Biomedical subjects

V Zecchi

Publications and source records attributed to V Zecchi.

At least 19 recordsLinked to original sources

PubMed2005

Capillary electrophoretic analysis of the antibiotic vancomycin in innovative microparticles and in commercial formulations.

A new fast capillary electrophoretic method has been developed for the analysis of the glycopeptide antibiotic vancomycin in formulations. An electrophoretic run is completed within 3.0 min; fused silica capillaries (100 microm i.d., 8.5 cm effective length and 48.5 cm total length) and a background electrolyte consisting of 12.5 mM, pH 2.5 phosphate buffer are used. The applied voltage is -20.0 kV; samples are injected by pressure (30 mbar x 3 s) at the anodic end of the capillary. The method was successfully applied to innovative controlled release microparticles consisting of a coated albumin core containing vancomycin. A simple procedure has been developed to obtain complete vancomycin extraction from microparticles using a 5% (w/v) sodium dodecyl sulphate aqueous solution. The method has been validated in terms of linearity, precision and accuracy. Good linearity was found in the 0.25-5.00 microg/mL range. Satisfactory precision was obtained, with relative standard deviation values always lower than 3.9%; accuracy was satisfactory, with recovery values between 97.8 and 102.2%. The method is also suitable for vancomycin determination in commercial capsules.

Anti-Bacterial Agents↗

PubMed2005

Chitosan and poly(methyl vinyl ether-co-maleic anhydride) microparticles as nasal sustained delivery systems.

An original dosage form for nasal delivery based on the encapsulation of hydrophilic drug in chitosan-poly(methyl vinyl ether-co-maleic anhydride) (CH-PVM/MA) microparticles prepared by spray-drying technique was developed. Microparticles were characterized in terms of morphology, size, swelling properties, encapsulation efficiency and drug release. The physical state of the drug and the polymer was determined by scanning electron microscopy (SEM) and infrared spectroscopy (IR). Propranolol hydrochloride (PH) was a beta-blocker, used for the treatment of hypertension and was chosen as a model of hydrophilic drug. SEM studies showed spherical particles with smooth surfaces for chitosan hydrochloride (CH-HCl), whereas rather gross surface defects resulted from the incorporation of poly(methyl vinyl ether-co-maleic anhydride) (PVM/MA). In vitro release studies revealed a sustained release of propranolol HCl from microparticles and in particular chitosan hydrochloride provided the lowest release of drug.

Adhesiveness↗

PubMed2004

Polymeric nanoparticles composed of fatty acids and polyvinylalcohol for topical application of sunscreens.

Benzophenone-3 (BZP) or oxybenzone is widely used in many cosmetic formulations, such as sunscreen lotions or emulsions, shampoos and hair sprays. The nature of the vehicle used can enhance or block the percutaneous absorption of UV filter. In this work, we hydrophobically modified polyvinylalcohol 10 000 (PVA) with fatty acids (FAs) to obtain PVA-FA derivatives for the preparation of lipophilic polymeric nanoparticles able to prevent BZP movement towards the skin. Synthesized PVA-FA derivatives were confirmed by H1 NMR. Nanoparticles loaded with BZP were prepared using a solvent extraction method. The particle size was monitored by means of dynamic light scattering measurements. In-vitro skin permeation studies were performed.

Administration, Topical↗

PubMed2003

Effect of chitosan on progesterone release from hydroxypropyl-beta-cyclodextrin complexes.

An inclusion complex composed of progesterone (Prog) and hydroxypropyl-beta-cyclodextrin (HPbetaCD) was prepared by the spray-drying and freeze-drying methods. Prog alone and its inclusion complex with HPbetaCD were incorporated into chitosan by spray-drying and freeze-drying. The inclusion complex was characterized by IR and DSC. The inclusion complex was investigated in solution by phase solubility diagrams and stability constant was determined at pH 7.4 and at different temperatures (10, 25 and 37 degrees C) to obtain the thermodynamic parameters of inclusion. The results indicate that the Prog-HPbetaCD inclusion complex is more water soluble than Prog alone. Release data from all samples showed significant improvement of the dissolution rate of Prog and a controlled release is obtained in the presence of chitosan.

2-Hydroxypropyl-beta-cyclodextrin↗

PubMed2003

Chitosan salts as nasal sustained delivery systems for peptidic drugs.

The aim of this study was to describe a sustained drug release system based on chitosan salts for vancomycin hydrochloride delivery. Chitosan lactate, chitosan aspartate, chitosan glutamate and chitosan hydrochloride were prepared by spray-drying technique. Vancomycin hydrochloride was used as a model peptidic drug, the nasal sustained release of which should avoid first-pass metabolism in the liver. This in-vitro study evaluated the influence of chitosan salts on the release behaviour of vancomycin hydrochloride from the physical mixtures at pH 5.5 and 7.4. In-vitro release of vancomycin was retarded by chitosan salts and, in particular, chitosan hydrochloride provided the lowest release of vancomycin.

Administration, Intranasal↗

PubMed2002

Influence of different chitosan salts on the release of sodium diclofenac in colon-specific delivery.

Chitosan (CH) was dissolved in aqueous solutions containing aspartic, glutamic, hydrochloric, lactic and citric acids to obtain different chitosan salts. Chitosan salts were collected from the solutions by spray-drying and the powders obtained were mixed with Sodium Diclofenac (SD), taken as a model anti-inflammatory drug. This study evaluated in vitro the influence of acid type on the release behaviour of SD from the physical mixture during gastrointestinal transit. The physical mixture of the chitosan salts with SD provided slower drug release than the pure drug both in acidic and alkaline pHs. In addition, the interaction with beta-glucosidase at pH 7.0 enhanced the release rate. Among the CH salts used, glutamic and aspartic salts provided the best control of release.

Algorithms↗

PubMed2002

Hydrogels formed by crosslinked poly(vinyl alcohol) as sustained drug delivery systems.

Poly(vinyl alcohol) was crosslinked with ethylene glycol diglycidyl ether to obtain hydrogel-forming polymers. The polymers were also substituted with oleoyl chloride, providing hydrogels with weak solubility. These new polymeric materials were evaluated for the formulation of sustained drug delivery systems. Vancomycin hydrochloride was used as a peptidic model drug whose sustained release should minimize its inactivation in the upper part of the gastrointestinal tract. Spray-dried mixtures of the drug and the polymer [at 1:4 and 1:8 (w:w) ratios] were prepared and the release of the drugs from the mixtures was evaluated in vitro at pH 2.0, 5.5, 7.4, and 8.0. The results indicated that the crosslinked polymers slowed down the release of the drugs with respect to the pure drug at each pH. The degree of crosslinking of ethylene glycol diglycidyl ether and the extent of substitution with oleoyl chloride were found to influence drug release.

Anti-Bacterial Agents↗

PubMed2002

Physically cross-linked chitosan hydrogels as topical vehicles for hydrophilic drugs.

Physically cross-linked chitosan hydrogels with lauric, myristic, palmitic or stearic acid were prepared by freeze-drying and have been studied for topical use. This study selected propranolol hydrochloride as a hydrophilic model drug to design a transdermal delivery system. We evaluated the effect of the nature of the cross-linker on drug permeation through porcine skin and the main permeation parameters (diffusion coefficient, flux and lag time) were calculated. All the chitosan hydrogels analysed provided more transcutaneous permeation of propranolol hydrochloride than the corresponding solution of the commercial drug. Among the different chitosan vehicles, chitosan-laurate and chitosan-myristate hydrogels enhanced lyophilised drug diffusion through the skin with respect to chitosan-palmitate and chitosan-stearate hydrogels. This can been explained by the interaction of the hydrogels with the stratum corneum, increasing the solubility of the drug in the skin.

Administration, Cutaneous↗

PubMed2001

Self-assembling poly(vinyl alcohol) derivatives, interactions with drugs and control of release.

The self-assembling properties of poly(vinyl alcohol) substituted with 2-hydroxypropyltrimethylammonium and with acyl chains of different molecular weights (butyryl, capryloyl, lauroyl, or myristoyl) were evaluated to assess the conditions favoring interaction with a poorly soluble drug such as indomethacin to increase its availability. To evaluate the effect of drug-polymer interactions on the solubility of the drug, phase-solubility diagrams were obtained from each substituted polymer at pH 2.0, 5.5, and 7.4 in the presence of indomethacin. To evaluate the availability of the free drug in solution, release profiles of the free drug from drug-polymer physical mixtures were obtained by a dissolution-diffusion apparatus containing a dialysis membrane allowing diffusion of the free drug towards a receiving phase where its concentration was determined over time. The phase-solubility diagrams revealed increasing drug solubility on increasing the polymer concentration. The drug-polymer affinity was slightly increased by lengthening the chain of the substituent on the polymer and was strongly increased by raising the pH of the aqueous phase. The thermodynamic evaluation of the drug-polymer interactions indicated that the interaction is enthalpically driven while the increase in drug-polymer affinity with increasing chain length could be attributed to an entropic contribution. The free drug availability from the drug-polymer systems increased on enhancing the drug-polymer affinity because it corresponded to an increase in the solubilizing effect of the polymer on the drug.

Delayed-Action Preparations↗

PubMed2001

Hydrogels formed by cross-linked polyvinylalcohol as colon-specific drug delivery systems.

Polyvinivlalcohol (PVA, of different molecular weights was cross-linked with succinyl, adipoyl, or sebacoyl chloride to obtain hydrogel-forming polymers and to determine their suitability as colon-specific drug delivery systems. Diclofenac sodium, propranolol hydrochloride, and vitamin B6 hydrochloride were used as hydrophilic model drugs with colon-specific release that should yield high concentrations in the large intestine, minimizing release in the upper part of the gastrointestinal tract. Spray -dried mixtures of the drugs and the polymer (at a 1:2 w/w ratio) were prepared, and the release of the drugs from the mixtures was evaluated in vitro at pH 2.0, 5.5, and 7.4. The results indicated the ability of the cross-linked polymers to slow the release of the drugs analyzed with respect to the pure drug dissolution at each pH. The lengthening of the cross-linker acyl chain was noted to decrease drug release further.

Algorithms↗

PubMed2000

Crosslinked polyvinylalcohol hydrogels as vehicles for hydrophilic drugs.

Polyvinylalcohol crosslinked with succinyl, adipoyl, or sebacoyl chloride at two different degrees of crosslinking was prepared and employed as a supporting material for aqueous topical gels containing propranolol hydrochloride, which was chosen as a hydrophilic model drug suitable for transdermal delivery. We analysed the effect of the nature of the crosslinker and the degree of crosslinking on drug permeation through porcine skin by means of the permeation parameters obtained from the gels and the corresponding aqueous solution. The gels showed greater drug permeation than the liquid solution due to an increase in drug solubility in the skin. Increasing degree of crosslinking and decreasing crosslinker acyl chain length in the gel enhance the drug permeability through the skin.

Administration, Topical↗

PubMed1999

Complexation of ursodeoxycholic acid with beta-cyclodextrin-choline dichloride coprecipitate.

The inclusion complexes of ursodeoxycholic acid (UDCA) with beta-cyclodextrin (betaCD) coprecipitated with choline dichloride (CDC) or beta-cyclodextrin were investigated to evaluate the effect of the presence of choline for UDCA inclusion in betaCD. The inclusion complexes were investigated in solution by phase solubility diagrams and 1H NMR spectrometry and in solid state (kneading, freeze-drying, sealed heating and spray-drying) by DSC, SEM, HSM, XRD and IR spectroscopy. Stability constants were determined at pH 5.5 and 7.0 to simulate the environmental pH of the first intestinal tract and at different temperatures (25, 30 and 37 degrees C) to obtain the thermodynamic parameters of inclusion. Both betaCD-CDC and betaCD increased the water solubility of UDCA particularly betaCD-CDC. All complexes showed a high dissolution rate particularly the spray-dried complexes obtained in the presence of betaCD-CDC.

Calorimetry, Differential Scanning↗

PubMed1998

Controlled insulin release from chitosan microparticles.

This study deals with the production of chitosan microparticles containing insulin by interfacial crosslinkage of chitosan solubilized in the aqueous phase of a water/oil dispersion in the presence of ascorbyl palmitate. The use of ascorbyl palmitate as interfacial crosslinker is based on its amphiphilic properties allowing its disposition at the water/oil interface of the preparative dispersion, thus permitting covalent bond formation with the amino groups of chitosan when its oxidation to dehydroascorbyl palmitate takes place during microparticle preparation. This preparation method produced microparticles characterized by high loading levels of insulin, completely releasing the drug in about 80 h at an almost constant release rate as determined by spectrophotometric and spectrofluorimetric methods. In contrast, the replacement of ascorbyl palmitate by dehydroascorbyl palmitate provided microparticles incompletely releasing the incorporated drug and characterized by a non-constant release rate over time due to the higher lipophilicity of dehydroascorbyl palmitate which hinders its disposition at the water/oil interface and thus decreases the crosslinking efficiency and increases the lipophilicity of the microparticle surface. The efficiency of the spectrofluorimetric and spectrophotometric methods used for determination of the stability and release of the insulin from the chitosan microparticles is also discussed.

Ascorbic Acid↗

PubMed1998

Substituted poly(methyl vinyl ether-alt-maleic anhydride) for the release control and targeting of methotrexate.

Poly(methyl vinyl ether-alt-maleic anhydride) substituted with cholamine (CA), aminoethylcholamine (AECA), or aminooctylcholamine (AOCA) at different substitution degrees, were used for methotrexate (MTX) complexation. The solid complexes, isolated by precipitation from the preparative mixture, showed lower fractional releases at pH 7.4 than at 5.5. This was ascribed to the establishment of ionic interactions between the ionized carboxyls of both the polymer and the drug and the quaternary ammonium groups of the substituents (CA, AECA, AOCA) inducing polymer self-aggregation and thus complex stabilization. The fractional release in pH 7.4 decreases with the increase in the substitution degree until a minimum characteristic for each substituent analyzed is reached and then rises with the increase in substitution degree. The minimum release at pH 7.4 was observed in the presence of AECA at the degree of substitution corresponding to 0.35 mole of substituent per mole of dimer (methyl vinyl ethermaleic anhydride). None of the substituted polymers studied had any haemolytic effect, indicating good biocompatibility.

Animals↗

PubMed1991

Release of ketoprofen from dermal bases in presence of cyclodextrins: effect of the affinity constant determined in semisolid vehicles.

We describe a method to determine the affinity constant values between Ketoprofen and beta-cyclodextrin and hydroxypropyl-beta-cyclodextrin in semisolid vehicles. The method is based on the diffusion of the drug, released from semisolid vehicles, through a lipidic non porous membrane. The affinity constants of Ketoprofen towards cyclodextrins as determined in semisolid media better represent the release of the drug from dermal bases than the corresponding values in aqueous systems.

Chemical Phenomena↗

PubMed1991

Chemical properties-dissolution relationship. IV. Behaviour in solution of the diclofenac/N-(2-hydroxyethyl) pyrrolidine salt (DHEP).

The behaviour in solution of the salt formed between diclofenac and N-(2-hydroxyethyl) pyrrolidine (DHEP) was examined. This salt is more soluble and dissolves more rapidly than sodium diclofenac and tends to give rise to supersaturated solutions, that only slowly evolve to equilibrium. Above 35 mM of DHEP, the solutions show unexpected solubilization ability towards sparingly soluble materials. The faster plasma level found, when DHEP is administered per os, can be associated to this weak detergency. These properties make DHEP a suitable pharmaceutical form to prepare extemporary solutions for short term analgesic therapy.

Diclofenac↗

PubMed1991

Diffusion of naproxen in presence of beta-cyclodextrin across a silicone rubber membrane.

The diffusion of Naproxen through a silicone rubber membrane has been studied for four different release systems: solution and suspension both of Naproxen and Naproxen beta-cyclodextrin coprecipitates. Differences in transport between the two forms indicate the existence of an interaction between the acid and beta-cyclodextrin in solution. Independence of the transport on pH in the case of the coprecipitate indicates rapid liberation of Naproxen from the complex prior to entering the membrane. Increase in the cumulative amount diffused for the suspension of Naproxen with increasing pH was interpreted as due to an increase in its solubility with increasing pH.

Cyclodextrins↗

PubMed1991

Controlled release of hydrocortisone acetate from dermal bases.

The effect of the complexation with beta-cyclodextrin, hydroxypropyl beta-cyclodextrin and polyvinylpyrrolidone on the diffusion kinetics of hydrocortisone acetate through a non porous lipidic membrane was analyzed starting from different dermal bases: a Carbopol gel and lanovaseline. A constant diffusive gradient was achieved; this suggests that the complexation equilibrium controls the diffusable form, according to its stability constant. The following sequence was observed for the cumulative amount diffused: hydrocortisone acetate greater than hydrocortisone acetate/polyvinylpyrrolidone greater than hydrocortisone acetate/hydroxypropyl beta-cyclodextrin greater than hydrocortisone acetate/beta-cyclodextrin. Such behaviour was analyzed in terms of the main physical chemical parameters of the systems examined.

Acrylic Resins↗