Alginate microparticles prepared by spray–coagulation method: Preparation, drug loading and release characterization

Tu, Junpin; Bolla, Srinivasa Rao; Barr, John T.; Miedema, J.; Li, X.; Jasti, Bhaskara

doi:10.1016/j.ijpharm.2005.07.008

Cited by 66 publications

(51 citation statements)

References 15 publications

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“…It exhibits mucoadhesion (Tu et al, 2005;Wittaya-areeku, Kruenate, Prahsarn, 2006;Rowe, Sheskey, Quinn, 2009), biocompatibility, biodegradability (Lee et al, 2006;Florczyk et al, 2011), immunogenicity, thickening properties and the ability to form gels in the presence of multivalent ions (Florczyk et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

Production and characterization of alginate-starch-chitosan microparticles containing stigmasterol through the external ionic gelation technique

Fujiwara

Campos

Costa

et al. 2013

Braz. J. Pharm. Sci.

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Stigmasterol -a plant sterol with several pharmacological activities -is susceptible to oxidation when exposed to air, a process enhanced by heat and humidity. In this context, microencapsulation is a way of preventing oxidation, allowing stigmasterol to be incorporated into various pharmaceutical forms while increasing its absorption. Microparticles were obtained using a blend of polymers of sodium alginate, starch and chitosan as the coating material through a one-stage process using the external gelation technique. Resultant microparticles were spherical, averaging 1.4 mm in size. Encapsulation efficiency was 90.42% and method yield 94.87%. The amount of stigmasterol in the oil recovered from microparticles was 9.97 mg/g. This technique proved feasible for the microencapsulation of stigmasterol.Uniterms: Stigmasterol/ microencapsulation. Microencapsulation. Sodium alginate/drugs coating. Chitosan/drugs coating. Starch/drugs coating. Natural polymers/drugs coating.O estigmasterol, um fitoesterol com diversas atividades farmacológicas, é suscetível à oxidação quando exposto ao ar, calor e umidade. Neste contexto, a microencapsulação é uma forma de proteção contra oxidação, permitindo a incorporação do estigmasterol em diversas formas farmacêuticas e aumentar sua absorção. As micropartículas foram obtidas por gelificação iônica externa, em uma etapa, utilizando como revestimento polímeros naturais de alginato de sódio, amido de milho e quitosana. As micropartículas apresentaram formato esférico com tamanho aproximado de 1,4 mm. O rendimento foi de 94,87% e a eficiência média de encapsulação de 90,42%. A quantidade de estigmasterol no óleo recuperado das micropartículas foi de 9,97 mg/g. O método mostrou-se viável para a microencapsulação do estigmasterol.Unitermos: Estigmasterol/microencapsulação. Microencapsulamento. Alginato de sódio/revestimento de fámacos. Quitosana/revestimento de fámacos. Amido/revestimento de fámacos. Polímeros naturais/ revestimento de fámacos.

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Section: Introductionmentioning

confidence: 99%

Production and characterization of alginate-starch-chitosan microparticles containing stigmasterol through the external ionic gelation technique

Fujiwara

Campos

Costa

et al. 2013

Braz. J. Pharm. Sci.

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“…Alginate is a linear copolymer made up of β-Dmannuronic acid and α-L-guluronic acid in different configurations (22,23). The carboxyl groups present on the alginate molecule is responsible for its pH-sensitive nature (23).…”

Section: Introductionmentioning

confidence: 99%

“…The carboxyl groups present on the alginate molecule is responsible for its pH-sensitive nature (23). Contact with a multivalent ion such as calcium results in instantaneous gelation (22). This gelation process can be explained through the egg-box model, where the carboxylic acid groups of two adjacent alginate molecules are bound by the multivalent ion (22,24).…”

Section: Introductionmentioning

confidence: 99%

“…Contact with a multivalent ion such as calcium results in instantaneous gelation (22). This gelation process can be explained through the egg-box model, where the carboxylic acid groups of two adjacent alginate molecules are bound by the multivalent ion (22,24). Pectin, a naturally occurring polysaccharide, mainly consists of α-(1,4)-galacturonic acid.…”

Section: Introductionmentioning

confidence: 99%

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Optimization of a Dual Mechanism Gastrofloatable and Gastroadhesive Delivery System for Narrow Absorption Window Drugs

et al. 2011

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Abstract. In order to overcome poor bioavailability of narrow absorption window drugs, a gastrosphere system comprising two mechanisms of gastric retention, namely buoyancy and gastroadhesion, has been investigated in this study employing poly(lactic-co-glycolic acid) (PLGA), polyacrylic acid (PAA), alginate, pectin, and a model drug metformin hydrochloride. Fifteen formulations were obtained using a Box-Behnken statistical design. The gastrosphere yield was above 80% in all cases; however, due to the high water solubility of metformin, drug entrapment efficacy was between 18% and 54%. Mean dissolution time and gastroadhesive strength were used as the formulation responses in order to optimize the formulation. Furthermore, the molecular mechanics force field simulations were performed to corroborate the experimental findings. Drug release profiles revealed three different release kinetics, namely, burst, first-order and zero-order release. Varying gastroadhesive results were obtained, and were highly sensitive to changes in polymer concentrations. FTIR revealed that strong bonds of PAA and PLGA were retained within the gastrosphere. Surface area and porosity analysis provided supporting evidence that the lyophilization process resulted in a significant increase in the porosity. Analysis of the surface morphology by SEM revealed that air pockets were spread over the entire surface of the gastrosphere, providing a visual proof of the high porosity and hence low density of the gastrosphere. The spatial disposition and energetic profile of the sterically constrained and geometrically optimized multi-polymeric complex of alginate, pectin, PAA, and PLGA corroborated the experimental results in terms of in vitro drug release and gastroadhesive strength of the fabricated gastrospheres.

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“…The alginic acid was known to form hydrated insoluble gels and promoted drug release to a larger extent than crosslinked alginate [20,21]. The observation of higher drug dissolution profile of alginate beads in microwave-treated water than untreated water denoted that the influence of water molecule mobility outweighed the effect of alginic acid on drug release from beads.…”

Section: Bead Swelling Erosion and Water Uptakementioning

confidence: 99%

Effects of Microwave on Water and Its Influence on Drug Dissolution

Wong¹,

Iskhandar²,

Kamal³

et al. 2009

PIER C

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Abstract-Use of water with different molecular mobilities could affect drug dissolution of a dosage form and such profile of water might be modifiable using microwave. This study investigated the effects of microwave on water and its influences on dissolution of free drugs and drugs in calcium-crosslinked alginate beads using sulphanilamide and sulphamerazine as hydrophilic and hydrophobic model drugs respectively. The water was treated by microwave at 300 W or without pre-treatment. The drug dissolution, pH and molecule mobility profiles of untreated and microwave-treated water were examined. Microwave-treated water had higher pH and water molecule mobility. The latter was characterized by higher conductivity, lower molecular interaction and crystallinity profiles. The dissolution of hydrophilic and hydrophobic free or encapsulated drugs was enhanced using microwave-treated water due to its higher molecular mobility. The untreated water of the same pH as microwave-treated water did not enhance drug dissolution. The drug dissolution from beads was increased by higher water uptake leading to matrix erosion and pore formation using microwave-treated water and was not promoted by the formation of non-crosslinked hydrated alginic acid matrix in untreated water of lower pH. Microwave treatment of water increased water molecule mobility and can promote drug dissolution.

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Alginate microparticles prepared by spray–coagulation method: Preparation, drug loading and release characterization

Cited by 66 publications

References 15 publications

Production and characterization of alginate-starch-chitosan microparticles containing stigmasterol through the external ionic gelation technique

Production and characterization of alginate-starch-chitosan microparticles containing stigmasterol through the external ionic gelation technique

Optimization of a Dual Mechanism Gastrofloatable and Gastroadhesive Delivery System for Narrow Absorption Window Drugs

Effects of Microwave on Water and Its Influence on Drug Dissolution

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