Engineering Polysaccharide-Based Polymeric Micelles to Enhance Permeability of Cyclosporin A Across Caco-2 Cells

Francis, Mira; Cristea, Mariana; Yang, Yuhong; Winnik, F. M.

doi:10.1007/s11095-004-1188-0

Cited by 79 publications

(48 citation statements)

References 81 publications

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“…In particular, these studies were carried out in fasted state simulated gastric fluid (FaSSGF) at pH 1.6 for 4 h to mimic gastric conditions, in fasted state simulated intestinal fluid (FaSSIF) at pH 6.5 for 24 h to mimic intestinal conditions, and in phosphate buffer solution (PBS) at pH 7.4/foetal calf serum (FCS) (50:50) for 24 h to mimic extracellular and plasmatic conditions (Francis et al, 2005;Roger et al, 2010;Zhang et al, 2011).…”

Section: Drug Release Studiesmentioning

confidence: 99%

Galactosylated polymeric carriers for liver targeting of sorafenib

Craparo

Sardo

Serio

et al. 2014

International Journal of Pharmaceutics

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Section: Drug Release Studiesmentioning

confidence: 99%

Galactosylated polymeric carriers for liver targeting of sorafenib

Craparo

Sardo

Serio

et al. 2014

International Journal of Pharmaceutics

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“…In addition, aiming to study the effect of nanoparticle concentration on the permeability in vitro, we conducted the same assay using crosslinked nanoparticles in two concentrations, namely 0.05% and 0.01% w/v. It is worth stressing that usually, this parameter is usually neglected in the scientific literature [48,49]. The use of non-crosslinked 0.01% w/v systems was precluded because this concentration is below the CMC and thus, the nanoparticles disassembled.…”

Section: Permeability Studiesmentioning

confidence: 99%

Permeability of Novel Chitosan-<em>g</em>-poly (Methyl Methacrylate) Amphiphilic Nanoparticles in a Model of Small Intestine <em>in Vitro</em>

Noi

Schlachet

Kumarasamy

et al. 2018

Preprint

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Engineering of drug nanocarriers combining fine-tuned mucoadhesive/mucopenetrating properties is currently being investigated to ensure more efficient mucosal drug delivery. Aiming to improve the transmucosal delivery of hydrophobic drugs, we designed a novel kind nanogel produced by the self-assembly of amphiphilic chitosan graft copolymers ionotropically crosslinked with sodium tripolyphosphate. In this work, we synthesized for the first time chitosan-gpoly(methyl methacrylate) nanoparticles thiolated by the conjugation of N-acetyl cysteine. First, we confirmed that both non-crosslinked and crosslinked nanoparticles in the 0.05-0.1% w/v concentration range display very good cell compatibility in two cell lines that are relevant to oral delivery, Caco2 cells that mimic the intestinal epithelium and HT29-MTX cells that produce mucin. Then, we evaluated the effect of crosslinking, nanoparticle concentration and thiolation on the permeability in vitro utilizing monolayers of (i) Caco2 and (ii) Caco2:HT29-MTX cells (9:1 cell number ratio). Results confirmed that the ability of the nanoparticles to cross Caco2 monolayer was affected by the crosslinking. In addition, thiolated nanoparticles interact more strongly with mucin, resulting in a decrease of the apparent permeability coefficient (Papp) compared to the pristine nanoparticles. Moreover, for all the nanoparticles, higher concentration resulted in lower Papp suggesting indicating that the transport pathways could undergo saturation.

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“…In a research, intestinal absorption of polymeric micelles loaded by cyclosporine A was compared with cyclosporine A loaded polymeric micelles which were designed by Vitamin B12 on their surface and the results demonstrate the significant increase in intestinal absorption of designed polymeric micelles. [66,67] Despite all these advantages, there are still some drawbacks in using these nanocarriers including polymer synthesis difficulties, slow extravasation and possible liver chronic toxicity due to slow metabolism. Therefore, more research and clinical studies are required to evaluate the polymeric micelles pharmacokinetic and pharmacodynamics.…”

Section: Advantages Disadvantagesmentioning

confidence: 99%

Untitled

Esfahani¹

2017

AJP

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Almost half of the orally administered drugs are poorly soluble in water; therefore they have low absorption in the gastrointestinal (GI) tract. In addition, drugs which are administered orally must remain stable during passing the GI tract, despite different physiologic challenges such as pH changes, and dilution effect. Hence, new methods are needed to increase the solubility of these drugs while making them more stable in the physiologic environment. Polymeric micelles are one of the new nanocarriers which are able to increase the solubility of these drugs while protecting them from pH changes, dilution effect, and biological barriers such as filtration in the spleen or scavenging by the phagocytic system. This article provides some important and basic information including polymeric micelles characteristics, structure, and preparation.

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Engineering Polysaccharide-Based Polymeric Micelles to Enhance Permeability of Cyclosporin A Across Caco-2 Cells

Abstract: Polysaccharide-based polymeric micelles are promising carriers for the oral delivery of poorly water soluble drugs. In vitro tests indicate that, overall, HM-HPC micelles are more effective compared to HM-DEX micelles.

Cited by 79 publications

References 81 publications

Galactosylated polymeric carriers for liver targeting of sorafenib

Galactosylated polymeric carriers for liver targeting of sorafenib

Permeability of Novel Chitosan-<em>g</em>-poly (Methyl Methacrylate) Amphiphilic Nanoparticles in a Model of Small Intestine <em>in Vitro</em>

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