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PubMedDate not supplied

Combined physical and chemical immobilization of glucose oxidase in alginate microspheres improves stability of encapsulation and activity.

Chemical sensors utilizing immobilized enzymes and proteins are important for monitoring chemical processes and biological systems. In this study, calcium-cross-linked alginate hydrogel microspheres were fabricated as enzyme carriers by an emulsification technique. Glucose oxidase (GOx) was encapsulated in alginate microspheres using three different methods: physical entrapment (emulsion), chemical conjugation (conjugation), and a combination of physical entrapment and chemical conjugation (emulsion-conjugation). Nano-organized coatings were applied on alginate/GOx microspheres using the layer-by-layer self-assembly technique in order to stabilize the hydrogel/enzyme system under biological environment. The encapsulation of GOx and formation of nanofilm coating on alginate microspheres were verified with FTIR spectral analysis, zeta-potential analysis, and confocal laser scanning microscopy. To compare both the immobilization properties of enzyme encapsulation techniques and the influence of nanofilms with uncoated microspheres, the relationship between enzyme loading, release, and effective GOx activity (enzyme activity per unit protein loading) were studied over a period of four weeks. The results produced four key findings: (1) the emulsion-conjugation technique improved the stability of GOx in alginate microspheres compared to the emulsion technique, reducing the GOx leaching from microsphere from 50% to 17%; (2) the polyelectrolyte nanofilm coatings increased the GOx stability over time, but also reduced the effective GOx activity; (3) the effective GOx activity for the emulsion-conjugation technique (about 3.5 x 10(-)(5) AU microg(-)(1) s(-)(1)) was higher than that for other methods, and did not change significantly over four weeks; and (4) the GOx concentration, when compared after one week for microspheres with three bilayers of poly(allylamine hydrochloride)/sodium poly(styrene sulfonate) ({PAH/PSS}) coating, was highest for the emulsion-conjugation technique. As a result, the comparison of these three techniques showed the emulsion-conjugation technique to be a potentially effective and practical way to fabricate alginate/GOx microspheres for implantable glucose biosensor application.

Alginates↗
PubMed2003

Evaluation of microspheres as surrogates for Cryptosporidium parvum oocysts in filtration experiments.

The size and surface characteristics of a surrogate particle and Cryptosporidium parvum oocysts are important in determining the ability of the particle to mimic the behavior of C. parvum oocysts in filtration and particle transport experiments. The zeta potential, hydrophobicity, and filterability of a surrogate particle, 5 microm carboxylated latex microspheres, and oocysts were compared for a variety of solution conditions. C. pervum oocysts had a slightly negative zeta potential (-1.5 to -12.5 mV) at pH 6.7 over a wide range of calcium concentration (10(-6)-10(-1) M), while the fluorescent microspheres were more negatively charged under the same conditions (-7.4 to -50.2 mV). After exposure to 5 mg of C/L of Suwanee River natural organic matter (NOM), the ; potentials of both particles became significantly more negative, with the microspheres consistently maintaining a more negative zeta potential than the oocysts. Alum was able to neutralize the negative zeta potentials of both particles when in the presence of NOM, but nearly twice the dosage was required for the microspheres. NOM also affected the hydrophobicity of the particles by increasing the hydrophobicity of the relatively hydrophilic oocysts and decreasing the hydrophobicity of the relatively hydrophobic microspheres. A bench-scale filtration system removed less microspheres (40.3 +/- 1.5%) than oocysts (49.7 +/- 2.9%) when 0.01 M CaCl2 was supplied as coagulant. After preexposure to 5 mg of C/L of NOM, the removals of both particles declined significantly, and the removals of microspheres (13.7 +/- 1.5%) and oocysts (16.3 +/- 1.5%) were similar. Finally, the removal efficiencies of microspheres and oocysts in the presence of NOM increased to 69.3 +/- 3.5% and 67.7 +/- 6.4%, respectively, when alum was supplied as coagulant at the optimum dosage needed to destabilize the oocysts. These experimental results suggest that microspheres can be used to provide a conservative estimate of oocyst removal in filters containing hydrophilic negatively charged filter media.

Animals↗
PubMed2003

Photocatalytic oxidation using a new catalyst--TiO2 microsphere--for water and wastewater treatment.

Since the suspended TiO2 powder enjoys free contact with UV irradiation in a photoreactor system, it can generally achieve better efficiency than the immobilized TiO2 catalysts. However, the separation and reuse of this catalyst powder from treated water often limit its application in practice. In this study, a new type of TiO2 catalyst called TiO2 microsphere was prepared by a sol-spraying-calcination method, which can easily settle in its aqueous suspensions under gravity. The SEM image of the TiO2 microsphere samples demonstrated that they had an almost spherical shape with a particle size of 30-160 microm, while the XRD analysis indicated that these TiO2 microspheres still had a crystal size of 8.1 nm. Since these TiO2 microspheres had a porous structure with higher specific surface area and pore volume than normal TiO2 powders, they appeared to have strong adsorption ability in its aqueous suspensions. The photocatalytic activity of the TiO2 microspheres was evaluated in the photodegradations of salicylic acid (SA) and sulfosalicylic acid (SSA). The experimental results showed that the reaction rate using the TiO2 microspheres was similar to that using the TiO2 powders in the SA suspensions and even higher than that in the SSA suspensions. Chemical and physical properties of the TiO2 microspheres and powders that are attributed to photoactivity were discussed based on the Langmuir-Hinshelwood kinetic model. The prepared TiO2 microsphere samples were reused in the photooxidation reaction more than 50 times. It was found that there was no significant weakening in their photoactivity and no change in their particle shape. This TiO2 microsphere catalyst can be simply used to conduct an effective photooxidation in its suspension for water and wastewater treatment with ease of recovery from treated water.

Catalysis↗
PubMed1998

Effect of interparticulate interaction on release kinetics of microsphere ensembles.

The release kinetics of microsphere ensembles is complicated by the mutual influence of the microspheres which are entrapped in small compartments such as body cavities. This work focused on the effect of interparticulate interaction on the release kinetics of microsphere ensembles with limited spreading. Experiments and finite element modeling were conducted to investigate diffusional drug release from a single sphere, a monolayer, and multiple layers of microspheres. Poly(methyl methacrylate-co-methacrylic acid) (P(MMA/MAA)) microspheres and azidothymidine (AZT) were used in the experiments. The order of the release rate of AZT from various microsphere populations was observed to be single sphere > monolayer > multiple layers. This evidenced the importance of interparticulate interaction. The finite element simulations elucidated the influence of various factors on the release kinetics of microsphere ensembles including the separation distance, location of the spheres, and the drug accumulation in the medium. Calibration of overall release kinetics for the neighboring effect was proposed on the basis of the spreading factor. Overall release profiles of microsphere ensembles were predicted using the release profiles of individual microspheres at various locations.

Diffusion↗
PubMed2000

Injectable chemotherapeutic microspheres and glioma II: enhanced survival following implantation into deep inoperable tumors.

PURPOSE: Delivery of chemotherapeutics using implantable, biodegradable polymers provides a potentially powerful method of treating brain tumors. The present studies examined the ability of injectable microspheres, formulated to release carboplatin or BCNU for 2-3 weeks, to enhance survival in a rodent model of deep, inoperable glioma. METHODS: Rat glioma (RG2) cells were implanted into the striatum of rats. In a first experiment, the tumors were allowed to grow for 3 days, followed by either no treatment, bolus chemotherapy (100 microg), or implantation of microspheres containing 10, 50, or 100 microg of carboplatin. The microspheres were implanted, via hypodermic injection, directly into the center of the small, 3-day-old tumors. In a second experiment, tumors grew for 8 days prior to treatment with either carboplatin- or BCNU-loaded microspheres. The microspheres were then injected either directly into the center of these larger tumors or into three sites along the perimeter of the tumor. Separate sets of animals received bolus chemotherapy (100 microg) into either the tumor center or around the tumor perimeter. RESULTS: Injection of carboplatin-loaded microspheres into the center of the small 3 day old, tumors produced dose-related increases in survival. When injections of carboplatin- or BCNU-loaded microspheres were made into the center of the larger, 8-day-old tumors, survival was not enhanced. However, when the microspheres were injected along the perimeter of the larger tumors, sustained-release chemotherapy did significantly prolong survival. Bolus chemotherapy was less effective than sustained release chemotherapy. CONCLUSIONS: Together, these data: (1) demonstrate that sustained delivery of chemotherapy in or near the tumor site is superior to equipotent bolus doses in inoperable tumors, (2) demonstrate that injection of sustained release microspheres into the tissue surrounding a growing tumor may provide superior effects over injections directly into the tumor mass, and (3) suggest that this approach may provide a useful means of selectively delivering chemotherapeutics to tumors or portions of tumors that cannot otherwise be treated with conventional surgical approaches.

Animals↗
PubMed1997

Stabilization of 10-hydroxycamptothecin in poly(lactide-co-glycolide) microsphere delivery vehicles.

PURPOSE: The purpose of this study was to investigate the potential of poly(lactide-co-glycolide) (PLGA) microspheres to stabilize and deliver the analogue of camptothecin, 10-hydroxycamptothecin (10-HCPT). METHODS: 10-HCPT was encapsulated in PLGA 50:50 microspheres by using an oil-in-water emulsion-solvent evaporation method. The influence of encapsulation conditions (i.e., polymer molecular weight (Mw), polymer concentration, and carrier solvent composition) on the release of 10-HCPT from microspheres at 37 degrees C under perfect sink conditions was examined. Analysis of the drug stability in the microspheres was performed by two methods: i) by extraction of 10-HCPT from microspheres and ii) by sampling release media before lactone--carboxylate conversion could take place. RESULTS: Microspheres made of low Mw polymer (inherent viscosity 0.15 dl/g) exhibited more continuous drug release than those prepared from polymers of higher Mw (i.v. = 0.58 and 1.07 dl/g). In addition, a high polymer concentration and the presence of cosolvent in the carrier solution to dissolve 10-HCPT were both necessary in the microsphere preparation in order to eliminate a large initial burst of the released 10-HCPT. An optimal microsphere formulation released 10-HCPT slowly and continuously for over two months with a relatively small initial burst of the released drug. Both analytical methods used to assess the stability of 10-HCPT revealed that the unreleased camptothecin analogue in the microspheres remained in its active lactone form (> 95%) over the entire 2-month duration of study. CONCLUSIONS: PLGA carriers such as those described here may be clinically useful to stabilize and deliver camptothecins for the treatment of cancer.

Antineoplastic Agents, Phytogenic↗
PubMed1992

Microencapsulation of solid dispersions: release of griseofulvin from griseofulvin:phospholipid coprecipitates in microspheres.

The preparation, characteristics, and behavior of microspheres of poly(L-lactic acid) (PLA) containing griseofulvin (Gris) or Gris:phospholipid coprecipitates are described. Microspheres were spherical and increased in size from 17 microns (empty) to 30 microns, containing 22% Gris. The release of coprecipitated Gris after 60 min from 146,000 MW PLA microspheres in pH 2.0 buffer at 37 degrees C was twofold greater than that from microspheres containing pure Gris. Also, the release profile from pure Gris microspheres was 25% lower than its dissolution profile, whereas the dissolution and microspheres of Gris coprecipitate suspended in PEG 600 in hard gelatin capsules for 1 week released Gris at levels comparable to the dissolution of coprecipitate. Decreasing the MW of PLA substantially increased the release of Gris from microspheres of coprecipitate after 20 min but insignificantly from microspheres of pure Gris. These findings suggest that microsphere formulation offers some new opportunities in the development of solid dispersions which normally encounter processing difficulties.

Chemical Precipitation↗
PubMed1994

Development and characterization of microencapsulated microspheres.

A process for the coating of polymer microspheres with the same or different polymers and the characterization of these particles is described. Coated microspheres were manufactured from degradable and non-degradable polymers. Several physicochemical methods were used to establish that the particles were fully coated. Polarized light microscopy revealed strong birefringence of coated microspheres resulting in the appearance of Maltese Crosses on coated microspheres. After staining the core and the coating of particles using different fluorescent dyes, the uneven distribution of the dyes in the core and on the surface allows one to verify the coating success. After cutting microspheres using a cryomicrotome we were able to assess the microstructure of the coated microspheres. Electron Spectroscopy for Chemical Analysis (ESCA) was used to determine the surface composition of coated microspheres. Determining the carbon and oxygen content of samples we were able to verify the completeness of the coating procedure. To examine the benefit of coating microspheres, the effect of coating on the release of tetanus toxoid from polylactide microspheres was studied as a possible pharmaceutical application.

Delayed-Action Preparations↗
PubMed2002

Determination of local tissue concentrations of bupivacaine released from biodegradable microspheres and the effect of vasoactive compounds on bupivacaine tissue clearance studied by microdialysis sampling.

PURPOSE: Incorporation of bupivacaine, a short acting local analgesic, into injectable microspheres provides a long acting formulation. Co-incorporation of dexamethasone into the microspheres results in extended activity. The purpose of this study is to compare tissue concentrations of bupivacaine resulting from the two types of microspheres and to determine if the observed sustained tissue concentration of bupivacaine is due to changes in its tissue clearance. METHODS: Microdialysis probes were implanted into rat muscle. Following microsphere injection, bupivacaine tissue concentration was monitored (HPLC-UV), and the tissues histologically examined. The effect of vasoactive compounds on the tissue concentration of bupivacaine, not formulated in microspheres, was monitored. RESULT: Hind muscle histology showed significant granulomatous reactions around the probe and both types of microspheres. A higher, prolonged bupivacaine concentration was observed from microspheres. A higher, prolonged bupivacaine concentration was observed from microspheres with co-incorporated dexamethasone relative to those without dexamethasone. Addition of vasoconstrictors to the perfusate containing bupivacaine resulted in decreased bupivacaine delivery compared to bupivacaine alone, whereas the addition of a vasodilator increased bupivacaine delivery. CONCLUSIONS: The longer lasting effect of microspheres with co-incorporated dexamethasone results from higher, prolonged tissue concentrations of bupivacaine. Dexamethasone, a vasoconstrictor, decreases the clearance rate of bupivacaine from the tissue resulting in a higher, prolonged tissue concentration of bupivacaine.

Animals↗
PubMed2003

Preparation and in vitro/in vivo evaluation of insulin-loaded poly(acryloyl-hydroxyethyl starch)-PLGA composite microspheres.

PURPOSE: The purpose of this study was to develop and evaluate a novel composite microsphere delivery system composed of poly(D,L-lactide-co-glycolide) (PLGA) and poly(acryloyl hydroxyethyl starch) (acryloyl derivatized HES; AcHES) hydrogel using bovine insulin as a model therapeutic protein. METHODS: Insulin was incorporated into the AcHES hydrogel microparticles by a swelling technique, and then the insulin-containing AcHES microparticles were encapsulated in a PLGA matrix using a solvent extraction/evaporation method. The composite microspheres were characterized for loading efficiency, particle size, and in vitro protein release. Protein stability was examined by sodium dodecyl sulfate polyacrylamide gel electrophoresis, high-performance liquid chromatography, and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. The hydrogel dispersion process was optimized to reduce the burst effect of microspheres and avoid hypoglycemic shock in the animal studies in which the serum glucose and insulin levels as well as animal body weight were monitored using a diabetic animal model. RESULTS: Both the drug incorporation efficiency and the in vitro release profiles were found to depend upon the preparation conditions. Sonication effectively dispersed the hydrogel particles in the PLGA polymer solution, and the higher energy resulted in microspheres with a lower burst and sustained in vitro release. Average size of the microspheres was around 22 microm and the size distribution was not influenced by sonication level. High-performance liquid chromatography, sodium dodecyl sulfate polyacrylamide gel electrophoresis, along with matrix-assisted laser desorption/ionization time-of-flight mass spectrometry showed the retention of insulin stability in the microspheres. Subcutaneous administration of microspheres provided glucose suppression <200 mg/dL for 8-10 days with hyperglycemia recurring by day 16. During the treatment, the time points with higher serum insulin level were consistent with a more significant glucose suppression. The microsphere-treated rats also grew virtually at the same rate as normal control until the insulin level declined and hyperglycemia returned. Multiple dosing given every 10 days demonstrated that the pharmacological effect and serum insulin levels from second or third doses were similar and comparable to that of the first dose. CONCLUSION: The AcHES-PLGA composite microsphere system provides satisfactory in vitro and in vivo sustained release performance for a model protein, insulin, to achieve 10-day glucose suppression.

Acrylic Resins↗
PubMed2004

Biodegradable triblock copolymer microspheres based on thermosensitive sol-gel transition.

PURPOSE: The purpose of this study is to design microspheres for sustained protein delivery using thermosensitive, biodegradable tri-block copolymer, poly (D,L-lactide-co-glycolide)-b-poly (ethylene glycol)-b-poly (D,L-lactide-co-glycolide) (PLGA-PEG-PLGA) without using organic solvent. METHODS: Microspheres of the triblock copolymer PLGA-PEG-PLGA were prepared in an aqueous-based method without using methylene chloride (Msp A). This method used the sol-gel transition property of the polymer. The size and morphology of the microspheres were examined by optical microscopy and scanning electron microscopy (SEM). Zinc crystalline recombinant human insulin was incorporated in Msp A as well as in the microspheres of the same polymer prepared by the conventional water-in-oil-in-water (w/o/w) double emulsion method using methylene chloride (Msp B). Insulin release from both microspheres was carried out using high-performance liquid chromatography (HPLC) as well as circular dichroism (CD) spectroscopy of released insulin. FITC-insulin-loaded Msp A and Msp B were observed under confocal microscopy. Both microspheres were injected subcutaneously to SD rats with diabetes induced by streptozotocin. Blood glucose and plasma insulin levels were monitored. RESULTS: Although the insulin release from Msp B exhibited initial burst and incomplete release, Msp A showed significant reduction of initial burst and continuous release over 3 weeks (>85%). CD spectra of released insulin showed that insulin from Msp A preserved its secondary structural integrity, whereas that from Msp B indicated changes in conformation. Confocal microscopy of FITC-insulin-loaded microspheres (both A and B) showed that the observed release profile may be attributed to homogeneous distribution of FITC-insulin within Msp A but inhomogeneiety in Msp B. Both microspheres were injected s.c. to diabetic rats. Whereas Msp B caused a burst effect (hypoglycemia) followed by quick change in blood glucose and insulin level, Msp A exhibited relatively sustained release of insulin and blood glucose level for at least 10 days. CONCLUSIONS: The PLGA-PEG-PLGA microspheres (Msp A) demonstrated continuous release of insulin in vitro and in vivo without serious burst effect and incomplete release, as shown by Msp B.

Animals↗
PubMedDate not supplied

The influence of magnesium stearate on the characteristics of mucoadhesive microspheres.

Microspheres containing the mucoadhesive polymer chitosan hydrochloride, with matrix polymer Eudragit RS, pipemidic acid as a model drug and agglomeration preventing agent magnesium stearate were prepared by the solvent evaporation method. The amount of magnesium stearate was varied and the following methods were used for microsphere evaluation: sieve analysis, drug content and dissolution determination, scanning electron microscopy, x-ray diffractometry, DSC and FTIR spectroscopy. The results showed that average particle size decreased with increasing amount of magnesium stearate used for microsphere preparation. This is probably a consequence of stabilization of the emulsion droplets with magnesium stearate. Higher pipemidic acid content in the microspheres was observed in larger particle size fractions and when higher amounts of magnesium stearate were used. It was also found that these two parameters significantly influenced the dissolution rate. The important reason for the differences in drug content in microspheres of different particle sizes is the diffusion of pipemidic acid from the acetone droplets in liquid paraffin during the preparation procedure. The physical state of pipemidic acid changed from crystalline to mostly amorphous with its incorporation in microspheres, as shown by x-ray diffractometry and differential scanning calorimetry. No differences were observed in the physical state of pipemidic acid and in microsphere shape and surface between different size fractions of microspheres, prepared with different amounts of magnesium stearate. Additionally, no correlation between the physical state of the drug in different microspheres and their biopharmaceutical properties was found.

Acrylic Resins↗
PubMedDate not supplied

Crosslinked chitosan microspheres for encapsulation of diclofenac sodium: effect of crosslinking agent.

Microspheres of chitosan crosslinked with three different crosslinking agents viz, glutaraldehyde, sulphuric acid and heat treatment have been prepared to encapsulate diclofenac sodium (DS). Chitosan microspheres are produced in a w/o emulsion followed by crosslinking in the water phase by one of the crosslinking methods. Encapsulation of DS has been carried out by soaking the already swollen crosslinked microspheres in a saturated solution of DS. Microspheres are further characterized by FTIR, x-RD and SEM. The in-vitro release studies are performed in 7.4 pH buffer solution. Microspheres produced are spherical and have smooth surfaces, with sizes ranging between 40-230 microm, as evidenced by SEM. The crosslinking of chitosan takes place at the free amino group in all the cases, as evidenced by FTIR. This leads to the formation of imine groups or ionic bonds. Polymer crystallinity increases after crosslinking, as determined by x-RD. The method adopted for drug loading into the microspheres is satisfactory, and up to 28-30% w/w loading is observed for the sulphuric acid-crosslinked microspheres, whereas 23-29 and 15-23% of loadings are obtained for the glutaraldehyde (GA)- and heat-crosslinked microspheres, respectively. Among all the systems studied, the 32% GA crosslinked microspheres have shown the sloxvest release i.e. 41% at 420 min, and a fastest release of 81% at 500 min is shown by heat crosslinking for 3 h. Drug release from the matrices deviates slightly from the Fickian process.

Chitin↗
PubMedDate not supplied

Formation of alginate microspheres produced using emulsification technique.

This study investigated the formative process of alginate microspheres produced using an emulsification technique. The alginate microspheres were produced by cross-linking alginate globules dispersed in a continuous organic phase using various calcium salts: calcium chloride, calcium acetate, calcium lactate and calcium gluconate. The size, shape, drug content and Ca2+ content of the microspheres were evaluated. The tack, viscosity and pH of the calcium salt solution and percentage of Ca2+ partitioned into the organic phase were determined. Microscopic examination of the test emulsion at various stages of the emulsification process was also carried out. The propensity of cross-linking reaction was found to be dependent on successful collision between alginate and calcium salt globules. Examination of the characteristics of microspheres indicated that the formed microsphere was a resultant product of alginate globule clustering. The growth propensity of microspheres was promoted by the higher rate and extent of cross-linkage which was governed by the pH, tack and/or Ca2+ content of the cross-linking solution, as well as the dissociation constant and diffusivity of the calcium salt. Overall, the amount of free Ca2+ cross-linked with alginate in the formed microspheres was in the following order: calcium acetate > calcium chloride + calcium acetate > calcium chloride + calcium gluconate; calcium chloride + calcium lactate > calcium chloride. In microencapsulation by emulsification, the mean size of the microspheres produced can be modified by varying the tack, pH and Ca2+ content of the cross-linking solution and through the use of a combination of calcium salts. The shape of the microspheres produced was, nonetheless, unaffected by the physicochemical properties of the cross-linking solution.

Alginates↗
PubMed2004

Cytotoxicity of 5-fluorouracil entrapped in gelatin microspheres.

Gelatin microspheres were prepared by water/oil emulsion polymerization and by cross-linking with glutaraldehyde. For the microsphere preparation procedure, two different gelatin (5 or 10% w/v) and three different glutaraldehyde (5, 0.5 or 0.1% v/v) concentrations were used. The influence of preparation compositions on microsphere recovery, particle size and morphology, swelling and degradation, 5-fluorouracil loading and release, and cytotoxicity were investigated. The concentrations of gelatin and glutaraldehyde influenced the size and surface properties of microspheres. The decrease in gelatin concentration and the increase in glutaraldehyde concentration resulted in the formation of smaller (140.82-71.47 microm for gelatin microspheres with a 5% gelatin content; 297.67-97.44 microm for gelatin microspheres with a 10% gelatin content) microspheres with smoother surface properties. Swelling values were decreased as the amount of glutaraldehyde was increased. In particular, for microspheres with a high glutaraldehyde content (5% v/v), only about 15% were degraded in 12 days, whereas for those with 0.5% (v/v) glutaraldehyde, almost 97% degradation occurred in the same period. The most rapid 5-fluorouracil release was observed from uncross-linked microspheres (about 88% in 4 h), whereas a particular slower release (about 36% in 4 h) profile was obtained for the highly cross-linked ones. Cytotoxicity tests of free and entrapped 5-fluorouracil were carried out with MCF-7 breast cancer cell line. Free 5-fluorouracil produced an immediate effect, whereas entrapped 5-fluorouracil showed a prolonged cytotoxic effect.

Antineoplastic Agents↗
PubMed2004

Effect of different dispersing agents on the characteristics of Eudragit microspheres prepared by a solvent evaporation method.

Eudragit RS microspheres containing verapamil HCl for oral use were prepared using three different dispersing agents: aluminium tristearate, magnesium stearate and sucrose stearate, by a solvent evaporation method. The effects of the type and concentration of the dispersing agents and the inner phase polymer concentration on the size and T63.2%, (the time at which 63.2% of the drug is released) of microspheres were determined by multiple linear regression analysis. The morphology of microspheres was characterized by scanning electron microscopy. The surface of microspheres prepared with sucrose stearate was smoother and non-porous and the drug release from these microspheres was the fastest. When aluminium tristearate or magnesium stearate were used as dispersing agents, the particle size of microspheres became smaller. Increasing amounts of these two dispersing agents led to the accumulation of their free particles onto the surfaces of the microspheres. The drug release from the microspheres was slower than that of the microspheres from sucrose stearate depending on their hydrophobic structures. According to the results of the multiple linear regression analysis among the dispersing agents used, aluminium tristearate showed the best correlation between the examined input (dispersing agent and polymer concentrations) and output (T63.2%. and particle size) variables.

Acrylic Resins↗
PubMed2004

In vitro cytotoxicity of mitoxantrone-incorporated albumin microspheres on acute promyelocytic leukaemia cells.

In the present study, the preparation and characterization of bovine serum albumin (BSA) microspheres and the evaluation of the in vitro cytotoxicity of these microspheres on acute promyelocytic leukaemia (HL-60) cells were described. Mitoxantrone (MTZ)-incorporated microspheres were evaluated for particle size, drug loading, release characteristics and surface morphology. The biological effect of MTZ released from BSA microspheres was determined on an in vitro cultured HL-60 cell line, showing that, after encapsulation, MTZ still retains cytotoxic activity. For this purpose, methyl-thiazol-tetrazolium (MTT) assay was used to evaluate the in vitro cytotoxicity of MTZ-loaded microspheres. Particle size of BSA microspheres was determined between 17.61-20.38 microm and they were smooth and spherical in shape. Encapsulation efficiency of the drug-loaded microspheres was between 22.26-60.50%. For MTZ-containing microspheres, the cell death ratios were greater than 80% for all formulations. This study demonstrate that BSA microspheres were well suited for the controlled release of MTZ and were promising for anti-cancer chemotherapy.

Animals↗
PubMed2005

Tabletted microspheres containing Cynara scolymus (var. Spinoso sardo) extract for the preparation of controlled release nutraceutical matrices.

Controlled release dosage forms based on tabletted microspheres containing fresh artichoke Cynara scolymus extract were performed for the oral administration of a nutritional supplement. Microspheres were prepared using a spray-drying technique; lactose or hypromellose have been chosen as excipients. Microspheres were characterized in terms of encapsulated extract content, size and morphology. Qualitative and quantitative composition of the extract before and after the spray process was determined. Compressed matrices (tablets) were prepared by direct compression of the spray-dried microspheres. In vitro release tests of microparticles and tablets prepared were carried out in both acidic and neutral media. Spray-drying is a good method to prepare microspheres containing the artichoke extract. The microspheres encapsulate an amount of extract close to the theoretical value. Particle size analyses indicate that the microparticles have dvs of approximately 6-7 microm. Electronic microscopy observations reveal that particles based on lactose have spherical shape and particles containing hypromellose are almost collapsed. The hydroalcoholic extract is stable to the microsphere production process: its polyphenolic composition (qualitative and quantitative) did not change after spraying. In vitro release studies show that microparticles characterized by a quick polyphenolic release both in acidic and neutral media due to the high water solubility of the carrier lactose. On the contrary, microspheres based hypromellose release only 20% of the loaded extract at pH 1.2 in 2 h and the total amount of polyphenols is released only after about further 6 h at pH 6.8. Matrices prepared tabletting lactose microspheres and hypromellose microparticles in the weight ratio 1:1 show a slow release rate, that lasts approximately 24 h. This one-a-day sustained release formulation containing Cynara scolymus extract could be proposed as a nutraceutical controlled release dosage form for oral administration.

Administration, Oral↗