Polymeric prodrugs, 1. Synthesis by Direct Coupling of Drugs

Pató, János; Azori, M.; Tüdős, F.

doi:10.1002/marc.1982.030030911

Cited by 34 publications

(7 citation statements)

References 3 publications

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“…Although the action mechanism of a polymer prodrug is not clear, it is assumed that its therapeutic effectiveness is governed by the chemical or biochemical release of the drug molecules 1) . Therefore the selection of a suitable carrier with an optimum molecular weight as well as a favourable attachment must be considered.…”

Section: Introductionmentioning

confidence: 99%

Bioactive polymers: Synthesis, release study and antimicrobial properties of polymer bound Ampicillin

Patel

Talpada

et al. 1999

Angew. Makromol. Chem.

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Matrices of poly(styrene‐co‐maleic anhydride) with surface containing functional anhydride groups of different percentage was prepared by solution polymerization. Ampicillin was bound on the surface of this matrix by chemical bonding in organic medium. The amount of Ampicillin chemically bound to the matrix was spectroscopically characterized and the in vitro release rate of Ampicillin in weakly basic medium was established along with the determination of its antimicrobial activity. This prodrug allows a prolonged release (6–8 days) of the drug.

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Section: Introductionmentioning

confidence: 99%

Bioactive polymers: Synthesis, release study and antimicrobial properties of polymer bound Ampicillin

Patel

Talpada

et al. 1999

Angew. Makromol. Chem.

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“…The polymeric carrier 1, an alternating copolymer, applied in the experiments, was prepared as described in ref. 14), and has the same molecular mass (2000).…”

Section: Experimental Partmentioning

confidence: 99%

“…Coupling reaction: It was essentially carried out as described in ref. 14). 500 mg of 1 was dissolved in 12 ml of dry DMF, then 0,3 ml of triethylamine was added.…”

Section: Preparation Of Succinyl-6-aminohwanoyl-~-phenylalanyl-4-nitrmentioning

confidence: 99%

Polymeric prodrugs, 4. IN vitro study of the drug release on a model p‐nitroanilide bound onto polyanionic carrier

et al. 1986

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The process of chymotrypsin catalysed hydrolysis of ~-phenylalanyl-4-nitroanilide (Phe-NNp) residues bound via 6-aminohexanoic acid (c-Ahx) spacer to the polyanionic carrier, poly(N-vinylpyrrolidone-co-maleic acid), was studied. The initial rate of hydrolysis was measured at pH 8 as a function of mole ratio of side chains (-e-Ahx-Phe-NNp) randomly distributed along the backbone. The polyanionic carrier studied shows a pronounced effect on the process, as overall kinetic parameters (kat and G ) of -&-Ahx-Phe-NNp, attached to the polymer, differ significantly from the respective values of the low-molecular-weight substrate analogue, succinyl-&-Ahx-Phe-NNp. Relationship between the side chain content and the kW, /& values, examined in the range of 1 to 20 mol-%, exhibits a saturation-profile. The limiting value of kWt /& (5 * Id 1 * mol-' * s -l ) appeared to be as much as 8-times higher than that of succinylc-Ahx-Phe-NNp. The course of chymotrypsin catalysed hydrolysis of the polymer-substrate bearing 20 mol-% of side chains shows first order kinetics, with the conversion approaching asymptotically 100%. pH dependence of the maximum velocity of hydrolysis (V,), determined in the range 5 -10, shows a maximum at about pH 8. The enzyme activity profile is broadened toward acidic region.

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“…The medical and pharmaceutical applications of MA copolymers are favored by several properties such as: biocompatibility, water solubility, generally well-defined structure, and possibility to vary hydrophilic/hydrophobic balance by proper choice of comonomers or by further chemical reactions on the copolymer. The maleic anhydride ring is versatile, allowing mild reactions with various partners (drugs, proteins, and enzymes) (Scott et al 2006;Pató et al 1982). In the spiroorthocarbonates class, 3,9-divinyl-2,4,8,10-tetraoxaspiro(5.5)undecane (U) is a hydrolysable comonomer containing a hydrolytically cleavable bicyclic acetal linkage.…”

Section: Introductionmentioning

confidence: 99%

In situ preparation of a magnetic composite during functionalization of poly[maleic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro(5.5)undecane] with erythritol

Neamţu¹,

Chiriac²,

Niţă³

et al. 2015

J Nanopart Res

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New magnetic hybrid composites were prepared, in situ, during the functionalization of poly [maleic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro(5.5)undecane] copolymer, by opening the anhydride ring with erythritol and by introducing magnetic nanoparticles into the polymeric matrix. The procedure allows for magnetic nanocomposite preparation. More than that, the new polymeric matrices owing to their suitable and specific functionalities are anticipated to be used for further link of biological molecules via the maleic anhydride moiety and the polyol presence. The hybrid composites are analyzed by infrared absorption spectrometry, dynamic light scattering (DLS), TG-DTG analysis, X-ray diffraction, SEM, TEM, and vibrating sample magnetometry. Examination of the magnetic composites by DLS analysis shows that the material consists mostly of particles with mean sizes between 295 and 342 nm, depending on the magnetite type in synthesis. The obtained results indicate the magnetite encapsulation and the interactions established with the polymeric matrix that lead to carbonyl band shifting in FTIR spectra, composite particle size decreasing, and influence on XRD and magnetic behavior data. The report of magnetization demonstrates that the prepared nanocomposites are superparamagnetic.

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Polymeric prodrugs, 1. Synthesis by Direct Coupling of Drugs

Cited by 34 publications

References 3 publications

Bioactive polymers: Synthesis, release study and antimicrobial properties of polymer bound Ampicillin

Bioactive polymers: Synthesis, release study and antimicrobial properties of polymer bound Ampicillin

Polymeric prodrugs, 4. IN vitro study of the drug release on a model p‐nitroanilide bound onto polyanionic carrier

In situ preparation of a magnetic composite during functionalization of poly[maleic anhydride-co-3,9-divinyl-2,4,8,10-tetraoxaspiro(5.5)undecane] with erythritol

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