Microencapsulation of self-microemulsifying system: Improving solubility and permeability of furosemide

Zvonar, Alenka; Berginc, Katja; Kristl, Albin; Gašperlin, Mirjana

doi:10.1016/j.ijpharm.2009.12.055

Cited by 72 publications

(40 citation statements)

References 28 publications

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“…6 A further report by Zvonar et al described use of a self-microemulsifying system to fabricate Ca-pectinate microcapsules to improve the release and permeability of furosemide. 7 Drug-loaded polymer microspheres have been variously prepared by phase separation, 8 interfacial polymerization, 9 spray-drying, 10 freeze-drying, 11 and emulsion evaporation. 12 However, these conventional strategies always either involve an intense operating process or preparation of particles with a wide particle size distribution and a relatively large amount of organic solvent residue.…”

Section: Introductionmentioning

confidence: 99%

Formation of methotrexate-PLLA-PEG-PLLA composite microspheres by microencapsulation through a process of suspension-enhanced dispersion by supercritical CO2

Chen¹,

Wang²,

Wang³

et al. 2012

IJN

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Background:The aim of this study was to improve the drug loading, encapsulation efficiency, and sustained-release properties of supercritical CO 2 -based drug-loaded polymer carriers via a process of suspension-enhanced dispersion by supercritical CO 2 (SpEDS), which is an advanced version of solution-enhanced dispersion by supercritical CO 2 (SEDS). Methods: Methotrexate nanoparticles were successfully microencapsulated into poly (L-lactide)-poly(ethylene glycol)-poly(L-lactide) (PLLA-PEG-PLLA) by SpEDS. Methotrexate nanoparticles were first prepared by SEDS, then suspended in PLLA-PEG-PLLA solution, and finally microencapsulated into PLLA-PEG-PLLA via SpEDS, where an "injector" was utilized in the suspension delivery system. Results: After microencapsulation, the composite methotrexate (MTX)-PLLA-PEG-PLLA microspheres obtained had a mean particle size of 545 nm, drug loading of 13.7%, and an encapsulation efficiency of 39.2%. After an initial burst release, with around 65% of the total methotrexate being released in the first 3 hours, the MTX-PLLA-PEG-PLLA microspheres released methotrexate in a sustained manner, with 85% of the total methotrexate dose released within 23 hours and nearly 100% within 144 hours. Conclusion: Compared with a parallel study of the coprecipitation process, microencapsulation using SpEDS offered greater potential to manufacture drug-loaded polymer microspheres for a drug delivery system.

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Section: Introductionmentioning

confidence: 99%

Formation of methotrexate-PLLA-PEG-PLLA composite microspheres by microencapsulation through a process of suspension-enhanced dispersion by supercritical CO2

Chen¹,

Wang²,

Wang³

et al. 2012

IJN

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“…The dissolution profile obtained from the tablets showed improved profile when compared to Glyburide alone. Zvonar et al (2010) suggested that, SMEFs possessing a composition similar to microcapsules with Ca-pectinate shell and a drug loaded SMEFs as the core phase, would be a potential approach for enhancing low permeability and solubility of BCS class II drugs.…”

Section: Self-microemulsifying Formulationsmentioning

confidence: 99%

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

Wadhwa¹,

Nair²,

Kumria³

2011

Braz. J. Pharm. Sci.

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Self-emulsifying therapeutic system (SETs) provide an effective and intelligent solution to the various issues related to the formulation of hydrophobic drugs with limited solubility in gastrointestinal fluid. Although the potential utility of SETs is well known, only in recent years has a mechanistic understanding of the impact of these systems on drug disposition emerged. These in situ emulsion-forming systems have a high stability when incorporated in various dosage forms. SETs are being looked upon as systems which can overcome the problems associated with delivery of poorly water soluble drugs. An in-depth knowledge about lipids and surfactants that can contribute to these systems, criterion for their selection and the proportion in which they can be used, represent some crucial factors determining the in vivo performance of these systems. This article presents a comprehensive account of various types of self-emulsifying formulations with emphasis on their composition and examples of currently marketed preparations.Uniterms: Lipid based formulations. Self-emulsifying therapeutic system. Self-emulsification.O sistema terapêutico auto-emulsionante (SETs) fornece solução eficaz e inteligente para os vários problemas relativos à formulação de fármacos hidrofóbicos com solubilidade limitada no fluido gastrintestinal. Embora a utilidade potencial dos SETs seja bem conhecida, só recentemente se compreendeu, mecanisticamente,o impacto desses sistemas na disposição de fármacos. Estes sistemas de formação de emulsão in situ têm alta estabilidade, quando incorporados em várias formas de dosagem. Os SETs têm sido considerados como sistemas que podem resolver problemas associados à liberação de fármacos pouco solúveis em água. O conhecimento profundo dos lipídios e tensoativos que podem ser utilizados para estes sistemas e o critério para a sua seleção e proporção na qual eles são utilizados são alguns dos fatores cruciais que determinam o desempenho do sistema in vivo. Este artigo apresenta o relato abrangente de vários tipos de formulações auto-emulsificantes, com ênfase em sua composição e exemplos das preparações que são correntemente comercializadas.Unitermos: Formulações baseadas em lipídio. Sistema terapêutico auto-emulsificante. Autoemulsificação.

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“…3 In general, SNEDDS is an isotropic mixture of drug, oil, surfactants, and cosurfactants, which forms an oil-in-water nanoemulsion upon contact with aqueous medium under gentle agitation. [4][5][6] SNEDDSs are commonly formulated in a liquid state and further encapsulated into soft gelatin capsules before use. However, the soft capsule formulations have some disadvantages, including low drug compatibility, poor stability, drug leakage and precipitation, capsule aging, and high production costs.…”

Section: Introductionmentioning

confidence: 99%

“…[11][12][13][14][15] Spray-drying has also been employed to formulate liquid SNEDDSs into free-flowing powders, using adsorbents such as Aerosil 200 16 and dextran. 17 Homar et al 18 and Zvonar et al 6 reported microencapsulation of liquid SNEDDSs to obtain solid powders of microcapsules. The powders containing liquid SNEDDS can be further formulated into solid dosage forms, such as tablets, capsules, and granules.…”

Section: Introductionmentioning

confidence: 99%

Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility

Yang¹,

Lü²,

Qi³

et al. 2011

IJN

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Background: The objective of this study was to evaluate fluid-bed coating as a new technique to prepare a pellet-based solid self-nanoemulsifying drug delivery system (SNEDDS) using cyclosporin A as a model of a poorly water-soluble drug. Methods: The rationale of this technique was to entrap a Liquid SNEDDS in the matrix of the coating material, polyvinylpyrrolidone K30, by fluid-bed coating. Pseudoternary phase diagrams were used to screen the liquid SNEDDS formulations. The optimal formulation was composed of Labrafil M ® 1944 CS, Transcutol P ® , and Cremophor ® EL in a ratio of 9:14:7. To prepare solid SNEDDS pellets, liquid SNEDDS was first dispersed in an aqueous solution of polyvinylpyrrolidone and then sprayed onto the surface of non-pareil pellets. Upon evaporation of water, polyvinylpyrrolidone precipitated and formed tight films to entrap the liquid SNEDDS. Visual observation and scanning electron microscopic analysis confirmed good appearance of the solid SNEDDS pellets. Results: Our results indicated that up to 40% of the liquid SNEDDS could be entrapped in the coating layer. Powder x-ray diffraction analysis confirmed nonexistence of crystalline cyclosporin A in the formulation. Solid SNEDDS pellets showed a slower redispersion rate than the liquid SNEDDS. An increase in the total liquid SNEDDS loading led to faster redispersion, whereas increased coating weight (up to 400%) significantly decreased the redispersion rate. Both cyclosporin A loading and protective coating with 5% polyvinylpyrrolidone K30 did not significantly affect the redispersion rate. Conclusion: It is concluded that fluid-bed coating is a new technique with considerable potential for preparation of pellet-based solid SNEDDS formulations.

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Microencapsulation of self-microemulsifying system: Improving solubility and permeability of furosemide

Cited by 72 publications

References 28 publications

Formation of methotrexate-PLLA-PEG-PLLA composite microspheres by microencapsulation through a process of suspension-enhanced dispersion by supercritical CO2

Formation of methotrexate-PLLA-PEG-PLLA composite microspheres by microencapsulation through a process of suspension-enhanced dispersion by supercritical CO2

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

Solid self-nanoemulsifying cyclosporin A pellets prepared by fluid-bed coating: preparation, characterization and in vitro redispersibility

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