Synthesis and pH-dependent micellization of diblock copolymer mixtures

in Journal of Colloid & Interface Science (2009), 329(2), 235-243

This work focused on the preparation and the aqueous solution properties of hybrid polymeric micelles consisting of a hydrophobic poly(ε-caprolactone) (PCL) core and a mixed shell of hydrophilic poly ... [more ▼]

This work focused on the preparation and the aqueous solution properties of hybrid polymeric micelles consisting of a hydrophobic poly(ε-caprolactone) (PCL) core and a mixed shell of hydrophilic poly(ethylene oxide) (PEO) and pH-sensitive poly(2-vinylpyridine) (P2VP). The hybrid micelles were successfully prepared by the rapid addition of acidic water to a binary solution of PCL34-b-PEO114 and PCL32-b-P2VP52 diblock copolymers in N,N-dimethylformamide. These micelles were pH-responsive as result of the pH-dependent ionization of the P2VP block. The impact of pH on the self-assembly of the binary mixture of diblocks—thus on the composition, shape, size and surface properties of the micelles—was studied by a variety of experimental techniques, i.e., dynamic and static light scattering, transmission electron microscopy, Zeta potential, fluorescence spectroscopy and complement hemolytic 50 test. [less ▲]

Synthesis and pharmacological effects of opened analogues of benzothiadiazine 1,1-dioxides with sulfonylurea moieties on diuresis and glycemia

Poster (2005, May)

Synthesis and pharmacological evaluation of a new targeted drug carrier system: β-Cyclodextrin coupled to oxytocin

in Bioorganic & Medicinal Chemistry Letters (2008), 18

β-Cyclodextrin (β-CD) was monofunctionalized into its carboxylic derivative and then conjugated to the N-side of oxytocin (OT), a nonapeptide involved in human behavior and myometrium contraction. On ... [more ▼]

β-Cyclodextrin (β-CD) was monofunctionalized into its carboxylic derivative and then conjugated to the N-side of oxytocin (OT), a nonapeptide involved in human behavior and myometrium contraction. On isolated rat myometrium, this conjugate (β-CD-OT) partly preserves the contracting activity of OT (EC50 = 0.40 μM vs 1.7 nM). Moreover, the contraction induced frequency is also lowered by β-CD-OT. This novel hydrophilic targeted carrier could form a host–guest complex with prostaglandins and their derivatives used as labor inducers or with anticancer drugs used in cervix and endometrial cancer. This strategy can improve the solubility, the stability, and/or the biological activity of these drugs as well as reducing their side-effects. [less ▲]

Synthesis and pharmacological evaluation of ATP-sensitive potassium channel openers related to cromakalim : introduction of N-methylated and non N-methylated arylsulfonylurea moieties

Poster (2005, May)

Synthesis and pharmacological evaluation of BM-613, an original thromboxane A2 antagonist

Poster (2003, May)

Synthesis and pharmacological evaluation of KATP-channel openers related to cromakalim: introduction of arylsulphonylurea moieties

in Pharmacy and Pharmacology Communications (1999), 5

Synthésis and pharmacological evaluation of original thromboxane A2 receptor antagonists derived from BM-573

in Fundamental & Clinical Pharmacology (2004)

Synthesis and pharmacological evaluation of pyridinic methanesulfonamides as potential COX-2 inhibitors

Conference (2001, May 24)

Synthesis and pharmacological evaluation of some N-arylsulfonyl-N-methyl-N'-(2,2-dimethyl-2-H-1-benzopyran-4-yl)ureas structurally related to cromakalim

in Bioorganic & Medicinal Chemistry (2006), 14

Synthesis and pharmacology of N"-(4-arylaminopyrid-3-yl)sulfonyl-N-cyano-N'-isopropyl-guanidines

in Journal de Pharmacie de Belgique (1995), 50