spectroscopy and DSC analysis. The solubility study in aqueous system showed an increase in solubility of conjugates. The dissolution / hydrolysis studies showed a specific acid–base catalysis pattern dependent on the pH of the medium. This indicated a good chemical stability in aqueous buffer solution of acidic medium and the extended release behavior was found in both prodrugs after 9 hour. The results demonstrate that, in the same condition, the rate of hydrolysis for PEG4000-Ibu is slower than other. The Writhing induced by acetic acid experiment and paw edema test after oral administration showed that both conjugates had extended analgesic and anti-inflammatory effects compared with Ibuprofen. These results suggest that PEG-Ibu could be a promising NSAID prodrug with an extended pharmacological effect owing to delayed-release of parent drug.

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Syntheses, chemical and enzymatic stability of new poly(ethylene glycol)–acyclovir prodrugs

Cited by 36 publications

References 6 publications

Effect of poly ethylene glycol on the mechanical and thermal properties of bioactive poly(ε-caprolactone) melt extrudates for pharmaceutical applications

Effect of poly ethylene glycol on the mechanical and thermal properties of bioactive poly(ε-caprolactone) melt extrudates for pharmaceutical applications

Polymeric micelles for acyclovir drug delivery

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

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