Insulin Loaded PLGA Microspheres: Effect of Zinc Salts on Encapsulation, Release, and Stability

Manoharan, Chandrasekar; Singh, Jagdish

doi:10.1002/jps.21445

Cited by 51 publications

(44 citation statements)

References 37 publications

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“…Its surface activity leads to adsorption at interfaces, resulting in instability caused by unfolding, inactivation or irreversible aggregation. Furthermore, high rates of shear, often associated with emulsification based techniques, affect the threedimensional structure of insulin, maintenance of which is essential for therapeutic activity (Manoharan and Singh, 2009;Perez et al, 2002). Formation of insulin loaded NP by a double emulsion technique uses either sonication or homogenisation as a source of high shear agitation (Blum and Saltzman, 2008).…”

Section: Effect Of Internal Aqueous Phase Volumementioning

confidence: 99%

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

Haggag

Abdel-Wahab

Ojo

et al. 2016

International Journal of Pharmaceutics

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A B S T R A C TThe aim of this study was to design a controlled release vehicle for insulin to preserve its stability and biological activity during fabrication and release. A modified, double emulsion, solvent evaporation, technique using homogenisation force optimised entrapment efficiency of insulin into biodegradable nanoparticles (NP) prepared from poly (DL-lactic-co-glycolic acid) (PLGA) and its PEGylated diblock copolymers. Formulation parameters (type of polymer and its concentration, stabiliser concentration and volume of internal aqueous phase) and physicochemical characteristics (size, zeta potential, encapsulation efficiency, in vitro release profiles and in vitro stability) were investigated. In vivo insulin sensitivity was tested by diet-induced type II diabetic mice. Bioactivity of insulin was studied using Swiss TO mice with streptozotocin-induced type I diabetic profile. Insulin-loaded NP were spherical and negatively charged with an average diameter of 200-400 nm. Insulin encapsulation efficiency increased significantly with increasing ratio of co-polymeric PEG. The internal aqueous phase volume had a significant impact on encapsulation efficiency, initial burst release and NP size. Optimised insulin NP formulated from 10% PEG-PLGA retained insulin integrity in vitro, insulin sensitivity in vivo and induced a sustained hypoglycaemic effect from 3 h to 6 days in type I diabetic mice..

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Section: Effect Of Internal Aqueous Phase Volumementioning

confidence: 99%

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

Haggag

Abdel-Wahab

Ojo

et al. 2016

International Journal of Pharmaceutics

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“…BSA has high water solubility (aqueous solubility: "40 mg/mL) [22], while risperidone is a small hydrophobic molecule (molecular formula: C 23 H 27 FN 4 O 2 ) with very low water solubility about 2.8 µg/mL [23]. Insulin also has limited solubility at neutral pH ("0.1 mg/mL) [2]. Our studies indicated that BSA showed highest initial burst release and released over shorter duration, followed by insulin and risperidone.…”

Section: In Vitro Releasementioning

confidence: 99%

“…The biologically derived molecules usually have a short half-life and are prone to physical and chemical instabilities [2][3][4][5][6]. Due to short biological half-life, these molecules are delivered by frequent injections.…”

Section: Introductionmentioning

confidence: 99%

Effect of Molar Mass and Water Solubility of Incorporated Molecules on the Degradation Profile of the Triblock Copolymer Delivery System

et al. 2015

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The purpose of this study was to investigate the effects of size and type of incorporated model molecules on the polymer degradation and release profile from thermosensitive triblock copolymer based controlled delivery systems. In vitro release of the incorporated molecules demonstrated slow release for risperidone (molecular weight (M w ) = 410.48 Da; partition coefficient (K o/w ) = 3.49), while bovine serum albumin (BSA) (M w = "66,400 Da; K o/w = 0.007) and insulin (M w = 5808 Da; K o/w = 0.02) showed initial burst release followed by controlled release. The proton NMR, Gel Permeation Chromatography, and Cryo-SEM studies suggest that the size and partition coefficient of incorporated molecules influence the pore size, polymer degradation, and their release. In spite of using a similar polymer delivery system the polymer degradation rate and drug release notably differ for these model molecules. Therefore, size and oil-water partition coefficient are important factors for designing the controlled release formulation of therapeutics from triblock copolymer based delivery systems.Polymers 2015, 7 1511

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“…Initial burst release and release kinetics were markedly changed with the addition of zinc salts. More than 87% of the encapsulated insulin was released over a 2-week period with the addition of a zinc salt (Manoharan et al, 2009). Collagen is a natural protein found in skin, bones and tendons.…”

Section: Introductionmentioning

confidence: 99%

Advanced Collagen-Insulin Systems for Diabetics

Manolache¹,

Kaya²,

Stancu³

et al. 2016

The International Conference on Advanced Materials and Systems

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Diabetes is the most common disease in our world. In our country over 50.000 of people are diagnosed with diabetes every year. Diabetes is a metabolic disorder generated by the pancreas inability to produce insulin in order to complete glucose metabolic process. Therefore, the life of the patients is sustained by the insulin administration. Existing methods on the market for insulin administration are not too various and there are a lots of disadvantages. Insulin glargine is a longaction, man-made version of human insulin. It replaces the insulin that is not produced by the body and helps the metabolic process of glucose. To increase insulin stability and releasing time, zinc oxide (ZnO) can be used for insulin encapsulation. Collagen is a natural protein that can be used as a support for controlled releases system because of its high biocompatibility. The aim of this study was to develop and characterize a controlled released subdermal support, for diabetics patients, made of a composite material based on collagen, zinc oxide and insulin. Obtained matrices were characterized by FT-IR spectroscopy, optical and scanning electronic microscopy, water up-take, degradation in collagenase solution. The results showed that the combination between collagen, ZnO and insulin could be suitable active supports for subdermal support with controlled delivery of insulin for diabetics.

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Insulin Loaded PLGA Microspheres: Effect of Zinc Salts on Encapsulation, Release, and Stability

Cited by 51 publications

References 37 publications

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

Effect of Molar Mass and Water Solubility of Incorporated Molecules on the Degradation Profile of the Triblock Copolymer Delivery System

Advanced Collagen-Insulin Systems for Diabetics

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