Thiolated chitosans

Bernkop‐Schnürch, Andreas; Hornof, M.; Guggi, D.

doi:10.1016/s0939-6411(03)00147-4

Cited by 222 publications

(138 citation statements)

References 46 publications

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“…Thiolated CS were synthesised and utilised for oral controlled drug delivery due to its mucoadhesive nature and high stability of the carrier matrix which provided good controlled release of the drug (49,107,108). Here, the primary amino groups of CS were coupled with the thiol-bearing functional groups to form thiolated CS (108).…”

Section: Thiolated Chitosanmentioning

confidence: 99%

Recent Advancement of Chitosan-Based Nanoparticles for Oral Controlled Delivery of Insulin and Other Therapeutic Agents

2010

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Abstract. Nanoparticles composed of naturally occurring biodegradable polymers have emerged as potential carriers of various therapeutic agents for controlled drug delivery through the oral route. Chitosan, a cationic polysaccharide, is one of such biodegradable polymers, which has been extensively exploited for the preparation of nanoparticles for oral controlled delivery of several therapeutic agents. In recent years, the area of focus has shifted from chitosan to chitosan derivatized polymers for the preparation of oral nanoparticles due to its vastly improved properties, such as better drug retention capability, improved permeation, enhanced mucoadhesion and sustained release of therapeutic agents. Chitosan derivatized polymers are primarily the quaternized chitosan derivatives, chitosan cyclodextrin complexes, thiolated chitosan, pegylated chitosan and chitosan combined with other peptides. The current review focuses on the recent advancements in the field of oral controlled release via chitosan nanoparticles and discusses about its in vitro and in vivo implications.

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Section: Thiolated Chitosanmentioning

confidence: 99%

Recent Advancement of Chitosan-Based Nanoparticles for Oral Controlled Delivery of Insulin and Other Therapeutic Agents

2010

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“…These salts are soluble in water, the solubility depending on the degree of deacetylation and the pH of solution. To further enhance the solubility of this polymer and to improve its mucoadhesive and permeation enhancing properties, various derivatives such as chitosan glutamate, N-trimethyl chitosan chloride and thiolated chitosans have been developed (6)(7)(8). However, these processes require extensive chemical treatment and processing steps which in turn lead to increased expense and time.…”

Section: Introductionmentioning

confidence: 99%

Characterization of a novel lyophilized chitosan hydrogel complex for the controlled release of a highly water soluble drug, niacinamide.

Ma¹,

Prabhu²

2011

Int J Drug Del

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The purpose of this research was to prepare and characterize a novel lyophilized chitosan-based hydrogel complex (termed CS-M) for controlled drug delivery applications using a highly water soluble model drug, niacinamide. Characterization studies were undertaken to evaluate the physical-chemical properties, polymer swelling, in vitro controlled release kinetics, tissue bioadhesion, intestinal permeability and stability of the novel chitosan complex. Additionally, a comparative analysis was conducted with commercial polymers namely, Carbopol 974P-NF® and hydroxypropyl methylcellulose (HPMC K4M). FT-IR and 1 H NMR studies confirmed that despite alteration in physical structure and morphology of the chitosan complex the chemical properties remained unchanged, when compared to the parent chitosan compound. Polymer swelling studies showed consistency in the structural integrity and water uptake of CS-M compared to other polymers which showed inconsistent swelling and disintegration behavior over a 5 h period. In vitro controlled release profiles of CS-M showed a slower, more controlled release rate of niacinamide than other polymers indicating the influence of polymer swelling capacity on water uptake and subsequent drug release. CS-M demonstrated an overall increase in bioadhesion to intestinal tissue when compared to commercial polymers at same concentrations. Similarly, drug transport through everted sac intestinal tissue showed enhanced absorption properties of CS-M when compared to other polymers. Finally, a 3 month accelerated stability study showed all polymers including CS-M to be stable when formulated with niacinamide. Overall, the modified chitosan-based hydrogel polymer, CS-M, demonstrated enhanced characteristics indicating its potential to be used as a controlled release excipient in oral drug formulations.

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“…Biodegradable microspheres break down completely into harmless metabolites that are easily eliminated through natural body functions. Polymers such as chitosan, gelatin, polylactic acids and their derivatives have all been extensively studied for their ability to form microspheres (4,8,9).…”

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confidence: 99%

Mucuna gum microspheres for oral delivery of glibenclamide: In vitro evaluation

Attama

Nwabunze²

2007

Acta Pharmaceutica

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Microspheres refer to the micro-particulate polymer based drug delivery system with an average particle size larger than 1 µm. Microsphere carrier systems made from naturally occurring biodegradable polymers have attracted considerable attention for several 161 Acta Pharm. 57 (2007) An investigation into the suitability of mucuna gum microspheres for oral delivery of glibenclamide is presented. Mucuna gum microspheres were formulated under different conditions of polymer concentration and crosslinking time at constant speed. The formulated microspheres were thereafter loaded with glibenclamide by the remote loading process. The microspheres were evaluated according to particle size, yield, loading efficiency and swelling.In vitro release of glibenclamide from the microspheres was studied in simulated intestinal fluid (SIF, pH 7.4). The release data was fitted into two release models to investigate the mechanism of glibenclamide release from the microspheres. All the microspheres showed good swelling characteristics in distilled water. The investigation revealed that the microspheres produced with 5% (m/V) mucuna gum with a crosslinking time of 5 h had the optimum prolonged release pattern. The microspheres produced using 10% (m/V) mucuna gum with a crosslinking time of 1 h had the highest delayed release of the incorporated drug, whereas those without crosslinking had the fastest release. The Ritger-Peppas case I transport model appeared to have adequately described the release process as about 54% of the batches of microspheres conformed to this model. This implies that a formulation of glibenclamide-loaded mucuna gum microspheres is likely to offer a reliable means of delivering glibenclamide by the oral route.

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Thiolated chitosans

Cited by 222 publications

References 46 publications

Recent Advancement of Chitosan-Based Nanoparticles for Oral Controlled Delivery of Insulin and Other Therapeutic Agents

Recent Advancement of Chitosan-Based Nanoparticles for Oral Controlled Delivery of Insulin and Other Therapeutic Agents

Characterization of a novel lyophilized chitosan hydrogel complex for the controlled release of a highly water soluble drug, niacinamide.

Mucuna gum microspheres for oral delivery of glibenclamide: In vitro evaluation

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