Predictive modeling of insulin release profile from cross-linked chitosan microspheres

Jose, Sajan; Fangueiro, Joana F.; Smitha, J.; Cinu, T.A.; Chacko, A.J.; Premaletha, K.; Souto, Eliana B.

doi:10.1016/j.ejmech.2012.12.011

Cited by 88 publications

(52 citation statements)

References 24 publications

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“…Specifically, insulin-loaded L/C NPs could be obtained without the use of cross-linking agents such as tripolyphosphate 29 or glutaraldehyde 26 through a simpler preparation procedure, which did not require homogenization or repeated washing and precipitation as done in previous studies. 30,27 Furthermore, the EE of self-assembled insulinloaded L/C NPs was much higher than that of other delivery systems.…”

Section: Discussionmentioning

confidence: 99%

Self-assembled lecithin/chitosan nanoparticles for oral insulin delivery: preparation and functional evaluation

Liu¹,

Zhou²,

Xia³

et al. 2016

IJN

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Purpose Here, we investigated the formation and functional properties of self-assembled lecithin/chitosan nanoparticles (L/C NPs) loaded with insulin following insulin–phospholipid complex preparation, with the aim of developing a method for oral insulin delivery. Methods Using a modified solvent-injection method, insulin-loaded L/C NPs were obtained by combining insulin–phospholipid complexes with L/C NPs. The nanoparticle size distribution was determined by dynamic light scattering, and morphologies were analyzed by cryogenic transmission electron microscopy. Fourier transform infrared spectroscopy analysis was used to disclose the molecular mechanism of prepared insulin-loaded L/C NPs. Fast ultrafiltration and a reversed-phase high-performance liquid chromatography assay were used to separate free insulin from insulin entrapped in the L/C NPs, as well as to measure the insulin-entrapment and drug-loading efficiencies. The in vitro release profile was obtained, and in vivo hypoglycemic effects were evaluated in streptozotocin-induced diabetic rats. Results Our results indicated that insulin-containing L/C NPs had a mean size of 180 nm, an insulin-entrapment efficiency of 94%, and an insulin-loading efficiency of 4.5%. Cryogenic transmission electron microscopy observations of insulin-loaded L/C NPs revealed multilamellar structures with a hollow core, encircled by several bilayers. In vitro analysis revealed that insulin release from L/C NPs depended on the L/C ratio. Insulin-loaded L/C NPs orally administered to streptozotocin-induced diabetic rats exerted a significant hypoglycemic effect. The relative pharmacological bioavailability following oral administration of L/C NPs was 6.01%. Conclusion With the aid of phospholipid-complexation techniques, some hydrophilic peptides, such as insulin, can be successfully entrapped into L/C NPs, which could improve oral bioavailability, time-dependent release, and therapeutic activity.

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Section: Discussionmentioning

confidence: 99%

Self-assembled lecithin/chitosan nanoparticles for oral insulin delivery: preparation and functional evaluation

Liu¹,

Zhou²,

Xia³

et al. 2016

IJN

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“…The CSN were prepared using an emulsion crosslinking method [24][25][26][27]. A stock solution of 2% (v/v) glutaraldehyde was prepared by dissolving 4.0 mL of glutaraldehyde in 46 mL of 1,4-dioxane.…”

Section: Preparation Of Csn Using An Emulsion Crosslinking Methodsmentioning

confidence: 99%

Sensitive detection of Au(III) using regenerative rhodamine B–functionalized chitosan nanoparticles

Liu

et al. 2016

Sensors and Actuators B: Chemical

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“…ACCEPTED MANUSCRIPT 21 In addition to thermal stress [59], proteins are prone to denaturation and aggregation by various factors in processes like the solvent evaporation/extraction methods described above, including exposure to high shear forces during processing (particularly emulsification), exposure to the large interfacial area between the emulsified oil and aqueous phases or at the air-water interface of small droplets, as well as interaction with an encapsulating polymer or organic solvent. The loss of protein activity by denaturation/aggregation can be minimized by using a number of stabilizers such as polyols, albumins and other proteins, surfactants, poloxamers, cyclodextrins, etc, depending on the stresses involved in the manufacturing processes for various oral drug delivery systems, which are further highlighted below.…”

Section: Accepted Manuscriptmentioning

confidence: 99%

Stabilization Challenges and Formulation Strategies Associated with Oral Biologic Drug Delivery Systems

Truong‐Le¹,

Lovalenti²,

Abdul‐Fattah³

2015

Advanced Drug Delivery Reviews

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Predictive modeling of insulin release profile from cross-linked chitosan microspheres

Cited by 88 publications

References 24 publications

Self-assembled lecithin/chitosan nanoparticles for oral insulin delivery: preparation and functional evaluation

Self-assembled lecithin/chitosan nanoparticles for oral insulin delivery: preparation and functional evaluation

Sensitive detection of Au(III) using regenerative rhodamine B–functionalized chitosan nanoparticles

Stabilization Challenges and Formulation Strategies Associated with Oral Biologic Drug Delivery Systems

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