In vivo comparison of various polymeric and low molecular mass inhibitors of intestinal P-glycoprotein

Föger, Florian; Hoyer, Herbert; Kafedjiiski, Krum; Thaurer, Michael; Bernkop‐Schnürch, Andreas

doi:10.1016/j.biomaterials.2006.08.004

Cited by 72 publications

(31 citation statements)

References 18 publications

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“…30,31 The nanoparticles were characterized by various methods. As can be seen from the transmission electron microscopic images ( Figure 1A), Cur/SLNs-HU-211 had a spherical shape and uniform size.…”

Section: Characterization Of Nanoparticlesmentioning

confidence: 99%

“…29 Polyoxyethylene (40) stearate (Myrj52), a material used for modifying SLNs, can modulate drug uptake via inhibiting the activity of P-gp. 30,31 In this paper, we aimed to develop and assess SLNs containing Cur and HU-211 (Cur/SLNs-HU-211) for achieving better antidepressant activity. We first synthesized Cur/ SLNs-HU-211 via an emulsification and low-temperature solidification method and examined by means of various apparatus, and then the antidepressant activities of nanoparticles in CORT-induced major depression model were investigated in vitro and in vivo.…”

Section: Introductionmentioning

confidence: 99%

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Antidepressant effects of curcumin and HU-211 coencapsulated solid lipid nanoparticles against corticosterone-induced cellular and animal models of major depression

Zhu

Wang

et al. 2016

IJN

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Major depression is a complex neuropsychiatric disorder with few treatment approaches. The use of nontargeted antidepressants induced many side effects with their low efficacy. A more precise targeting strategy is to develop nanotechnology-based drug delivery systems; hence, we employed solid lipid nanoparticles (SLNs) to encapsulate HU-211 and curcumin (Cur). The antidepressant effects of the dual-drug nanoparticles (Cur/SLNs-HU-211) for major depression treatment were investigated in corticosterone-induced cellular and animal models of major depression. Cur/SLNs-HU-211 can effectively protect PC12 cells from corticosterone-induced apoptosis and can release more dopamine, which may be associated with the higher uptake of Cur/SLNs-HU-211 shown by cellular uptake behavior analysis. Additionally, Cur/SLNs-HU-211 significantly reduced the immobility time in forced swim test, enhanced fall latency in rotarod test, and improved the level of dopamine in mice blood. Cur/SLNs-HU-211 can deliver more Cur to the brain and thus produce a significant increase in neurotransmitters level in brain tissue, especially in the hippocampus and striatum. The results of Western blot and immunofluorescence revealed that Cur/SLNs-HU-211 can significantly enhance the expression of CB1, p-MEK1, and p-ERK1/2. Our study suggests that Cur/SLNs-HU-211 may have great potential for major depression treatment.

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Section: Characterization Of Nanoparticlesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Antidepressant effects of curcumin and HU-211 coencapsulated solid lipid nanoparticles against corticosterone-induced cellular and animal models of major depression

Zhu

Wang

et al. 2016

IJN

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“…There are several papers published, that describe the experimental procedure [43,44]. In brief, the oral dosage form based on the multifunctional polymer is administered either orally or in situ and then drug plasma levels or a therapeutic effect is monitored.…”

Section: Discussionmentioning

confidence: 99%

Analytical Methods for the Characterisation of Multifunctional Polymers for Oral Drug Delivery

Werle¹,

Hsu²,

Chang³

et al. 2007

CPA

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Multifunctional polymers are highly promising auxiliary agents for the oral delivery of a broad variety of drugs. The main features of multifunctional polymers include controlled release, mucoadhesive, cohesive and permeation enhancing properties and enzyme as well efflux pump inhibitory properties. Within the current review, the most important multifunctional polymers for oral drug delivery as well as various analytical methods including the rotating cylinder method, tensile studies, confocal laser scanning microscopy, permeation studies, and also enzyme and efflux pump inhibition studies are discussed.

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“…Recently, it has been demonstrated that thiomers can inhibit efflux pumps in vitro (Werle and Hoffer 2006). These findings have been supported by in vivo studies with the efflux pump substrates rhodamine 123 (Fö ger et al 2006a) and saquinavir (Fö ger et al 2006b). One main feature of this class of polymeric inhibitors is their strongly enhanced mucoadhesiveness that would allow a controlled release of paclitaxel at the same intestinal segments as the efflux pump inhibition takes places (BernkopSchnü rch 2004).…”

Section: Introductionmentioning

confidence: 92%

Effect of a thiolated polymer on oral paclitaxel absorption and tumor growth in rats

Föger

Malaivijitnond

Wannaprasert

et al. 2008

Journal of Drug Targeting

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The anticancer agent paclitaxel is currently commercially available only as an infusion due to its low oral bioavailability. An oral formulation would be highly beneficial for patients. Besides the low solubility, the main reason for the limited oral bioavailability of paclitaxel is that it is a substrate of the efflux pump P-glycoprotein (P-gp). Recently, it has been demonstrated that P-gp can be inhibited by thiolated polymers. In this study, an oral paclitaxel formulation based on thiolated polycarbophil was evaluated in vivo in wild-type rats and in mammary cancer-induced rats. The paclitaxel plasma level after a single administration of paclitaxel was observed for 12 h in healthy rats. Moreover, cancer-induced rats were treated weekly for 5 weeks with the novel formulation. It was demonstrated that (1) co-administration of thiolated polycarbophil significantly improved paclitaxel plasma levels, (2) a more constant pharmacokinetic profile could be achieved and (3) the tumor growth was reduced. These effects can most likely be attributed to P-gp inhibition. According to the achieved results, thiolated polymers are believed to be interesting tools for the delivery of P-gp substrates such as paclitaxel.

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In vivo comparison of various polymeric and low molecular mass inhibitors of intestinal P-glycoprotein

Cited by 72 publications

References 18 publications

Antidepressant effects of curcumin and HU-211 coencapsulated solid lipid nanoparticles against corticosterone-induced cellular and animal models of major depression

Antidepressant effects of curcumin and HU-211 coencapsulated solid lipid nanoparticles against corticosterone-induced cellular and animal models of major depression

Analytical Methods for the Characterisation of Multifunctional Polymers for Oral Drug Delivery

Effect of a thiolated polymer on oral paclitaxel absorption and tumor growth in rats

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