Partition rate of some nonsteroidal antiinflammatory agents in a three-phase water/n-octanol/water system. Effect of the pH of the first aqueous phase.
Explore the source record for details and available documents.
1-Octanol↗
Biomedical subjects
I Orienti
Publications and source records attributed to I Orienti.
Chemical properties-dissolution of nonsteroidal antiinflammatory drugs. II. Factors affecting the release of NSAID from monoliths.
Explore the source record for details and available documents.
Anti-Inflammatory Agents, Non-Steroidal↗
Preparation and evaluation of polyvinyl alcohol-co-oleylvinyl ether derivatives as tumor-specific cytotoxic systems.
A series of poly(vinyl alcohol) amphiphilic derivatives have been prepared to obtain polymeric aggregates in aqueous phase holding thermodynamic instability. The aim was to evaluate their ability to interact with tumor cells eliciting selective cytotoxicity. The poly(vinyl alcohol) derivatives were prepared by partial substitution of poly(vinyl alcohol) (MW 10 kDa) with both oleyl chains and poly(ethylene glycol) monoethyl ethers (PEGMEE) of different molecular weights. The substitution degree was 1.5% for the oleyl chains and 1% for the PEGMEE chains (moles of substituent per 100 mol of hydroxyvinyl monomer). The polyvinyl derivatives obtained easily dissolved in water. Dynamic and static light scattering measurements on the polymer aqueous solutions indicated the formation of polymeric aggregates characterized by low polydispersity (0.232-0.299) and mean size (218-382 nm) in the range suitable for intravenous administration. Moreover, they were characterized by different packing densities and thermodynamic instabilities driving the polymers to interact with hydrophobic membranes. Among the analyzed polymers, the poly(vinyl alcohol)-co-oleylvinyl ether substituted with triethylene glycol monoethyl ether (P10(4)) provided in solution the highest affinity for hydrophobic membranes. P10(4), moreover, was the most cytotoxic toward the tumor cell lines analyzed (neuroblastoma: SH-SY5Y, IMR-32, HTLA-230. melanoma: MZ2-MEL, RPMI7932.), while it did not appreciably alter the viability of the normal resting lymphocytes. The peculiar behavior of the P10(4) aggregates has been correlated to their high thermodynamic instability in solution due to the high packing density that triggers the polymeric aggregates to interact with hydrophobic membranes such as the tumor cell membranes, thus eliciting cytotoxicity.
Antineoplastic Agents↗
Fatty acid substituted polyvinyl alcohol as a supporting material for microsphere preparation.
Polyvinyl alcohol, substituted with lauric, myristic, palmitic, and stearic acids at different substitution degrees was employed for the preparation of biodegradable microspheres containing progesterone or indomethacin. A solvent extraction/method was followed, starting from an oil-in-water dispersion containing the polymer and drug in the inner phase. Microspheres were obtained with high loading efficiency, whose release properties were dependent on the nature of the acyl substituent and the substitution degree. Kinetics approaching zero-order were obtained for the most hydrophile microspheres such as those based on the least substituted polymers and lowest molecular weight substituents. The hydrophilicity of these systems hindered protein absorption on their surface, suggesting their suitability for parenteral use.
Adsorption↗
Controlled release of vancomycin from freeze-dried chitosan salts coated with different fatty acids by spray-drying.
The aim of this study was to describe a controlled drug release system based on chitosan salts for vancomycin hydrochloride delivery. Chitosan aspartate (CH-Asp), chitosan glutamate (CH-Glu) and chitosan hydrochloride (CH-HCl) were prepared by freeze-drying and coated with stearic, palmitic, myristic and lauric acids by spray-drying technique. Vancomycin hydrochloride was used as a peptidic model drug whose sustained release should minimize its inactivation in the upper part of the gastrointestinal tract. This study evaluated, in vitro, the influence of chitosan salts on the release behaviour of vancomycin hydrochloride from the freeze-dried and spray-dried systems at pH 2.0 and 7.4.
Anti-Bacterial Agents↗
Poly(vinylalcohol-co-vinyloleate) for the preparation of micelles enhancing retinyl palmitate transcutaneous permeation.
The amphiphilic properties of poly(vinylalcohol) substituted with oleic acid was evaluated to assess the possibility to prepare polymeric micelles in an aqueous phase containing a hydrophobic core able to host lipophilic drugs such as retinyl palmitate and thereby enhance its transcutaneous absorption in the stratum corneum. The effect of the increased drug absorption suggests the possibility of interaction between the substituted polymer and the components present in the intercorneocyte spaces. Correlations between the drug concentration in the preparative mixture, micelle size, and drug permeation were evaluated to establish the best functional properties of the micellar systems enhancing retinyl palmitate absorption. Transcutaneous absorption increased with decreasing micelle size, and micelle size decreased on decreasing the drug concentration in the preparative mixture.
Administration, Cutaneous↗
Modified doxorubicin for improved encapsulation in PVA polymeric micelles.
Polyvinylalcohol, partially substituted with lipophilic acyl chains, generates polymeric micelles in aqueous phase, containing a hydrophobic core able to encapsulate lipophilic drugs. Two types of polymers were obtained by conjugation of polyvinylalcohol with oleoyl or linoleoyl chains as pendant groups. The polymers, at a substitution degree of approximately 1%, are soluble in water and form polymeric micelles whose size increases with polymer concentration. Doxorubicin was hydrophobized, by linking an oleoyl chain via amide bond, to make the drug more similar to the substituted polymers and promote its encapsulation into the inner core of the micelles. The properties of the drug-polymer systems were evaluated in solution by dynamic light scattering technique and correlated to the physicochemical characteristics of the drug and the substituted polymers. Solubilization tests revealed that the similarity of the chain, in both the polymer and the drug, promotes better drug encapsulation in the oleoyl than linoleoyl derivative. The drug-polymer systems are stable in phosphate buffer saline (pH 7.4) at 37 degrees C, and the release of the drug is activated by the presence of the proteolytic enzyme pronase-E. The enzyme activated drug release and the size of the polymeric micelles, compatible with the pore dimensions of the tumor vessels, make these systems interesting for targeting lipophilic drugs to solid tumors, where the proteolytic enzyme concentration strongly raises with respect to the other body compartments.
Doxorubicin↗
Crosslinked poly(methyl vinyl ether-co-maleic anhydride) as topical vehicles for hydrophilic and lipophilic drugs.
Poly(methyl vinyl ether-co-maleic anhydride) crosslinked with ethylene glycol (GZ-ET), 1,4-butanediol (GZ-BUT), 1,6-exandiol (GZ-EX), 1,8-octanediol (GZ-OCT), 1,10-decanediol (GZ-DEC) or 1,12-dodecanediol (GZ-DOD) was prepared and employed as a supporting material for aqueous topical gels containing pyridoxine hydrochloride (PYCL) chosen as a hydrophilic model molecule or for O/A emulsion containing beta-carotene chosen as a hydrophobic model molecule. We analyzed the effect of the nature of the crosslinker on the permeation of hydrophilic and lipophilic vitamins through porcine skin by in vitro permeation studies. The vehicles formed by crosslinked poly(methyl vinyl ether-co-maleic anhydride) showed enhanced vitamins permeation with respect to the same vehicles formed by noncrosslinked poly(methyl vinyl ether-co-maleic anhydride) (GZ). The decrease in the crosslinker acyl chain length provides vehicles accelerating the drug permeability through the skin.
Administration, Topical↗
Indomethacin loaded chitosan microspheres. Correlation between the erosion process and release kinetics.
The preparation of chitosan microspheres covalently linked with citric acid and loaded with indomethacin is described. The release kinetics correlated with the concentration of chitosan in the microsphere preparative mixture and the pH of the release medium. Deviations from Fickian to zero order kinetics were observed at higher concentrations of chitosan and at pH 7.4. The variations induced by these parameters on drug diffusion and solubility in the matrix undergoing erosion were analyzed.
Anti-Inflammatory Agents, Non-Steroidal↗
Chitosan microcapsules as controlled release systems for insulin.
This study analyses the use of chitosan for the production of surface crosslinked microparticulate systems containing insulin. The microcapsules were prepared by an innovative technique based on interfacial crosslinkage of different amounts of chitosan solubilized in the inner phase of a water/oil emulsion by means of ascorbyl palmitate. The correlation between the main formulation parameters and the functional properties of the microcapsules were analysed. Insulin is incorporated with high efficiency. The peptide release is constant for appreciable periods of time. The content of chitosan modulates the main physico-chemical properties of the matrix.
Biocompatible Materials↗
Influence of physico-chemical parameters on the release kinetics of ketoprofen from Poly(HEMA) crosslinked microspheres.
This report analyses the release of Ketoprofen from Poly(HEMA) microspheres crosslinked with EGDMA at different crosslinking ratios and loaded by soaking in saturated solutions of the drug. Release appears to be influenced by the dissolution of Ketoprofen in the hydrogel and it is strictly correlated with the diffusibility of the drug in the gelled matrix. The release rate of the drug in the hydrogel rises with the increase in the diffusional conductance and the release kinetics approaches zero order particularly at the higher values of the diffusional conductance.
Cross-Linking Reagents↗
Modulation of the release of naproxen from calcium phosphate monoliths.
Explore the source record for details and available documents.
Calcium Phosphates↗
Laminar flux apparatus for dissolution studies of solid pharmaceutical formulations: a proposal.
Explore the source record for details and available documents.
Chemistry, Pharmaceutical↗
Microparticles of BSA substituted with deoxycholic acid and triethylene glycol glutarate. Correlations between the physico-chemical properties of the matrix and the release kinetics.
Bovine serum albumin or bovine serum albumin covalently linked to deoxycholic acid and triethylene glycol glutarate were used for the preparation of microspheres loaded with indomethacin. The presence of these residues on the bovine serum albumin molecule increased the loading levels. The kinetic analysis of release evidenced a zero order release period from the start of release in the microparticles obtained by bovine serum albumin linked to deoxycholic acid and triethylene glycol glutarate, followed by a decreasing rate release and a first Anomalous period followed by a zero order period in the albumin microparticles. These different release behaviours were correlated to the modifications induced by deoxycholic acid and triethylene glycol glutarate on the drug diffusivity and solubility in the matrix undergoing erosion.
Chemical Phenomena↗