The mechanism of enhancement on oral absorption of paclitaxel by N-octyl-O-sulfate chitosan micelles

Mo, Ran; Xiang, Jun; Li, Nan; Ju, Caoyun; Sun, Minjie; Zhang, Can; Ping, Qineng

doi:10.1016/j.biomaterials.2011.03.005

Cited by 182 publications

(124 citation statements)

References 42 publications

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“…These results indicated that the involvement of energy-dependent active transport process for micelles and NPs. However, in the presence of chlorpromazine, the cellular uptake of T-NPs and FQS-NPs remarkably decreased to 72.1% (p50.05) and 51.9% (p50.01) (Figure 4), respectively, while there was no significant change in micelles group, suggesting that the endocytosis of T-NPs/FQS-NPs was specifically clathrin-mediated (Mo et al, 2011). This phenomenon might be caused by the different surface properties possessed between NPs and micelles.…”

Section: Endocytosis Pathway Studiesmentioning

confidence: 89%

A novel ligand conjugated nanoparticles for oral insulin delivery

et al. 2015

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In order to enhance the interaction between nanocarrier and gastrointestinal epithelial cells, we developed nanoparticles (NPs) modified with targeting ligand FQSIYPpIK (FQS), which specifically interact with integrin avb3 receptor expressing on the intestinal epithelium. The targeting NPs were prepared by coating the insulin-loaded poly(lactide-co-glycolide)-monomethoxy-poly(polyethylene glycol) micelle cores with FQS modified trimethyl chitosan chloride. In in vitro study, the fabricated NPs showed ameliorated drug release profile and improved enzymatic stability compared with micelles alone. In the integrin avb3 receptor over-expressed Caco-2 cells model, FQS modified NPs exhibited significantly accelerated intracellular uptake due to the active ligand-receptor mediation. Meanwhile, the targeting NPs also showed enhanced transport across the Caco-2 monolayer cells via both transcellular and paracellular pathways. Besides, orally administered FQS modified NPs produced a prominent hypoglycemic response and an increase of the serum insulin concentration in diabetic rats. Both in vitro and in vivo results demonstrated the FQS peptide modified NPs as promising intestinal cell-targeting nanocarriers for efficient oral delivery of insulin.

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Section: Endocytosis Pathway Studiesmentioning

confidence: 89%

A novel ligand conjugated nanoparticles for oral insulin delivery

et al. 2015

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“…Compared with injection, it shows more convenience, better patient compliance, less cost and more chronic treatment regimen (Russell-Jones, 2004;Simoes et al, 2015). However, as the result of the poor solubility (0.25 mg/mL), the action of the multidrug efflux transporter P-gp, highly expressed in intestinal tract, as well as the extensive first-pass metabolisms by either the intestinal or liver cytochrome P450 enzymes like CYP3A4, the oral bioavailability of PTX is even less than 10% (Mo et al, 2011).…”

Section: Introductionmentioning

confidence: 99%

“…Due to these problems, many efforts have been taken to develop an alternative oral delivery system for PTX to improve its poor solubility and low permeability across the intestinal barrier as well as overcome the multidrug resistance against it (Nornoo et al, 2009;Agueros et al, 2010;Mo et al, 2011;Yao et al, 2011). Among these drug delivery systems, polymeric micelles have gained considerable attention owing to their unique core/shell structure and high loading capacity for drugs (Kataoka et al, 2001;Nishiyama & Kataoka, 2006).…”

Section: Introductionmentioning

confidence: 99%

“…For example, clinically, Taxol is a commercial preparation of PTX for intravenous administration and is composed of 50:50 (v/v) mixtures of Cremophor EL and dehydrated alcohol. Unfortunately, Cremophor EL causes severe adverse effects, such as hypersensitivity, nephrotoxicity and neurotoxicity (Mo et al, 2011;Vader et al, 2013). Thus, many alternative delivery systems for PTX have been developed.…”

Section: Introductionmentioning

confidence: 99%

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Preparation of sodium cholate-based micelles through non-covalent ıbonding interaction and application as oral delivery systems for paclitaxel

Zhao

2015

Drug Delivery

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In present study, two types of micelles based on sodium cholate (NaC) were prepared through non-covalent bonding interaction and the potential of micelles as oral drug delivery systems for paclitaxel (PTX) was evaluated. Pluronic-chitosan (F127-CS) and Pluronic-poly (acrylic acid) (F127-PAA) copolymers were synthesized. Electrostatic interaction and hydrogen bond were used to prepare F127-CS/NaC micelles and F127-PAA/NaC micelles, respectively. The physicochemical characteristics of micelles were determined. An average diameter of 67.5 nm and unimodal pattern of size distribution were observed for F127-CS/NaC micelles. While for F127-PAA/NaC micelles, an average diameter of 85.89 nm and non-unimodal pattern of size distribution were observed. The results revealed that F127-CS/NaC micelles were more integrated than F127-PAA/NaC micelles. Further experiments showed that the F127-CS/NaC micelles had a higher drug-loading content of 12.8% and a lower critical micelle concentration (CMC) of 2.5 Â 10 À3 mol/L compared with F127-PAA/NaC micelles. In vitro cytotoxicity analysis demonstrated that the PTX-loaded F127-CS/NaC micelles were of great efficiency in inhibiting the growth of drug-resistant breast cancer MCF-7 cells (MCF-7/Adr). The intragastric administration of the PTX-loaded F127-CS/NaC micelles in rats provided a 4.33-fold higher absolute bioavailability compared to commercial Taxol Õ , indicating an efficient oral absorption of PTX delivered by micelles. These findings signify that F127-CS/NaC micelle may be a promising carrier for the delivery of PTX.

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“…For PTX, plenty of works have arisen lately to attempt its oral administration. Alternatives vary from the co administration of Taxol® with selective Pgp inhibitors such as cyclosporin A [8], to its encapsulation in drug delivery systems, such as micelles [9,10], self microemulsifying formulations [11], lipid nanoparticles [12,13] or biodegradable polymeric nanoparticle [14 17]. …”

Section: Introductionmentioning

confidence: 99%