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Biomedical subjects

U Conte

Publications and source records attributed to U Conte.

At least 19 recordsLinked to original sources
PubMed2006

Matrices containing NaCMC and HPMC 1. Dissolution performance characterization.

In this study hydroxypropylmethylcellulose (HPMC) and sodium carboxymethylcellulose (NaCMC) were used as polymeric carriers to improve controlled release performances of matrix tablets containing a soluble drug. The drug release behaviour of the systems containing these two polymers mixture and each material separately was investigated. To evaluate the effect of the dissolution medium pH, on the drug release performance, release tests were conducted at pH 1, 4.5 and 6.8. In vitro release studies demonstrated that the mixture of the two cellulose derivatives enables a better control of the drug release profiles at pH 4.5 and at 6.8 both in term of rate and mechanism. Texture analysis on the swollen tablets helps to understand drug release kinetic and mechanism. In fact, the results obtained confirm that a gel, which is characterized by high strength and consistence is less susceptible to erosion and chains disentanglement and the drug release mechanism is mainly governed by diffusion. On the contrary, gels, which show a low strength and texture, have low resistance to the fluid erosion action and the release of the active molecule is manly due to polymer relaxation and chains disentanglement moving the drug delivery kinetic towards an erosion/relaxation mechanism.

Carboxymethylcellulose Sodium↗
PubMed2005

Preparation and evaluation of release characteristics of 3TabGum, a novel chewing device.

A new chewing gum device in the form of a three layers tablet (3TabGum) has been developed. The new drug delivery system is obtained, at room temperature, by direct compression using conventional pharmaceutical equipment. Basically, the resulting chewing gum tablets comprise a gum core combined with two protective antiadherent external layers, which prevent gum adhesion to the punches of the tableting machine. Drug release from a dosage form is the critical step in drug absorption and bioavailability, thus an experimental protocol has been designed to evaluate the efficiency of this kind of therapeutic system by verifying its capability to release the drug dose and by assessing the delivery rate. Simple diffusion into the medium causes the release of only a small percentage of the drug contained in the medicated chewing gum, while the delivery of the major part of the dose occurs during mastication. The results obtained in this study suggest that water soluble drugs are freely and easily released by chewing gums, while for actives characterized by reduced water solubility the release rate depends on the chewing time although all the drugs tested are completely released after a reasonable mastication time.

Chewing Gum↗
PubMed2004

Polymers-gamma ray interaction. Effects of gamma irradiation on modified release drug delivery systems for oral administration.

The aim of this work is to verify the efficiency of two kinds of matrix tablets formulations containing PEO or PVA as retarding polymer. Moreover, since in the last years the exposure to ionizing radiation is a more and more used method to reduce bacterial charge in pharmaceutical products, the effects of gamma irradiation on these two kinds of polymers has been evaluated. The study is performed on matrix tablets containing diltiazem HCl, as model drug, and polyethylene oxides (PEO) of two different molecular weights or polyvinylalchool (PVA) of medium degree of hydrolysis, as drug release modulators. Dissolution of the matrices, release of diltiazem and morphological behaviour of the samples, before and after exposure to increasing doses of gamma irradiation, are investigated in order to verify their stability. The results show that the ionizing radiation does not modify significantly the dissolution trend of the PVA samples; on the contrary, the dissolution and the morphological behaviour of the PEO matrices is strongly affected by the radiation dose received. In particular, the dissolution rate of the irradiated PEO tablets dramatically increases as a function of the irradiation dose and the swelling process, which characterised the non-irradiated PEO samples, was replaced by a rapid erosion process responsible for the quickly dissolution of the matrices. The changes of the dissolution and morphological PEO tablets performances could be explained by a breaking of the polymeric chains (shown by EPR studies) as a consequence of the exposure to gamma rays. These chemical-structural modifications of the polymers are responsible for the reduced efficacy of the PEO systems in controlling the drug release rate.

Administration, Oral↗
PubMed2003

Chemical and physical stability of hydroxypropylmethylcellulose matrices containing diltiazem hydrochloride after gamma irradiation.

In recent years, the exposure to gamma-radiation is an increasingly used method to sterilize or to reduce bacterial charge in drug-delivery devices. The aim of this study was to investigate whether the ionizing radiation may be responsible for drug inactivation or for the alteration of the functional excipient used to modulate drug release from a controlled-release delivery system. In this work, we investigated the physical and dissolution stability of prolonged release matrix tablets containing diltiazem hydrochloride, as a model drug, and hydroxypropylmethylcellulose (HPMC) of two different viscosity grades, as the retarding polymer, before and after exposure to increasing doses of gamma-rays. The results show that gamma-irradiation induces chemical modifications in the structure of the active agent, and also of the hydrophilic polymer. The electronic paramagnetic resonance analysis of gamma-irradiated diltiazem has afforded evidence of carbon radicals stemming from C-H bond ruptures and sulphur radicals, the latter being formed mainly after admission of air at room temperature. The major radical products in the HPMC polymer radiolysis have been reckoned with chain scission events in agreement with the results of viscosity measurements that show a progressive decrease of the average molecular weight with increasing the radiation dose. The elaboration of the viscosity data has led to linear relationships between the eta(o)/eta ratio and the radiation dose D which were rationalized with the following equation under the assumption of a Mark-Houwink Sakurada coefficient a approximately equal 1: eta(o)/eta = (1 + uy(o) D)(a). In this equation, D is gamma-radiation dose, eta(o) and eta are the reduced viscosities before and after the irradiation respectively, u is the number average degree of polymerization, and y(o) is the chain scission radiolytic yield. From the linear relationships G(chain scissions) = 1.2 x 10(-6) and 1.4 x 10(-6) moles/J have been obtained for the two HPMC polymer samples M100 and M4 of different molecular weight used in the experiments. These changes could be responsible for the alteration of the drug-release mechanism and reduced polymer efficacy in controlling drug release.

Chemistry, Pharmaceutical↗
PubMed2003

Photostability of extended-release matrix formulations.

The photostability of drugs has been widely studied while less attention is devoted to the possible modifications that UV light may induce on the excipients of a dosage form, in particular, on the functional polymers used to modulate drug delivery. In this work we have evaluated the effect of UV light on the release characteristics of extended-release matrix tablets containing hydroxypropylmethylcellulose (HPMC) or polyethylene oxide (PEO) as retarding polymers. Two different model drugs have been used: nifedipine (insoluble and photolabile drug) and diltiazem (soluble and photostable drug). Photodecomposition of nifedipine was evaluated and the formation of the photoproducts was followed during the dissolution process. Regarding the dissolution stability, the matrix tablets containing HPMC exposed to UV light have not shown significant differences in drug release profiles compared to the same non-irradiated formulation, while the matrix tablets containing PEO and exposed to the same conditions of UV light have shown a remarkable increase of drug release rate within the first minutes of the dissolution test (burst effect) which is particularly critical because it can cause the loss of the desired therapeutic control.

Chemistry, Pharmaceutical↗
PubMed2002

Boar semen controlled delivery system: storage and in vitro spermatozoa release.

Swine spermatozoa were encapsulated in barium alginate and protamine-barium alginate membranes to lengthen their preservation time and to provide a means of controlling their release. Precocious acrosome reactions and secondary anomalies were measured as indices of semen quality. These characteristics were observed for two forms of encapsulated spermatozoa when stored at 18 and 38 degrees C for 24 h and for semen diluted in a classical extender at both temperatures. The results indicate that encapsulation enhances semen preservation, providing protection against membrane damage upon dilution. The effect is even more evident at the higher temperature (38 degrees C), where cell metabolism is higher. An in vitro release test of spermatozoa showed a massive cell delivery from barium alginate capsules within 6 h, and a slow release from protamine-barium alginate capsules. The properties of spermatozoa 24 h after release did not differ from the semen stored at the same temperature in capsules, indicating that the release process does not impair semen quality.

Alginates↗
PubMed2002

Boar semen controlled delivery system: analysis of batch seasonal variability.

A new encapsulation technology of swine semen is proposed to improve the quality of stored spermatozoa and to obtain the controlled release of viable cells, reducing the number of instrumental inseminations. This technology has been employed to produce barium alginate gel capsules in different seasons; an analysis of batch reproducibility was performed, and total capsule diameter, gel thickness and weight of capsules were determined as indices of batch properties. A seasonal variability was found but each batch was substantially homogeneous. The variability could be related to the biological variability of the semen employed as raw material as well as to the technological process.

Animals↗
PubMed2002

Barium alginate cell-delivery systems: correlation between technological parameters.

The most recent trends for the development of several in vitro cell cultures have been oriented towards the cell immobilisation in 3-dimensional scaffolds and cell encapsulation. In fact, an important requirement of cell survival is self-assembly in functional communities, in the presence of an artificial extracellular matrix. In our research, a previously described technique for spermatozoa encapsulation was applied to obtain capsules loaded with an opaque agent as a model, and to perform a formulative study. A process variable, barium ion concentration, was correlated to some capsule properties, such as weight, gel thickness, total and core diameter. Ion concentration can be modified to obtain capsules with predictable characteristics.

Alginates↗
PubMed2002

Dissolution behaviour of hydrophilic matrix tablets containing two different polyethylene oxides (PEOs) for the controlled release of a water-soluble drug. Dimensionality study.

Hydrophilic matrix tablets containing polyethylene oxides as the retarding polymer have been successfully employed in the controlled release of drugs. To evaluate the relative influence of drug diffusion and polymer erosion mechanisms in the drug delivery process, we studied the hydration behaviour of matrix tablets containing a water-soluble drug and PEOs of two different molecular weights: Polyox WSRN 1105 (Mw = 0.9 x 10(6)) and Polyox WSRN 301 (Mw = 4 x 10(6)). The hydration rate, the extent of swelling, and the erosion rate of matrices containing the polymer, the drug and tableting excipients were evaluated in comparison to tablets made of pure polymer. The results of these studies on function of the release behaviour were then discussed. The results show that the higher molecular weight PEO swells to a greater extent and tends to form, upon hydration, a stronger gel, which is therefore less liable to erosion, if compared to the lower molecular weight PEO. This difference in the erosion behaviour can explain the different efficiencies of the two polymeric products in modulating the delivery rate of the water-soluble drug. Moreover, the presence of other soluble components (drug and excipients) in the dosage form enhances the erosion trend of the tablets with a consequent reduction of the efficiency of the polymer in drug release control.

Biocompatible Materials↗
PubMed2002

Characterization and selection of vaginal Lactobacillus strains for the preparation of vaginal tablets.

AIMS: To characterize and select Lactobacillus strains for properties that would make them a good alternative to the use of antibiotics to treat human vaginal infections. METHODS AND RESULTS: Ten Lactobacillus strains belonging to four different Lactobacillus species were analysed for properties relating to mucosal colonization or microbial antagonism (adhesion to human epithelial cells, hydrogen peroxide production, antimicrobial activity towards Gardnerella vaginalis and Candida albicans and coaggregation with pathogens). The involvement of electrostatic interactions and the influence of bacterial metabolic state in the binding of lactobacilli to the cell surface were also studied. Adherence to epithelial cells varied greatly among the Lactobacillus species and among different strains belonging to the same Lactobacillus species. The reduction in surface negative electric charge promoted the binding of several Lactobacillus strains to the cell membrane whereas lyophilization reduced the adhesion capacity of many isolates. The antimicrobial activity of lactobacilli culture supernatant fluids was not directly related to the production of H2O2. CONCLUSIONS: Three strains (Lactobacillus brevis CD2, Lact. salivarius FV2 and Lact. gasseri MB335) showed optimal properties and were, therefore, selected for the preparation of vaginal tablets. The selected strains adhered to epithelial cells displacing vaginal pathogens; they produced high levels of H2O2, coaggregated with pathogens and inhibited the growth of G. vaginalis. SIGNIFICANCE AND IMPACT OF THE STUDY: The dosage formulation developed in this study appears to be a good candidate for the probiotic prophylaxis and treatment of human vaginal infections.

Bacterial Adhesion↗
PubMed2001

Emulsion spray-drying for the preparation of albumin-loaded PLGA microspheres.

The purpose of this work was to study the encapsulation of bovine serum albumin (BSA) in polylactide-co-glycolide (PLGA) microspheres using an emulsion/ spray-drying method. Albumin was dissolved in an aqueous phase (w) in the presence of surfactant and emulsified in an organic phase containing the polymer (o). To stabilize the emulsion, different types of surfactant (Pluronic F68, Pluronic F127, sodium oleate, dioctylsulfosuccinate) were added to the aqueous phase. The w/o emulsion was spray-dried to obtain BSA-loaded PLGA microspheres. The effect of type of surfactant on microsphere characteristics was evaluated. The microspheres were characterized for their morphology by scanning electron microscopy (SEM) and granulometric analysis; drug content determination and in vitro dissolution tests were performed. Results showed that the emulsion/spray-drying method is suitable for obtaining small microparticles (2-5 micron) characterized by high drug payloads (70%-80% encapsulation efficiency). The type of surfactant affects the microsphere shape and BSA release

Animals↗
PubMed2000

High molecular weight polyethylene oxides (PEOs) as an alternative to HPMC in controlled release dosage forms.

High molecular weight polyethylene oxides (PEOs) have recently been proposed as an alternative to hydroxypropylmethylcellulose (HPMC) in controlled release matrix tablets. In this study, we compared the performance of PEO and HPMC polymers when employed in the Geomatrix technology, a versatile, well-known method to achieve extended release of drugs at a constant rate. Four core formulations were prepared, containing a soluble drug (diltiazem) and, alternatively, PEO or HPMC of two different viscosity grades. These formulations have the same composition except for the polymer employed. Similarly, four barrier formulations were also prepared, which only differ in the kind of polymer employed. Three-layer Geomatrix systems were then prepared using these core and barrier formulations. The release profiles of the different three-layer systems obtained were compared, to verify if PEO could efficiently replace HPMC in this type of dosage form. The results show that slower release rates can be obtained from the plain matrices containing HPMC compared to PEO, moreover HPMC, used in the barrier formulations, is generally more efficient in controlling drug release rate in three-layer Geomatrix systems.

Calcium Channel Blockers↗
PubMed2000

Controlled release of swine semen encapsulated in calcium alginate beads.

A quick and successful encapsulation method of swine spermatozoa is described: hydroxypropylmethylcellulose and calcium chloride were added to the sampled ejaculate swine sperm (sperm-rich fraction: creamy white) and then this suspension was dropped into an aqueous solution of sodium alginate. In order to obtain different capsule thicknesses, different calcium chloride concentrations were used. The influence of different formulations on in vitro spermatozoa release behavior and on the mechanical properties has been studied. In vitro sperm kinetics (motility and average velocity) have been determined. The results obtained from motility and average velocity tests of treated seminal material are promising, especially if the difficulty of preservation of swine spermatozoa compared to bovine sperm is considered. The different membranes obtained from the different calcium concentrations have had an influence on mechanical properties and on the release profile of spermatozoa from the capsules, and therefore, it is possible to modulate the release rate of the cells.

Alginates↗
PubMed2000

Technological and biological evaluation of tablets containing different strains of lactobacilli for vaginal administration.

Ten strains of lactobacilli were evaluated for the administration of viable microorganisms to restore the normal indigenous flora in the treatment of urogenital tract infections (UTI) in women. As the strains considered are facultative anaerobes, optimization of the production process was particularly critical to preserve bacterial viability. The microorganisms were formulated in single- and double-layer vaginal tablets. The two layers were characterized by different release properties: one is an effervescent composition that ensures a rapid and complete distribution of the active ingredient over the whole vaginal surface; while the second is a sustained release composition capable of releasing the lactobacilli over a longer period of time. Three different retarding polymers were tested, and all the formulations and tablets were evaluated in terms of technological processability, bacterial viability and stability, and cell adhesion properties of the microorganisms. From the results obtained, three out of ten strains appear particularly suitable for their application in the treatment of UTI. A larger batch of tablets made with a mixture of the three strains was then evaluated, confirming the feasibility of their industrial production and a good bacterial viability in the final dosage form.

Administration, Intravaginal↗
PubMed2000

Enhancement of ursodeoxycholic acid bioavailability by cross-linked sodium carboxymethyl cellulose.

The bioavailability of ursodeoxycholic acid from a new formulation based on drug-loaded cross-linked sodium carboxymethyl cellulose was studied in man. The plasma levels of ursodeoxycholic acid were determined by gas chromatography-mass spectrometry after derivatization and sample purification by solid-phase extraction. Capsules containing the drug/polymer system were prepared and compared with conventional commercial ursodeoxycholic acid capsules after single oral administration using a randomized crossover experimental design. Although the drug/polymer system improved the in-vitro dissolution rate of ursodeoxycholic acid in simulated intestinal fluid, statistical evaluation of the area under the plasma concentration curves indicated no significant difference in the extent of bioavailability between the two formulations (14.93+/-4.43 vs 14.95+/-5.79 microM h; P > 0.2). However, following the administration of the ursodeoxycholic acid/cross-linked sodium carboxymethyl cellulose system with an enteric-coated capsule, the mean area under the plasma concentration curve (27.60+/-10.11 microM h) was significantly higher than that obtained after treatment with the commercially available ursodeoxycholic acid capsule (16.24+/-8-38 microM h; P < 0.05). We concluded that improved intestinal absorption of the drug was obtained with enteric-coated capsules filled with the ursodeoxycholic acid/polymer system. Moreover, the simplicity of the preparation and the non-toxicity of the polymer used as the carrier represented additional advantages of this dosage form.

Adult↗
PubMed1999

Influence of the moisture on the performance of a new dry powder inhaler.

An accelerated stability test was carried out on two prototypes of a new dry powder inhaler (DPI) to verify the influence of moisture uptake on the performance of the device. The prototypes were stored at 40 degrees C and 75% relative humidity (RH) for different storage times and their performance was assessed in terms of emitted dose and respirable fraction (Twin Impinger). At the same time intervals, the water content of the powder contained in the drug reservoir was evaluated using Karl Fischer's method. The respirable fraction was strongly influenced by the moisture content of the powder, on the contrary, the dosing precision and reproducibility is independent of this variable. The results show that a suitable protection from the external environment is necessary to prevent moisture uptake in the powder and the consequent loss of efficiency of the delivery device.

Drug Delivery Systems↗
PubMed1999

Pectin microspheres as ophthalmic carriers for piroxicam: evaluation in vitro and in vivo in albino rabbits.

Microparticulate polymeric delivery systems have been suggested as a possible approach to improve the low bioavailability characteristics shown by standard ophthalmic vehicles (collyria). Purpose of this study was the evaluation of pectin microspheres as delivery system for piroxicam (Px). The microspheres were prepared by a spray-drying technique; their morphological characteristics were investigated by scanning electron microscopy (SEM), and their in vitro release behavior was evaluated in pH 7.0 USP buffer using a flow-through apparatus. Px loaded in the pectin microspheres showed a faster in vitro dissolution rate with respect to solid micronized drug. The precorneal retention of fluorescein-loaded microspheres was evaluated in vivo in albino rabbits: an aqueous dispersion of fluorescent microspheres showed a significantly increased residence time in the eye (2.5 vs. 0.5 h) when compared with a fluorescein solution. In vivo tests in rabbits of dispersions of Px-loaded microspheres also indicated a significant improvement of Px bioavailability in the aqueous humour (2.5-fold) when compared with commercial Px eyedrops. The potential advantages and limitations of this delivery system are discussed.

Animals↗