Synthèse et polymérisation de polyméthacrylates porteurs de la quinine. Etude comparée de la toxicité et de l'immunogénicité des formes libres et polymériques

Pinazzi, Christian; Rabadeux, Jean Claude; Pleurdeau, A.; Nivière, P; Paubel, J.P.; Benoit, J.

doi:10.1002/macp.1978.021790705

Cited by 21 publications

(1 citation statement)

References 8 publications

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“…With a view to reducing the side effects due to the repeated administration of free drugs, many attempts have been made in recent years to prolong the activity of drugs by attaching the drugs to synthetic and natural polymers. [1][2][3][4][5][6][7][8][9] A hydrolyzable bond between drug and macromolecule is required if the drug is active only in its free form. This linkage can undergo chemical and enzymatic hydrolysis with subsequent release of the drug in the body.…”

Section: Introductionmentioning

confidence: 99%

Antiinflammatory polymer‐bound steroids for topical applications II. Controlled release of the steroids

Khue

Jung

Poindron

1986

J. Polym. Sci. A Polym. Chem.

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SynopsisThe release of hydrocortisone and dexamethasone due to hydrolysis of the carbonate linkage from the polymeric supports of polfloxyethyleneglycol), hydroxypropyl cellulose, and N-vinylpyrrolidone/hydrocortisone-z1CHz-vinylcarbonate copolymer was observed in a living system, by induction of aGPDH activity in rat C6 glial cells, and in uitro by a kinetic study of release in aqueous sodium phosphate buffer medium. The glucocorticoid reiease is pH and temperature dependent and highly sensitive to steric hindrance. In uiw, testing on antiinflammatory activity in rats with poly foxyethyleneglycol) and hydroxypropyl cellulhse bound dexamethasone was performed. However, it produced negative results probably due to difficulty in splitting the carbonate linkage in the inflammatory region of acidic pH values.

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Section: Introductionmentioning

confidence: 99%

Antiinflammatory polymer‐bound steroids for topical applications II. Controlled release of the steroids

Khue

Jung

Poindron

1986

J. Polym. Sci. A Polym. Chem.

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Antiinflammatory polymer‐bound steroids for topical applications. I. Synthesis and characterization

Khue¹,

Galin²

1985

J of Applied Polymer Sci

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Covalent binding of hydrocortisone and dexamethasone to hydrophylic biocompatible macromolecular carriers through hydrolizable carbonate linkage was investigated according to two complementary strategies. (a) Radical copolymerization of hydrocortisone‐21C‐vinylcarbonate with N‐vinylpyrrolidone (NVP,60°C), or N‐[tris(hydroxymethyl)methyl]acrylamide (THMMA, 50°C) in dimethylacetamide solution: In spite of a nearly zero reactivity ratio for the steroid monomer which behaves as a degradative transfer agent—CT ∼ 5.7 × 10−2 and 6.8 × 10−3 for NVP and THMMA, respectively–this process may afford fairly high molecular weight polymers (M̄w ≃ 104–105) with high enough hydrocortisone content (0.03–0.10 mole.fraction). (b) Condensation of the hydrocortisone or dexamethasone‐21C‐chloroformates onto poly(oxyethylene glycol) (M̄n = 6220) or hydroxypropylcellulose (HPC, M̄w = 1.35 × 105) in tetrahydrofuran solution (30°C): This straightforward process is of low efficiency (yields >50%), and only HPC derivatives show good chemical homogeneity.

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Recherche de télomères à activité pharmacologique potentielle, 2. Télomères de l'acide acrylique et greffage de composés hydroxylés

et al. 1981

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Several telomers of acrylic acid with carbone tetrachloride were prepared. Their average degree of polymerization, which was between 10 and 50, was determined by several analytical methods (elemental analysis,viscosimetry, and GPC). From the kinetic equations of telomerization a relation between DP, of these telomers and the experimental conditions is established. Fixation of hydroxylic compounds through direct esterification was studied and it was found that the prepared telomers can be used as hydrosoluble carriers for drugs containing primary alcohol or phenol functions.

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Synthèse et polymérisation de polyméthacrylates porteurs de la quinine. Etude comparée de la toxicité et de l'immunogénicité des formes libres et polymériques

Cited by 21 publications

References 8 publications

Antiinflammatory polymer‐bound steroids for topical applications II. Controlled release of the steroids

Antiinflammatory polymer‐bound steroids for topical applications II. Controlled release of the steroids

Antiinflammatory polymer‐bound steroids for topical applications. I. Synthesis and characterization

Recherche de télomères à activité pharmacologique potentielle, 2. Télomères de l'acide acrylique et greffage de composés hydroxylés

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