Stability of insulin during the erosion of poly(lactic acid) and poly(lactic-co-glycolic acid) microspheres

Ibrahim, Mohamed A.; Ismail, Ahmed; Fetouh, Mohamed I.; Göpferich, Achim

doi:10.1016/j.jconrel.2005.02.025

Cited by 113 publications

(67 citation statements)

References 24 publications

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“…Although we optimized the formula of the BSA-PLGA microspheres prepared by conventional methods, the burst release of BSA at 0.5 h from PLGA microspheres still remained (≥ 30%) high. The high initial release of protein drug from PLGA microspheres is usually caused by the surface-adsorbed drug and the fast drug diffusion from interconnecting network of pores (Ibrahim et al, 2005). To modulate the initial release rate, a kind of composite microsphere was developed by modifying the conventional PLGA microspheres with alginate and chitosan.…”

Section: Discussionmentioning

confidence: 99%

A one-step modified method to reduce the burst initial release from PLGA microspheres

Zheng

Liang

2010

Drug Delivery

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Section: Discussionmentioning

confidence: 99%

A one-step modified method to reduce the burst initial release from PLGA microspheres

Zheng

Liang

2010

Drug Delivery

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“…Covalent aggregation via thiol-disulphide exchange-reaction due to acidification inside the microspheres was also demonstrated using an SDS-PAGE under reducing conditions Kim et al, 2004). Additionally, chemical degradation reactions such as acylation (Lucke et al, 2002) and deamidation (Ibrahim et al, 2005), not detected by the SDS-PAGE results, may happen during the incubation period and they should also be considered.…”

Section: Trends Toward a Sustained And Complete Releasementioning

confidence: 93%

How to achieve sustained and complete protein release from PLGA-based microparticles?

Giteau

Venier-Julienne

Aubert-Pouëssel

et al. 2008

International Journal of Pharmaceutics

234

184

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One of the most challenging tasks in the delivery of therapeutic proteins from PLGAbased microparticles is the sustained and complete release of the protein in its native form.The mechanisms responsible for incomplete protein release from these devices are numerous and complex; the beneficial effect of different formulations has often been evaluated in vitro.Strategies employed for overcoming protein destabilization during the release step are reviewed in this paper. Proteins have been protected in the deleterious environment by adding stabilizers to the formulation, or by modifying the protein or the polymer. Alternatively, some strategies have aimed at avoiding the formation of the destabilizing environment. As experimental conditions may influence the results from in vitro release studies, we initially report precautions to avoid adverse effects.

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“…Alternatively, the use of sonication as the source of agitation to form the two emulsion types preserves the physical and chemical stability of insulin during NP fabrication (Fonte et al, 2012;Sarmento et al, 2007;Sheshala et al, 2009). However, low encapsulation efficiency (Sarmento et al, 2007;Sheshala et al, 2009) and high initial burst effect (Fonte et al, 2012;Ibrahim et al, 2005) are observed.…”

Section: Introductionmentioning

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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Stability of insulin during the erosion of poly(lactic acid) and poly(lactic-co-glycolic acid) microspheres

Cited by 113 publications

References 24 publications

A one-step modified method to reduce the burst initial release from PLGA microspheres

A one-step modified method to reduce the burst initial release from PLGA microspheres

How to achieve sustained and complete protein release from PLGA-based microparticles?

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

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