Preparation and evaluation of alginate–chitosan microspheres for oral delivery of insulin

Zhang, Yueling; Wei, Wei; Lv, Piping; Wang, Lianyan; Ma, Guanghui

doi:10.1016/j.ejpb.2010.09.016

Cited by 280 publications

(156 citation statements)

References 33 publications

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“…This REFD approach to prepare insulin-loaded nanoparticles had the outstanding advantages that the drug entrapment efficiency (∼95%) and drug loading content were much higher as compared to the most widely investigated approaches such as ionic gelation method to prepare insulinloaded chitosan-alginate nanoparticles and W/O/W emulsion method to prepare insulin-loaded PLGA nanoparticles (19). Insulin is a hydrophilic peptide hormone, while conventional preparation techniques for insulin nanoparticle formulations commonly used water as external phase and insulin tended to diffuse to the external phase, resulting in relatively low drug entrapment efficiency and drug loading content (20,21). Low drug entrapment efficiency is thought as one of the limitations for large-scale production.…”

Section: Scheme 1 Preparation Of Insulin-loaded Ha Nanoparticles By mentioning

confidence: 99%

Insulin-Loaded pH-Sensitive Hyaluronic Acid Nanoparticles Enhance Transcellular Delivery

et al. 2012

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Abstract. In the present study, we developed novel insulin-loaded hyaluronic acid (HA) nanoparticles for insulin delivery. The insulin-loaded HA nanoparticles were prepared by reverse-emulsion-freeze-drying method. This method led to a homogenous population of small HA nanoparticles with average size of 182.2 nm and achieved high insulin entrapment efficiencies (approximately 95%). The pH-sensitive HA nanoparticles as an oral delivery carrier showed advantages in protecting insulin against the strongly acidic environment of the stomach, and not destroying the junction integrity of epithelial cells which promise long-term safety for chronic insulin treatment. The results of transport experiments suggested that insulinloaded HA nanoparticles were transported across Caco-2 cell monolayers mainly via transcellular pathway and their apparent permeability coefficient from apical to basolateral had more than twofold increase compared with insulin solution. The efflux ratio of P app (B to A) to P app (A to B) less than 1 demonstrated that HA nanoparticle-mediated transport of insulin across Caco-2 cell monolayers underwent active transport. The results of permeability through the rat small intestine confirmed that HA nanoparticles significantly enhanced insulin transport through the duodenum and ileum. Diabetic rats treated with oral insulin-loaded HA nanoparticles also showed stronger hypoglycemic effects than insulin solution. Therefore, these HA nanoparticles could be a promising candidate for oral insulin delivery.

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Section: Scheme 1 Preparation Of Insulin-loaded Ha Nanoparticles By mentioning

confidence: 99%

Insulin-Loaded pH-Sensitive Hyaluronic Acid Nanoparticles Enhance Transcellular Delivery

et al. 2012

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“…Further advantages of microspheres include effective protection of encapsulated drugs against degradation, increased drug solubility, reduced adverse or toxic effects, site-specific drug delivery and controlled drug release (Singh et al, 2010). Microspheres based on Eudragits Õ have been explored for various drug delivery applications (Agyilirah & Banker, 2000;Haznedar & Dortunc, 2004;Sahoo et al, 2009;Apurba et al, 2009;Kishori et al, 2013), including insulin delivery (Kinesh et al, 2010;Singh et al, 2010b;Zhang et al, 2011;Cárdenas-Bailón et al, 2013). Eudragit Õ polymers are more favored in the formulation of pH-sensitive drug molecules.…”

Section: Introductionmentioning

confidence: 99%

Influence of magnesium stearate on the physicochemical and pharmacodynamic characteristics of insulin-loaded Eudragit entrapped mucoadhesive microspheres

et al. 2014

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Effective oral insulin delivery has remained a challenge to the pharmaceutical industry. This study was designed to evaluate the effect of magnesium stearate on the properties of insulin-loaded Eudragit Õ RL 100 entrapped mucoadhesive microspheres. Microspheres containing Eudragit Õ RL 100, insulin, and varying concentrations of magnesium stearate (agglomeration-preventing agent) were prepared by emulsification-coacervation method and characterized with respect to differential scanning calorimetry (DSC), morphology, particle size, loading efficiency, mucoadhesive and micromeritics properties. The in vitro release of insulin from the microspheres was performed in simulated intestinal fluid (SIF, pH 7.2) while the in vivo hypoglycemic effect was investigated by monitoring the plasma glucose level of the alloxaninduced diabetic rats after oral administration. Stable, spherical, brownish, mucoadhesive, discrete and free flowing insulin-loaded microspheres were formed. While the average particle size and mucoadhesiveness of the microspheres increased with an increase in the proportion of magnesium stearate, loading efficiency generally decreased. After 12 h, microspheres prepared with Eudragit Õ RL 100: magnesium stearate ratios of 15:1, 15:2, 15:3 and 15:4 released 68.20 ± 1.57, 79.40 ± 1.52, 76.60 ± 1.93 and 70.00 ± 1.00 (%) of insulin, respectively. Reduction in the blood glucose level for the subcutaneously (sc) administered insulin was significantly (p 0.05) higher than for most of the formulations. However, the blood glucose reduction effect produced by the orally administered insulin-loaded microspheres prepared with four parts of magnesium stearate and fifteen parts of Eudragit Õ RL 100 after 12 h was equal to that produced by subcutaneously administered insulin solution. The results of this study can suggest that this carrier system could be an alternative for the delivery of insulin.

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“…[7][8][9][10] Membrane emulsification is another popular method to form spherical morphology. 11,12 The membrane shapes the solution into uniform drops and the oil phase keeps the drops in the same morphology. We and others have utilized atomization equipped with air-flow or an external electric field to make alginate microspheres.…”

Section: Introductionmentioning

confidence: 99%

Fabrication of inorganic hydroxyapatite nanoparticles and organic biomolecules-dual encapsulated alginate microspheres

Wang¹,

Liao²,

Liu³

et al. 2015

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Preparation and evaluation of alginate–chitosan microspheres for oral delivery of insulin

Cited by 280 publications

References 33 publications

Insulin-Loaded pH-Sensitive Hyaluronic Acid Nanoparticles Enhance Transcellular Delivery

Insulin-Loaded pH-Sensitive Hyaluronic Acid Nanoparticles Enhance Transcellular Delivery

Influence of magnesium stearate on the physicochemical and pharmacodynamic characteristics of insulin-loaded Eudragit entrapped mucoadhesive microspheres

Fabrication of inorganic hydroxyapatite nanoparticles and organic biomolecules-dual encapsulated alginate microspheres

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