Dextran-based hydrogel microspheres obtained in w/o emulsion: preparation, characterisation and in vivo studies.

The cross-linking reaction in w/o emulsions of dextran (DEX) functionalised with methacrylic groups, having or not acid residues in side chain, can be used to easily prepare polysaccharide hydrogel microspheres with properties suitable for drug delivery applications. The formation of a chemical network within the obtained particles was evaluated with FT-IR spectroscopy, whereas morphology and dimensions of the microspheres were investigated with optical and scanning electron microscopy. At the same time, swelling measurements were carried out on freeze-dried particles in different aqueous media simulating biological fluids.

Novel pH-sensitive physical hydrogels of carboxymethyl scleroglucan.

A carboxymethyl derivative of scleroglucan (Scl-CM) with derivatization degree 300 ± 10 was synthesized and characterized by Fourier transform infrared spectroscopy, potentiometer titration, mucus adhesion studies, and rheological measurements. Rheological measurements showed the ability of the polymer to undergo sol-gel transitions even in the absence of salts. Swelling experiments, performed on freeze-dried samples in different media, showed good affinity of these hydrogels toward the aqueous media and a pH-sensitive behavior.

Antiproliferative and cytotoxic activity of extracts from Cistus incanus L. and Cistus monspeliensis L. on human prostate cell lines.

Benign prostatic hypertrophy (BPH) is a common condition in elderly men that impairs quality of life and leads to a number of medical complications. The use of phytotherapeutic compounds in patients with relatively moderate BPH symptoms has been growing steadily. In the present study, acute toxicity of lyophilised aqueous extracts of Cistus incanus L.

Physical carboxymethylscleroglucan/calcium ion hydrogels as modified drug delivery systems in topical formulations.

A carboxymethyl derivative of scleroglucan (Scl-CM) with a 65+/-5% carboxylic group degree of derivatization (DD) was recently synthesized and characterized. Aqueous solutions of the polymer underwent to a sharp transition toward a gel like behaviour in the presence of divalent ions such as Ca(+2). Physical hydrogels with different Scl-CM/Ca(+2) ratios were prepared and characterized for their rheological behaviour.

pH-sensitive hydrogels of dextran: synthesis, characterization and in vivo studies.

pH-Sensitive hydrogels of dextran were synthesized by photochemical cross-linking reaction of methacrylate dextran (DEX-MA) at different derivatization degree, functionalized with acidic residues through reaction with phthalic anhydride. The hydrogels were characterized by FT-IR spectra, swelling measurements, experiments of chemical and enzymatic hydrolyses. The swelling data agreed with the formation of networks having pH-sensitive behaviour.

Inhibition of intestinal motility and secretion by extracts of Epilobium spp. in mice.

Ethanol extracts of the fresh aerial parts of various Epilobium species were tested to elucidate the mechanism of their gastrointestinal activity in animals. The methods of charcoal meal, castor oil-induced diarrhoea, and enteropooling assay were used to evaluate their effect on mouse gut at various dose levels. The extracts were found to have a significant activity in all models.

Effect of a standardized extract of red orange juice on proliferation of human prostate cells in vitro.

A standardized extract of red orange juice (ROE) was shown to inhibit proliferation of fibroblast and epithelial prostate cells. These data suggest that the antiproliferative properties of ROE cannot be ascribed to cytotoxic effect and highlight its potential usefulness in the management of benign prostatic hyperplasia.

Studies on antidiarrhoeal activity of an extract of wine from Jacquez grapes in mice.

The present study was designed to verify the antidiarrhoeal effects of a lyophilized extract of wine from Jacquez grapes (Ord. Rhamnales; Fam. Vitaceae; Sp.

Biological evaluation of a polyvinyl siloxane impression material.

Objectives: The aim of this study was to determine the irritant properties of a new polyvinyl siloxane impression material (Ghenesil, Lascod-Italy) after single application to intact skin of the rabbit.

Methods: The material was evaluated for primary skin irritation according to the UNI EN ISO 10993-10:1996 using three healthy male New Zealand White rabbits. The back of the animals was clipped free of fur and divided into four sites with the same area 24 h before application of the sample.

'In vitro' antioxidant and photoprotective properties and interaction with model membranes of three new quercetin esters.

Quercetin is well known to possess the strongest protective effect against UV light-induced lipoperoxidation. However, the absolute water insolubility of quercetin is a key step that may limit its bioavailability and, thus, its 'in vivo' employment as a photoprotective agent. The aim of the present paper was to evaluate 'in vitro' the antioxidant and photoprotective properties and the interaction with model membranes of three new semisynthetic quercetin derivatives, quercetin-3-O-acetate (Q-ac), quercetin-3-O-propionate (Q-pr) and quercetin-3-O-palmitate (Q-pal), obtained by esterification of the C-3 OH function with an aliphatic side-chain of different length.

Characterization of the effect of Epilobium extracts on human cell proliferation.

We have previously shown that extracts of different Epilobium species, a phytotherapeutic agent used in folk medicine as a treatment for benign prostatic hyperplasia, inhibit proliferation of human prostate cells. The selectivity of this effect was evaluated in four different human cell lines (PZ-HPV-7, normal prostate cells; LNCaP, transformed prostate cells; HMEC, mammary cells, and 1321N1, astrocytoma cells). Different extracts of Epilobium species (E.

Extracts of various species of Epilobium inhibit proliferation of human prostate cells.

This study examined whether various species of Epilobium, a phytotherapeutic agent used in folk medicine as a treatment for benign prostatic hyperplasia, may have an antiproliferative effect in PZ-HPV-7 human prostatic epithelial cells in-vitro. The MTT (3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide) test, [methyl-(3)H]thymidine incorporation into DNA and flow cytometry analysis were used to evaluate cell proliferation. Ethanolic extracts of E.

Recent studies on lonidamine, the lead compound of the antispermatogenic indazol-carboxylic acids.

Lonidamine (LND) or [1-(2,4-dichlorobenzyl)-1H-indazole-3-carboxylic acid] is an anticancer and an antispermatogenic drug whose mechanism of action is still incompletely understood. LND is effective against a number of tumors, including head, neck and breast cancers, probably because of the inhibition of mitochondrial electron transport and the enzyme hexokinase and to the induction of apoptosis. Instead, the antispermatogenic activity of LND appeared to be related not only to its energolytic activity but also to other effects activities such as the inhibition of specific chloride channels in the epididymis and the disruption of the inter-Sertoli-germ cell junctions, leading to premature release of germ cells.

Indazole carboxylic acids in male contraception.

Two new chemical entities, 1-(2,4-dichlorobenzyl)-indazole-3-carbohydrazide and 1-(2,4-dichlorobenzyl)-indazole-3-acrylic acid, were synthesized based on the core structure of lonidamine (1-(2,4-dichlorobenzyl)-indazole-3-carboxylic acid). These compounds apparently exert their effects in the testis by perturbing the Sertoli-germ cell adherens junctions causing germ cell loss from the seminiferous epithelium. Recently completed studies in the rat have demonstrated the efficacy, reversibility, and potential use of these two compounds as oral contraceptives for men.

Interaction of melatonin with model membranes and possible implications in its photoprotective activity.

It is well known that administration of antioxidants represents a successful strategy for preventing the occurrence and for reducing the severity of UV-mediated oxidative damage. Melatonin was recently shown to be an efficacious photoprotective agent. The aim of the present study was to better investigate the interaction of melatonin with model membranes and the possible implications in its photoprotective activity.