Peroral delivery of insulin using chitosan derivatives: A comparative study of polyelectrolyte nanocomplexes and nanoparticles

Jintapattanakit, Anchalee; Junyaprasert, Varaporn Buraphacheep; Mao, Shirui; Sitterberg, Johannes; Bakowsky, Udo; Kissel, Thomas

doi:10.1016/j.ijpharm.2007.05.015

Cited by 136 publications

(79 citation statements)

References 45 publications

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“…Interestingly, it was observed that PEC with TMC and PEG-graft-TMC copolymer were more stable in SIF and could efficiently protect insulin from proteolytic enzymes when compared to the NPs (72). Despite this drawback, other researchers have continued their investigation on CS derivatives for NP preparation for oral delivery of therapeutic agents.…”

Section: Trimethyl 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: Trimethyl Chitosanmentioning

confidence: 99%

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

2010

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“…However, limited solubility has prevented its widespread use. 9,10 The mucoadhesive and absorption-promoting properties of chitosan have been extensively evaluated. The positive charge gained in acidic pH conditions, in which chitosan has high solubility, appears to be effective for enhanced absorption.…”

Section: Introductionmentioning

confidence: 99%

Enteric trimethyl chitosan nanoparticles containing hepatitis B surface antigen for oral delivery

Farhadian

Dounighi

Avadi³

2015

Human Vaccines & Immunotherapeutics

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Oral vaccination is the preferred route of immunization. However, the degradative condition of the gastrointestinal tract and the higher molecular size of peptides pose major challenges in developing an effective oral vaccination system. One of the most excellent methods used in the development of oral vaccine delivery system relies on the entrapment of the antigen in polymeric nanoparticles. In this work, trimethyl chitosan (TMC) nanoparticles were fabricated using ionic gelation teqnique by interaction hydroxypropyl methylcellulose phthalate (HPMCP), a pHsensitive polymer, with TMC and the utility of the particles in the oral delivery of hepatitis B surface antigen (HBsAg) was evaluated employing solutions that simulated gastric and intestinal conditions. The particle size, morphology, zeta potential, loading capacity, loading efficiency, in vitro release behavior, structure, and morphology of nanoparticles were evaluated, and the activity of the loaded antigen was assessed. Size of the optimized TMC/HPMCP nanoparticles and that of the antigen-loaded nanoparticles were 85 nm and 158 nm, respectively. Optimum loading capacity (76.75%) and loading efficiency (86.29%) were achieved at 300 mg/mL concentration of the antigen. SEM images revealed a spherical shape as well as a smooth and near-homogenous surface of nanoparticles. Results of the in vitro release studies showed that formulation with HPMCP improved the acid stability of the TMC nanoparticles as well as their capability to preserve the loaded HBsAg from gastric destruction. The antigen showed good activity both before and after loading. The results suggest that TMC/HPMCP nanoparticles could be used in the oral delivery of HBsAg vaccine.

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“…The animals fasted for another 0.5 h, then the small intestine (jejunum) was recovered and frozen in liquid nitrogen in the presence of tissue-freezing medium OCT (VWR, Atlanta, GA). The frozen tissues were sectioned into 10 mm thick specimens using a Leica 3050 microtome, then observed by CLSM (Jintapattanakit et al, 2007;Zou et al, 2010;Sonia et al, 2011).…”

Section: Determination Of Ins Absorbed By Intestine Ex Vivo and In Vivomentioning

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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Peroral delivery of insulin using chitosan derivatives: A comparative study of polyelectrolyte nanocomplexes and nanoparticles

Cited by 136 publications

References 45 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

Enteric trimethyl chitosan nanoparticles containing hepatitis B surface antigen for oral delivery

A natural lipopeptide of surfactin for oral delivery of insulin

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