In Vivo Evaluation of Thiolated Chitosan Tablets for Oral Insulin Delivery

Millotti, Gioconda; Laffleur, Flavia; Perera, Glen; Vigl, Claudia; Pickl, Karin E.; Sinner, Frank; Bernkop‐Schnürch, Andreas

doi:10.1002/jps.24102

Cited by 47 publications

(24 citation statements)

References 24 publications

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“…Thus, the thiolation of CS plays a pivotal role in enhancing mucoadhesion and anti-inflammatory properties. The increased mucoadhesion of TCS is well-documented in literature (Lee et al 2006, Zhu et al 2012, Milloti et al 2014, Boateng and Ayensu 2014.The TCS was prepared as described by Lee et al (2006). The chemical modification of CS and freeze-dried TCS resulted in a fibrous white powder easily soluble in water.…”

Section: Resultsmentioning

confidence: 97%

Pharmacological evaluation of nasal delivery of selegiline hydrochloride-loaded thiolated chitosan nanoparticles for the treatment of depression

Singh

Rashid

Hallan

et al. 2015

Artificial Cells, Nanomedicine, and Biotechnology

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The aim of the present study was to investigate the propensity of thiolated chitosan nanoparticles (TCNs) to enhance the nasal delivery of selegiline hydrochloride. TCNs were synthesized by the ionic gelation method. The particle size distribution (PDI), entrapment efficiency (EE), and zeta potential of modified chitosan (CS) nanoparticles were found to be 215 ± 34.71 nm, 70 ± 2.71%, and + 17.06 mV, respectively. The forced swim and the tail suspension tests were used to evaluate the anti-depressant activity, in which elevated immobility time was found to reduce on treatment. TCNs seem to be promising candidates for nose-to-brain delivery in the evaluation of antidepressant activity.

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Section: Resultsmentioning

confidence: 97%

Pharmacological evaluation of nasal delivery of selegiline hydrochloride-loaded thiolated chitosan nanoparticles for the treatment of depression

Singh

Rashid

Hallan

et al. 2015

Artificial Cells, Nanomedicine, and Biotechnology

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“…As compared to previous studies on mucoadhesion of anionic polymers 28,29 , we could show pronounced mucoadhesive properties for an at least 2-fold smaller polymer than the so far tested smallest polymer. The mucoadhesive properties of thiolated chitosan 20 kDa have been shown earlier both as coating for nanoparticles 30 and in tablet form 31 , although there was no focus on the mucoadhesive properties of LMWPs.…”

Section: Discussionmentioning

confidence: 98%

Can thiolation render a low molecular weight polymer of just 20-kDa mucoadhesive?

Mahmood

Bonengel

Laffleur

et al. 2015

Drug Development and Industrial Pharmacy

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The objective was to investigate whether even low-molecular weight polymers (LMWPs) can be rendered mucoadhesive due to thiolation. Interceded by the double catalytic system carbodiimide/N-hydroxysuccinimide, cysteamine was covalently attached to a copolymer, poly(4-styrenesulfonic acid-co-maleic acid) (PSSA-MA) exhibiting a molecular weight of just 20 kDa. Depending on the amount of added N-hydroxysuccinimide and cysteamine, the resulting PSSA-MA-cysteamine (PC) conjugates exhibited increasing degree of thiolation, highest being "PC 2300" exhibiting 2300.16 ± 149.86 μmol thiol groups per gram of polymer (mean ± SD; n = 3). This newly developed thiolated polymer was evaluated regarding mucoadhesive, rheological and drug release properties as well from the toxicological point of view. Swelling behavior in 100 mM phosphate buffer pH 6.8 was improved up to 180-fold. Furthermore, due to thiolation, the mucoadhesive properties of the polymer were 240-fold improved. Rheological measurements of polymer/mucus mixtures confirmed results obtained by mucoadhesion studies. In comparison to unmodified polymer, PC 2300 showed 2.3-, 2.3- and 2.4-fold increase in dynamic viscosity, elastic modulus and viscous modulus, respectively. Sustained release of the model drug codeine HCl out of the thiomer was provided for 2.5 h (p < 0.05), whereas the drug was immediately released from the unmodified polymer. Moreover, the thiomer was found non-toxic over Caco-2 cells for a period of 6- and 24-h exposure. Findings of the present study provide evidence that due to thiolation LMWPs can be rendered highly mucoadhesive as well as cohesive and that a controlled drug release out of such polymers can be provided.

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“…Apart from enteric coating, unmodified chitosan was used as an absorption enhancer in our study. Chitosan is often used in oral formulations to improve the bioavailability of proteins because of its mucoadhesive properties . Chitosan possesses permeation‐enhancing effects and is capable of opening the tight junctions transiently for oral protein delivery .…”

Section: Discussionmentioning

confidence: 99%

“…The effects of absorption‐enhancing and mucoadhesive properties were studied using 2.75 mg insulin and 7.25 mg unmodified chitosan in an animal study. When compared to the usual subcutaneous insulin injection route, the oral formulation had a relative bioavailability of 3.19%, and decrease in blood glucose level was reported …”

Section: Discussionmentioning

confidence: 99%

In-vitro evaluation of enteric coated insulin tablets containing absorption enhancer and enzyme inhibitor

Wong

Martinez

Carnagarin

et al. 2017

Journal of Pharmacy and Pharmacology

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In Vivo Evaluation of Thiolated Chitosan Tablets for Oral Insulin Delivery

Cited by 47 publications

References 24 publications

Pharmacological evaluation of nasal delivery of selegiline hydrochloride-loaded thiolated chitosan nanoparticles for the treatment of depression

Pharmacological evaluation of nasal delivery of selegiline hydrochloride-loaded thiolated chitosan nanoparticles for the treatment of depression

Can thiolation render a low molecular weight polymer of just 20-kDa mucoadhesive?

In-vitro evaluation of enteric coated insulin tablets containing absorption enhancer and enzyme inhibitor

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