Cyclodextrin complexed insulin encapsulated hydrogel microparticles: An oral delivery system for insulin

Sajeesh, S.; Bouchemal, Kawthar; Marsaud, Véronique; Vauthier, Christine; Sharma, Chandra P.

doi:10.1016/j.jconrel.2010.08.007

Cited by 120 publications

(52 citation statements)

References 37 publications

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“…Experiments were performed in triplicate. ) dissolved in citrate buffer (pH 4.5) (20). After 3 days of injection, rats were considered to be diabetic when the glycaemia was above 250 mg dL -1 .…”

Section: Protein Release Studiesmentioning

confidence: 99%

Biomimetic insulin-imprinted polymer nanoparticles as a potential oral drug delivery system

2017

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In this study, we investigate molecularly imprinted polymers (MIPs), which form a three-dimensional image of the region at and around the active binding sites of pharmaceutically active insulin or are analogous to b cells bound to insulin. This approach was employed to create a welldefined structure within the nanospace cavities that make up functional monomers by cross-linking. The obtained MIPs exhibited a high adsorption capacity for the target insulin, which showed a significantly higher release of insulin in solution at pH 7.4 than at pH 1.2. In vivo studies on diabetic Wistar rats showed that the fast onset within 2 h is similar to subcutaneous injection with a maximum at 4 h, giving an engaged function responsible for the duration of glucose reduction for up to 24 h. These MIPs, prepared as nanosized material, may open a new horizon for oral insulin delivery.

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Section: Protein Release Studiesmentioning

confidence: 99%

Biomimetic insulin-imprinted polymer nanoparticles as a potential oral drug delivery system

2017

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“…[37] Miscellaneous Several other novel systems are developed for oral insulin delivery such as layered double hydroxides, [38,39] carbon nanospheres, [40,41] and cyclodextrin complexed insulin. [42,43] …”

Section: Microspheresmentioning

confidence: 99%

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2017

AJP

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Diabetes is a disorder related to the deficiency in the secretion or action of insulin -a peptide hormone synthesized by the β cells of islets of pancreas. Insulin is given by the subcutaneous (SC) route. Patient non-compliance is frequent with the SC route. To remove the hurdle related to oral insulin delivery various efforts have been made. Thus, oral insulin is a dream of patients. Nanotechnology is an emerging era of science which provides an innovative means to detect, diagnose and to treat a disorder. Nanocarriers have been garnering more attention recently because of their size in nano range and greater surface area. These characteristics improve their absorption in contrast to bigger carriers. This article gives an insight into different novel approaches to get better oral insulin delivery. These novel formulations improve bioavailability; absorption problems associated with insulin and give protection from enzymatic degradation. More research has been done on nanoparticles (NPs) as a carrier to deliver insulin orally. At present, researchers from both industries as well as academics are working on oral insulin. With this struggle, the dream of researcher to deliver insulin orally will turn out to be a reality in the future.

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“…where F is the fasting blood glucose level, Pt is the blood glucose level at time (t) post-administration (Rekha & Sharma, 2009;Sonaje et al, 2009;Sajeesh et al, 2010;Makhlof et al, 2011). For determination of oral BA of INS plus surfactin, 24 diabetic mice were randomly divided into two groups for 12 mice per group and fasted as described above.…”

Section: Determination Of Hypoglycemic Effects Of Oral Ins Plus Surfamentioning

confidence: 99%

A natural lipopeptide of surfactin for oral delivery of insulin

et al. 2016

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Surfactin, a natural lipopeptide produced by Bacillus, is gaining attention for potentially biomedical and pharmaceutical applications. Here, surfactin was assayed for oral delivery of insulin (INS) by its ability to bind to and promote protein to penetrate through the cell membrane. Analysis by sodium dodecyl sulfate-polyacrylamide gel electrophoresis, surfactin was found to form co-precipitates with INS to protect it from acidic and enzymatic attack in the gastrointestinal tract. Further analysis by non-reductive electrophoresis showed surfactin could bind to INS forming heteropolymers. Analysis with circular dichroism, we found this binding significantly influenced the INS structure with decreased rigid a-helix and b-turn, but with increased flexible b-sheet and random coil. The change with more flexible structure was favorable for INS to penetrate through the cell membrane. Fluorescence spectra analysis also showed surfactin could lead Phe and Tyr in the inner of INS exposed outside, further promoting INS permeabilization by improving the hydrophobic-lipophilic interactions between INS and cell membrane. As a result, the effective permeability (Peff) of INS plus surfactin was 4.3 times of that of INS alone. In vivo assay showed oral INS with surfactin displayed excellent hypoglycemic effects with a relative bioavailability of 12.48% and 5.97% in diabetic mice and non-diabetic dogs, respectively. Summary, surfactin is potential for oral delivery of INS by its role as an effective protease inhibitor and permeability enhancer.

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Cyclodextrin complexed insulin encapsulated hydrogel microparticles: An oral delivery system for insulin

Cited by 120 publications

References 37 publications

Biomimetic insulin-imprinted polymer nanoparticles as a potential oral drug delivery system

Biomimetic insulin-imprinted polymer nanoparticles as a potential oral drug delivery system

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A natural lipopeptide of surfactin for oral delivery of insulin

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