Self-Assembled Polyelectrolyte Nanocomplexes between Chitosan Derivatives and Insulin

Mao, Shirui; Bakowsky, Udo; Jintapattanakit, Anchalee; Kissel, Thomas

doi:10.1002/jps.20520

Cited by 167 publications

(96 citation statements)

References 28 publications

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“…Turbidimetric titrations consist in the measurement of the decrease in the intensity of a light flow passing through a solution with particles in suspension and is proportional to both molecular weight and the concentration of the particles in the solution [45]. High turbidity indicates a high precipitation of the particles that occurs when the polymers are neutralized.…”

Section: Potentiometric and Turbidimetric Titrationsmentioning

confidence: 99%

Films based on chitosan polyelectrolyte complexes for skin drug delivery: Development and characterization

Silva

Pereira

Ramalho

et al. 2008

Journal of Membrane Science

116

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a b s t r a c tNovel chitosan based polyelectrolyte complexes (PEC) were developed and optimized in order to obtain films possessing the optimal functional properties (flexibility, resistance, water vapour transmission rate and bioadhesion) to be applied on skin. The development was based on the combination of chitosan and two polyacrylic acid (PAA) polymers with different crosslinkers and crosslinking densities. The interaction between the polymers was maximized controlling the pH, and by forming the films at a pH value close to the pK a of the respective components as identified by potentiometric and turbidimetric titrations. The action of glycerol, PEG200, Hydrovance and trehalose upon the functional properties of the films was also evaluated. Glycerol was found to improve the film properties in terms of flexibility, resistance and water vapour transmission rate (WVTR) with a maximum effect at 30%. The application of a pressure sensitive adhesive (PSA) significantly improved bioadhesion with a negligible influence in the resistance and flexibility of the films.The optimized film, including adhesive, has shown very good properties for application in the skin and represents a very promising formulation for further incorporation of drugs for topical and transdermal administration.

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Section: Potentiometric and Turbidimetric Titrationsmentioning

confidence: 99%

Films based on chitosan polyelectrolyte complexes for skin drug delivery: Development and characterization

Silva

Pereira

Ramalho

et al. 2008

Journal of Membrane Science

116

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show abstract

“…12 Significant progress has been achieved in synthesizing and purifying chitosan, as well as in applications of modified chitosan NPs for efficient oral insulin delivery. 13,14 However, the above-mentioned methods have drawbacks, such as the requirement of chemical cross-linking agents and/or repeated washing and precipitation steps. Based on the development of the self-assembly technique, a novel self-assembled nanoparticulate system consisting of lecithin and chitosan was fabricated by the solvent-injection method.…”

Section: Introductionmentioning

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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“…The positive charge gained in acidic pH conditions, in which chitosan has high solubility, appears to be effective for enhanced absorption. 11 With due attention to very low solubility of chitosan above pH 6.5, its application is limited to absorption facilitator in the body. Therefore, chitosan derivatives with enhanced solubility at basic and neutral pH are essential.…”

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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Self-Assembled Polyelectrolyte Nanocomplexes between Chitosan Derivatives and Insulin

Cited by 167 publications

References 28 publications

Films based on chitosan polyelectrolyte complexes for skin drug delivery: Development and characterization

Films based on chitosan polyelectrolyte complexes for skin drug delivery: Development and characterization

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

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

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