Polymeric hydrogels for oral insulin delivery

Chaturvedi, Kiran; Ganguly, Kuntal; Nadagouda, Mallikarjuna N.; Aminabhavi, Tejraj M.

doi:10.1016/j.jconrel.2012.11.005

Cited by 218 publications

(154 citation statements)

References 100 publications

(111 reference statements)

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“…During crystallization process, short chain polymers organize themselves into highly ordered crystalline structures more readily than long chain polymers. Polymer morphology is also dependent on the size and shape of the substituent groups [33]. The diffractograms support the DSC findings and we may infer that the thiolated polymer is amorphous in nature.…”

Section: Powder X-ray Diffraction Analysis (Pxrd)supporting

confidence: 80%

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Synthesis and Characterization of a Novel Mucoadhesive Derivative of Psyllium Seed Polysaccharide

Rao¹,

Gaikwad²,

Shevate³

2017

Int J Pharm Pharm Sci

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Objective: In the present study, thiol-functionalization of psyllium seed polysaccharide (PSY) was cross-linked with thioglycolic acid by esterification in an attempt to reveal the mucoadhesive properties of thiolated psyllium seed polysaccharide (TPSY). Methods:The crosslinking was carried out by the microwave-assisted method. A simplex centroid design was employed to systematically study the mucoadhesive strength, mucoadhesive retention time and drug release profile. Comparative evaluation of carbopol-based ciprofloxacin hydrochloride (HCl) tablets containing PSY and TPSY was carried out. Acute oral toxicity studies and repeated oral toxicity for TPSY were also conducted.Results: Thiol-functionalization was confirmed by-SH stretch in Fourier Transform infra-red spectra at 2353 cm -1 . Thiolation was observed in thiolated PSY (TPSY) by a change in the surface morphology of psyllium from fibrous to granular and resulted in 82 %swelling in deionized water. TPSY was found to contain 102.35 mmol of thiol groups/g as determined by the Ellman's method. The percent increase in mucoadhesive strength of TPSY was found to be 50.31 % as compared to PSY and 128.30 % as compared to carbopol. The percent increase in mucoadhesive retention time of TPSY was found to be 110 % as compared to PSY and 50 % as compared to carbopol. Conclusion:Mucoadhesion strength and mucoadhesive retention time were greater of tablets containing a higher amount of TPSY. Further, the acute oral toxicity studies and repeated oral toxicity for TPSY proved it as non-toxic and hence safe for human use.

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Section: Powder X-ray Diffraction Analysis (Pxrd)supporting

confidence: 80%

“…Pseudoplastic systems are shear thinning in nature and are characterised by structural rigidity at rest. Application of shear results in the breakdown of the structure and an apparent fall in viscosity due to the release of entrapped water molecules [33]. TPSY exhibited a sudden breakdown in structure with increase in shear rate.…”

Section: Rheological Datamentioning

confidence: 99%

Synthesis and Characterization of a Novel Mucoadhesive Derivative of Psyllium Seed Polysaccharide

Rao¹,

Gaikwad²,

Shevate³

2017

Int J Pharm Pharm Sci

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“…gastrointestinal tract could be helpful in reducing the insulin burst release. 32,33 Relevant approaches include enteric coating and/or modification of NP surfaces. Thus, Eudragit S100 and HP-55 have demonstrated potential as enteric coatings for insulin-loaded L/C NPs.…”

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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“…3,4 Orally delivered insulin undergoes a hepatic bypass before entering the circulation, so it has the potential to mimic the effects of pancreas-secreted insulin in terms of inhibiting hepatic gluconeogenesis and hepatic glucose output. [5][6][7][8] Many different strategies have been attempted to develop a biologically active oral insulin formulation. It is generally acknowledged that degradation of protein drug by the harsh conditions of the gastrointestinal (GI) tract, including gastric medium and digestive enzymes, is a major obstacle.…”

Section: Introductionmentioning

confidence: 99%

pH-sensitive poly(lactide-co-glycolide) nanoparticle composite microcapsules for oral delivery of insulin

Sun¹,

Liang²,

Yamamoto³

et al. 2015

IJN

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This study proposes a new concept of pH-sensitive poly(lactide-co-glycolide) (PLGA) nanoparticle composite microcapsules for oral delivery of insulin. Firstly, insulin–sodium oleate complex was prepared by the hydrophobic ion pairing method and then encapsulated into PLGA nanoparticles by the emulsion solvent diffusion method. In order to reduce the burst release of insulin from PLGA nanoparticles and deliver insulin to specific gastrointestinal regions, hence to enhance bioavailability of insulin, the PLGA nanoparticles were further encapsulated into Eudragit ® FS 30D to prepare PLGA nanoparticle composite microcapsules by organic spray-drying method. The preparation was evaluated in vitro and in vivo, and the absorption mechanism was discussed. The in vitro drug release studies revealed that the drug release was pH dependent, and the in vivo results demonstrated that the formulation of PLGA nanoparticle composite microcapsules was an effective candidate for oral insulin delivery.

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Polymeric hydrogels for oral insulin delivery

Cited by 218 publications

References 100 publications

Synthesis and Characterization of a Novel Mucoadhesive Derivative of Psyllium Seed Polysaccharide

Synthesis and Characterization of a Novel Mucoadhesive Derivative of Psyllium Seed Polysaccharide

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

pH-sensitive poly(lactide-co-glycolide) nanoparticle composite microcapsules for oral delivery of insulin

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