Multiple Emulsions for the Delivery of Proteins

Shively, Merrick L.

doi:10.1007/0-306-46803-4_7

Cited by 10 publications

(3 citation statements)

References 30 publications

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“…Water-in-oil-in-water (w/o/w) emulsions are thermodynamically unstable multiple emulsions that are difficult to stabilise, which is a factor that restricts their application in delivery of proteins (reviewed in [307]). Intestinal delivery of peptides in w/o/w emulsions was first tested over 45 years ago [308] and several prototypes have been shown to improve peptide permeability in animal models, including insulin [309] and sCT [310].…”

Section: Permeation Enhancement From Multiple Emulsionsmentioning

confidence: 99%

Intestinal permeation enhancers for oral peptide delivery

Maher

Mrsny

Brayden

2016

Advanced Drug Delivery Reviews

282

201

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Publication informationAdvanced Drug Delivery Reviews, (Part B): 277-319 Publisher ElsevierItem record/more information http://hdl.handle.net/10197/7800Publisher's statement þÿ T h i s i s t h e a u t h o r s v e r s i o n o f a w o r k t h a t w a s a c c e p t e d f o r p u b l i c a t i o n i n A d v a n c e d D r u g Delivery Reviews. Changes resulting from the publishing process, such as peer review,

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Section: Permeation Enhancement From Multiple Emulsionsmentioning

confidence: 99%

Intestinal permeation enhancers for oral peptide delivery

Maher

Mrsny

Brayden

2016

Advanced Drug Delivery Reviews

282

201

View full text Add to dashboard Cite

show abstract

“…Thus, an impeller rotational speed of 400 rpm was chosen to allow the achievement of small microspheres with a narrow size distribution. Moreover, protein drugs are susceptible to denaturation when they are submitted to high shear forces (Shively, 1997).…”

Section: Formulation Optimizationmentioning

confidence: 99%

Alginate microspheres prepared by internal gelation: Development and effect on insulin stability

Silva

Ribeiro

Figueiredo

et al. 2006

International Journal of Pharmaceutics

184

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Recombinant human insulin was encapsulated within alginate microspheres by the emulsification/internal gelation technique with the objective of preserving protein stability during encapsulation procedure. The influence of process and formulation parameters was evaluated on the morphology and encapsulation efficiency of insulin. The in vitro release of insulin from microspheres was studied under simulated gastrointestinal conditions and the in vivo activity of protein after processing was assessed by subcutaneous administration of extracted insulin from microspheres to streptozotocin-induced diabetic rats. Microspheres mean diameter, ranging from 21 to 287 m, decreased with the internal phase ratio, emulsifier concentration, mixer rotational speed and increased with alginate concentration. Insulin encapsulation efficiency, near 75%, was not affected by emulsifier concentration, mixer rotational speed and zinc/insulin hexamer molar ratio but decreased either by increasing internal phase ratio and calcium/alginate mass ratio or by decreasing acid/calcium molar ratio and alginate concentration. A high insulin release, above 75%, was obtained at pH 1.2 and under simulated intestinal pH a complete dissolution of microspheres occurred. Extracted insulin from microspheres decreased hyperglycemia of diabetic rats proving to be bioactive and showing that encapsulation in alginate microspheres using the emulsification/internal gelation is an appropriate method for protein encapsulation.

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“…Although peptides and proteins are more important for drug substance, most peptides and proteins are not stable and, therefore, not effective by oral given (Hilderbrand and Tack, 2000). To avoid destruction of peptide and protein by intestinal proteases, emulsification and microencapsulation techniques have been frequently used (Shively, 1997). Figure 2 showed an antihypertensive effect of oral administration of emulsified egg albumen hydrolysate.…”

Section: Resultsmentioning

confidence: 99%

Production of Angiotensin-I Converting Enzyme Inhibitory Hydrolysates from Egg Albumen

Kim¹,

Ham²,

Jeong³

et al. 2003

Asian Australas. J. Anim. Sci

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ACE (Angiotensin-I converting enzyme) inhibitory peptides derived from foods are thought to suppress high blood pressure by inhibiting ACE. We tried to make efficient production of the ACE inhibitory hydrolysate from egg albumen. A hydrolysate digested by neutrase presented the highest ACE inhibitory activity (IC 50 value=256.35 µg/ml) and the proper proteolysis was occurred by 1.0% enzyme addition and 4 h incubation at 47°C. Antihypertensive effect of neutrase hydrolysate was investigated in spontaneously hypertensive rats (SHR, n=5). Systolic blood pressure (SBP) was decrease by 6.88% (-14.14 mmHg, p<0.05) at 3 h after oral administration of 300 mg/kg body weight, and by 13.33% (-27.72 mmHg, p<0.05) by emulsified hydrolysate. These results showed that it is very effective to utilize egg albumen as a protein source for the production of ACE inhibitory peptides. However, further studies are required to investigate the methods to increase recovery yield and the isolation of active peptide is necessary for determining its sequence responsible for ACE inhibitory activity.

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Multiple Emulsions for the Delivery of Proteins

Cited by 10 publications

References 30 publications

Intestinal permeation enhancers for oral peptide delivery

Intestinal permeation enhancers for oral peptide delivery

Alginate microspheres prepared by internal gelation: Development and effect on insulin stability

Production of Angiotensin-I Converting Enzyme Inhibitory Hydrolysates from Egg Albumen

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