Research on Preparation of Sodium-Alginate Microsphere and its Release of BSA
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First,the sodium-alginate microsphere was prepared by the condensation phase separation method.Second,the BSA as model drug and sodium-alginate as the investment material were used to prepare the drug-loaded microsphere,while the investment rate of the drug-loaded microsphere was detected.The result showed that sodium-alginate as the investment material had good investment rate and a certain low-release effect on BSA.Keywords:
Sodium alginate
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To investigate the formation mechanism, macromolecular drug loading capacity and release property of alginate-chitosan microcapsules (ACM).ACM was prepared by emulsification-gelation method and its formation mechanism was studied by DSC analysis. Using bovine serum albumin (BSA) as model drug, the drug loading and release properties of the microcapsules on macromolecular drug were investigated.The results of DSC analysis showed that there is electrostatic interaction between materials encapsulated in the microcapsule. With the increase of BSA microcapsule ratio, the BSA loading percentage rose from 9.20% to 35.08%; and with the ascent of chitosan (CTS) concentration, the BSA loading percentage increased from 30.29% to 38.12%. The BSA microcapsules whowed a two-phase release in both 0.1 mol.L-1 HCl and phosphate buffer saline (pH 7.4). With the increase of CTS concentration, the BSA release more and more slowly in 0.1 mol.L-1 HCl.Spheric and well-dispersed alginate-chitosan microcapsules were prepared. The microcapsule showed good loading capacity to BSA as well as sustained release to a certain degree.
Bovine serum albumin
Phosphate buffered saline
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The chitosan sodium alginate microcapsules for injectable usage were prepared by emulsification method. The diameter of microcapsules is less than 200 micron and posses a relative narrow and normal gauss distribution. The loading efficiency of Bovine Serum Album(BSA) in microcapsules is more than 50%. By the coating with chitosan on the surface of sodium alginate microcapsules, the BSA release from microcapsules is extended from several hours to more than half a month.
Sodium alginate
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Double-emulsion gelation method was employed for the preparation of monodispersed calcium alginate microspheres.The effects of experimental conditions such as the concentration of sodium alginate,calcium chloride,emulsifying speed,the volume ration of organic phase to aqueous phase and emulsifier concentration on particle size and morphology were investi-gated.Monodispersed microspheres with ideal spherical in shape and mean diameter of 4μm were obtained under the optimized conditions.Encapsulation efficiency of the model protein BSA in the calcium alginate was about 13%.But when the pH value of the washing liquor was adjusted to 3.2,the BSA encapsulation efficiency was calculated to be 66% with the loading capacity of 16%.Subsequent release characteristics of the BSA from calcium alginate microspheres in vitro were investigated.The release studies showed that the BSA was released at low rate in simulated gastric fluid while a large amount of BSA was released from the microspheres in a short time in simulated intestinal fluid.These results suggest that the double-emulsion gelation is a promising method to prepare alginate microspheres in the development of solid dosage forms for the peroral protein delivery and targeted release.
Calcium alginate
Aqueous two-phase system
Sodium alginate
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The present study deals with formulation of a Sustained-release calcium alginate microbeads containing Diclofenac sodium by the ionotropic gelation technique at various concentrations of sodium alginate and calcium chloride. Prepared microbeads were evaluated for drug entrapment efficiency, drug content, density, flow properties, particle size and in vitrodrug release. The prepared beads were free flowing, white in colour and showed an acceptable range of bulk density, tapped density and angle of repose. Mean diameter of the particles was found to in the range of 350-450 µ. The drug loaded beads showed 83.5 – 95.57 % drug entrapment, which was found to increase with increase in sodium alginate. In vitrodrug release study of these microbeads indicated controlled release for Diclofenac sodium 84.54 – 95.23 % release at the end of 10 h. From this study it is concluded that the calcium alginate microbeads can provide a better carrier system for delivery of drugs.
Diclofenac Sodium
Angle of repose
Sodium alginate
Entrapment
Diclofenac
Calcium alginate
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To develop a multi-unit gastroretentive sustained release dosage form of a water-soluble drug, Verapamil hydrochloride, from a completely aqueous environment. avoiding the use of any organic solvent, thus releasing the drug for a prolonged duration of time. Emulsion gelation technique was used to prepare emulsion gel beads using sodium alginate as the polymer. The gel beads containing oil was prepared by gently mixing and homogenizing oil and water phase containing sodium alginate which was then extruded in to calcium chloride solution. The effects of factors like concentration of oil, drug: polymer ratio and alginate: pectin ratio on drug entrapment efficiency, floating lag time and morphology and drug release was studied. The use of sodium alginate and combinations of sodium alginate and pectin were used to study the effect on the sustaining property of the formed beads. It was found that sodium alginate was not sufficient to sustain the drug release at gastric pH. Instead of it, appropriate combination of alginate and pectin could provide the sustain release of drug. The results show that these beads can entrap even a water soluble drug as Verapamil hydrochloride in sufficient amount and also can successfully deliver the drug in stomach for a prolong duration of time without using any organic solvent and any time consuming step in the preparation.
Pectin
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This project aimed to design nanoparticles-in-beads made of alginate, chitosan and their derivatives as oral insulin carrier. In the first part of the study, the calcium alginate beads were prepared using the vibratory nozzle extrusion microencapsulation technique through concurrent core and coat formation with chlorpheniramine maleate as a model drug. These beads were coated with chitosan/chitosan-oleic acid conjugate of which the latter was synthesized via covalent reaction. The formability of beads was optimized through varying alginate solution concentration, alginate/chitosan solution flow rate and nozzle vibrational frequency. The size, shape, morphology, swelling, erosion, water uptake, drug content, drug release and matrix molecular profiles of beads were characterized. Spherical discrete coated beads were produced through critical interplay of nozzle vibrational frequency and polymeric solution flow rate. The conjugate-coated beads had their swelling and water uptake tendency negated through the introduction of tripolyphosphate ions as a crosslinking agent to attract the conjugate to the alginate core interface for coacervation to take place. The drug release propensity of tripolyphosphate-crosslinked, chitosan-oleic acid conjugate-coated beads was unexpectedly higher than the uncoated beads. This was attributed to reduced drug-alginate interaction as a result of alginate coacervating with chitosan-oleic acid conjugate and loss of calcium alginate crosslinkage to tripolyphosphate species. In the second part of the study, nanoparticles of simple calcium alginate, calcium alginatestearic acid, and calcium alginate-C18 conjugate were prepared by nanospray drying technique…
Conjugate
Coacervate
Calcium alginate
Bead
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Bovine serum albumin
Sodium alginate
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Metformin microspheres with sodium alginate alone and in combination with gellan were prepared using an emulsion-cross linking method. The prepared microspheres were evaluated for their physico-chemical characteristics like particle size, morphology using SEM, incorporation efficiency, equilibrium water content (swelling) and in vitro drug release. The effect of various formulation variables like polymer concentration (sodium alginate; and proportion of gellan in microspheres prepared by a combination of sodium alginate and gellan), drug loading, crosslinking agent concentration and cross-linking time on the in vitro dissolution of the prepared microspheres were evaluated. The results showed that both the particle size and the incorporation efficiency were proportional to the polymer concentration. In case of microspheres containing both sodium alginate and gellan, the mean diameter and the incorporation efficiency were higher than the corresponding microspheres containing only alginate, both increasing with an increase in proportion of gellan. The prepared microspheres were found to be discrete and spherical in shape and were successful in sustaining the drug release for 8 hours. Incorporation of gellan caused a significant decrease in drug release. The release followed a biphasic profile, in all cases, characterized by an initial phase of moderate drug release followed by a phase of higher release. Further, the kinetic treatment of the dissolution data revealed the prevalence of matrix diffusion kinetics.
Gellan gum
Sodium alginate
Microparticle
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The present investigation was to formulate theophylline loaded microspheres using different grade of chitosan, chitosan - sodium alginate and chitosan-albumin by the following methods such as phase separation emulsification, modified ionotropic gelation and heat stabilization method. The prepared microspheres were evaluated in terms of drug content, incorporation efficiency, micromeritic studies, moisture content and in vitro drug release profile. Chitosan –sodium alginate combination produced microspheres with spherical, smooth surface and frees flowing. It exhibited incorporation efficiency above 75% and size range between 999-994 μm. The drug release from the microspheres follows first order kinetics and the mechanism is Higguchi’s diffusion. Theophylline loaded microspheres prepared from Chitosan–sodium alginate combination exhibited good sustained release characteristics and was found suitable for chronic obstructive pulmonary disease (COPD) and nocturnal asthma.
Diclofenac Sodium
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