Nanoparticles of glycol chitosan and its thiolated derivative significantly improved the pulmonary delivery of calcitonin

Makhlof, Abdallah; Werle, Martin; Tozuka, Yuichi; Takeuchi, Hirofumi

doi:10.1016/j.ijpharm.2010.07.001

Cited by 96 publications

(47 citation statements)

References 24 publications

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“…13,14,29 On the other hand, glycol chitosan, an ethylene glycol conjugated form, is known to have greater water solubility and to retain its positive charges. 12 Consequently, glycol chitosan is more mucoadhesive due to increased electrostatic attraction, hydrogen bonding, and hydrophobicity. 30 In the present study, chitosan-coated PLGA NPs were found to be better adsorbed by A549 cells (Figure 3).…”

Section: Discussionmentioning

confidence: 99%

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Long-acting inhalable chitosan-coated poly(lactic-co-glycolic acid) nanoparticles containing hydrophobically modified exendin-4 for treating type 2 diabetes

Lee¹,

Choi²,

Kim³

et al. 2013

IJN

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Inhalable glycol chitosan-coated poly(lactic-co-glycolic acid) (PLGA) nanoparticles containing palmitic acid-modified exendin-4 (Pal-Ex4) (chitosan Pal-Ex4 PLGA NPs) were prepared and characterized. The surface morphology, particle size, and zeta potential of chitosan Pal-Ex4 PLGA NPs were investigated, and the adsorption and cytotoxicity of chitosan Pal-Ex4 PLGA NPs were evaluated in human lung epithelial cells (A549). Finally, the lung deposition characteristics and hypoglycemia caused by chitosan Pal-Ex4 PLGA NPs were evaluated after pulmonary administration in imprinting control region (ICR) and type 2 diabetic db/db mice. Results showed that chitosan Pal-Ex4 PLGA NPs were spherical, compact and had a diameter of ∼700 nm and a positive surface charge of +28.5 mV. Chitosan-coated PLGA NPs were adsorbed onto A549 cells much more so than non-coated PLGA NPs. Pal-Ex4 release from chitosan-coated PLGA NPs was delayed by as much as 1.5 days as compared with chitosan-coated Ex4 PLGA NPs. In addition, chitosan-coated PLGA NPs remained in the lungs for ∼72 hours after pulmonary administration, whereas most non-coated PLGA NPs were lost at 8 hours after administration. Furthermore, the hypoglycemic efficacy of inhaled chitosan Pal-Ex4 PLGA NPs was 3.1-fold greater than that of chitosan Ex4 PLGA NPs in db/db mice. The authors believe chitosan Pal-Ex4 PLGA NPs have considerable potential as a long-acting inhalation delivery system for the treatment of type 2 diabetes.

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Section: Discussionmentioning

confidence: 99%

“…[12][13][14] Chitosan, the N-acetylated derivative of chitin, has been widely used as a building material for nanoparticles. It has excellent biocompatibility and biodegradability characteristics, and little toxicity, presumably because of its natural origin.…”

Section: Introductionmentioning

confidence: 99%

Long-acting inhalable chitosan-coated poly(lactic-co-glycolic acid) nanoparticles containing hydrophobically modified exendin-4 for treating type 2 diabetes

Lee¹,

Choi²,

Kim³

et al. 2013

IJN

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“…Chitosan has a hydrophilic chemical group and is the only positively charged natural material (Muzio et al, 2010) that can provide good adhesion with negatively charged cells. Chitosan also has antibacterial effects that can provide a sterile environment for cell growth (Aimin et al, 1999;Makhlof et al, 2010;Wang et al, 2011). Previous experiments confirmed the strong absorbent ability of the fibroin protein/chitosan scaffolds, allowing cells to be absorbed in the scaffolds during the vaccination.…”

Section: A D C Bmentioning

confidence: 99%

Fibroin protein/chitosan scaffolds and bone marrow mesenchymal stem cells culture in vitro

Deng¹,

She²,

Huang³

et al. 2014

Genet. Mol. Res.

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ABSTRACT.A previous experiment demonstrated that fibroin protein and chitosan mixed in proper proportion presented good physical and chemical properties and biological characteristics, which can make up for their respective disadvantages. To observe the growth of bone marrow mesenchymal stem cells (BMSCs) on these fibroin protein/ chitosan 3D scaffolds, induced rabbit BMSCs were seeded on fibroin protein/chitosan scaffolds. The cell adhesion rate was measured, and cell growth was observed under an inverted microscope and a scanning electron microscope. The cell adhesion rate increased with time. The inverted microscope observations showed that the cells on fibroin protein/chitosan scaffolds could not be seen clearly. As time passed, the number of cells around the stent increased and some cells stretched inside the scaffolds. Electron microscopy showed active cell growth and normal proliferation, and the granular and filamentous matrix substances could be seen around cells. The microfilaments of cell and scaffold materials were tightly connected. The cells not only grew on the surface of the adherent material, but also stretched inside of the materials. These results indicated that the fibroin protein/ chitosan mixed scaffolds have good biocompatibility.

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“…The polymeric carrier can maintain the drug in a specific location in the body, have a prolonged duration of contact with the tissue, and increase the treatment efficiency. This is important since localizing the drug at a targeted site of absorption and transporting the drug across the intestinal epithelial layer are two problems associated with the low bioavailability that often plagues oral insulin delivery (Huang et al, 2003;Makhlof et al, 2010). Among these carriers, the pH-sensitive graft polymers of methacrylic acid and polyethylene glycol have been widely investigated for oral delivery of insulin (Chang and Hsiao, 1989;Samir and Sakr, 2003;Ebube and Jone 2004;Damgé et al, 2007).…”

Section: Introductionmentioning

confidence: 99%

Microspheres of insulin-Eudragit complex: Formulation, characterization and in vivo studies

Momoh¹,

Jackson²,

Musiliu³

et al. 2017

Afr. J. Pharm. Pharmacol.

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Insulin, a hormonal drug for the management of diabetes mellitus has continued to attract attention of many researchers and pharmaceutical formulators for more than a decade. However, its low oral bioavailability due to the activities of intestinal enzymes restricts its route of administration to only the parenteral route. This study was designed to evaluate the capacity of mucoadhesive microspheres formulated with varying blends of Eudragit ® RL 100 and Eudragit ® RS 100 to protect insulin for oral administration. Microspheres containing varying blends of Eudragit ® RL 100/RS100 loaded insulin was prepared by solvent evaporation method and were characterized in vitro and in vivo. Results showed that stable formulation with high encapsulation efficiency, positive zeta potential and high bioadhesion were obtained in all the formulations. In vitro release showed a maximum release of 9 and 87% release in pH 1.2 and 7.2, respectively. Single oral studies showed a decreased in blood glucose level comparably equal to that of subcutaneous (sc) administration. The results of this study indicate that insulin-loaded Eudragit RL100/RS100 microspheres could be a promising drug delivery system to improve oral absorption of insulin.

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Nanoparticles of glycol chitosan and its thiolated derivative significantly improved the pulmonary delivery of calcitonin

Cited by 96 publications

References 24 publications

Long-acting inhalable chitosan-coated poly(lactic-co-glycolic acid) nanoparticles containing hydrophobically modified exendin-4 for treating type 2 diabetes

Long-acting inhalable chitosan-coated poly(lactic-co-glycolic acid) nanoparticles containing hydrophobically modified exendin-4 for treating type 2 diabetes

Fibroin protein/chitosan scaffolds and bone marrow mesenchymal stem cells culture in vitro

Microspheres of insulin-Eudragit complex: Formulation, characterization and in vivo studies

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