Development of docetaxel-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) for enhanced chemotherapeutic effect

Seo, Youn Gee; Kim, Dae Hwan; Ramasamy, Thiruganesh; Kim, Jeong Hwan; Marasini, Nirmal; Oh, Yu‐Kyoung; Kim, Dong-Wuk; Kim, Jin Ki; Yong, Chul Soon; Kim, Jong Oh; Choi, Han‐Gon

doi:10.1016/j.ijpharm.2013.05.034

Cited by 144 publications

(67 citation statements)

References 49 publications

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“…In general, anti-cancer efficacy of one system will differ from that of another if there is a significant difference in plasma circulation time and t 1/2 parameters, as a prolonged blood circulation time will increase the chance of drug internalization into cancer cells via the enhanced permeability and retention (EPR) effect. 30 However, in the current study, after administration for 4 hours, the plasma levels of DCT were similar for both groups. Although significant differences in pharmacokinetic parameters were observed during the initial time points, it was not sufficient to elicit a pronounced tumor response.…”

contrasting

confidence: 42%

“…Some studies have reported that mice treated with commercial injection shed at least 10% of their body weight and were found to be lethargic with overt signs of severe toxicity. 14,[30][31][32] In contrast, orally administered DCT solution did not have any effect on tumor progression, and tumor volume increased rapidly, equal to that of control.…”

mentioning

confidence: 86%

“…All of these observations led to the speculation that Taxotere ® was very toxic, while the orally administered drug solution did not have any effect on tumor response, and therefore, both are unsuitable. 30 On the other hand, DCTloaded nanomicelles with, and without bile salt were very efficacious in controlling the tumor burden, and, at the same time, completely safe. Furthermore, enhanced anti-tumor efficacy of DCT-loaded nanomicelles was partly attributed to the ability to counter p-gp (ABCB1) mediated efflux activity.…”

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confidence: 99%

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The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles

Kim¹,

Ramasamy²,

Choi³

et al. 2014

IJN

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The primary aim of this work was to investigate the potential of bile salt, sodium taurocholate (NaTC), in improving the bioavailability and anti-tumor efficacy of docetaxel (DCT) upon rectal administration. Poloxamer-based nanomicelles with thermosensitive and mucoadhesive properties were prepared using the cold method. The optimized nanomicellar formulation was evaluated in terms of physicochemical and viscoelastic parameters. Nanomicelles containing bile salt maintained sufficient gelation strength (234×10 2 mPa·s) and mucoadhesive force (17.3×10 2 dyne/cm 2 ) to be retained in the upper part of the rectum. They significantly enhanced the DCT internalization across the rectal mucosa and showed a high plasma level during the first 4 hours of the study period, compared to nanomicelles with no bile salt. As a result, a slightly higher rectal bioavailability of ~33% was observed in nanomicelles containing bile salt, compared to ~28% from the latter system. The higher pharmacokinetic parameters for rectally administered DCT/P407/P188/Tween 80/NaTC (0.25%/11%/15%/10%/0.1% by weight, respectively) resulted in significant anti-tumor efficacy. However, the tumor regression rate for the NaTC group was not statistically different from that for nanomicelles without NaTC. Therefore, overall results suggest that thermosensitive nanomicelles could be a potential dosage form for improvement of the bioavailability and chemotherapeutic profile of DCT.

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confidence: 42%

mentioning

confidence: 86%

mentioning

confidence: 99%

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The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles

Kim¹,

Ramasamy²,

Choi³

et al. 2014

IJN

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“…10 The release profiles of DTX from DTX-LPH were evaluated in PBS (pH =7.4) and ABS (pH =5.0) ( Figure 2D). In both release media, DTX-LPH exhibited a biphasic release pattern, with 20% of the drug released within the first 24 hours, followed by a sustained release pattern over the next 24 hours.…”

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confidence: 99%

Tumor-targeting, pH-sensitive nanoparticles for docetaxel delivery to drug-resistant cancer cells

Kim¹,

Tran²,

Ramasamy³

et al. 2015

IJN

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The attachment of polyethylene glycol (PEG) increases the circulation time of drug-containing nanoparticles; however, this also negatively affects cellular uptake. To overcome this problem, unique lipid polymer hybrid (LPH) nanoparticles were developed with a pH-responsive PEG layer that detached prior to cell uptake. Docetaxel (DTX) was incorporated into the lipid core of the nanoparticles, which was then shielded with the pH-responsive block co-polymer polyethylene glycol- b -polyaspartic acid (PEG- b -PAsp) using a modified emulsion method. The optimized LPH nanoparticles were ~200 nm and had a narrow size distribution. Drug release from DTX-loaded LPH (DTX-LPH) nanoparticles was pH-sensitive, which is beneficial for tumor targeting. More importantly, DTX-LPH nanoparticles were able to effectively induce apoptosis in cancer cells. The negative surface charge and PEG shell of vehicle remarkably enhanced the blood circulation and physiological activity of DTX-LPH nanoparticles compared with that of free DTX. The nanoparticles were also found to reduce the size of tumors in tumor-bearing xenograft mice. The in vivo anticancer effect of DTX-LPH nanoparticles was further confirmed by the elevated levels of caspase-3 and poly ADP ribose polymerase found in the tumors after treatment. Thus, the results suggest that this novel LPH system could be an effective new treatment for cancer.

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“…One way to circumvent this problem and render emulsions more attractive for use could be to transform them into dry powdered nanoemulsions. First described in the early 1960s, a dry powdered emulsion, a type of nanoparticle, is a dispersion of an immiscible oil phase within a solid phase, and is achieved by elimination of the aqueous phase of a liquid emulsion by spray-drying, 16 lyophilization, 17 and later solvent evaporation. 18,19 These nanoparticles are lipid-based powder formulations from which an oil/water (o/w) emulsion can be reconstituted in vivo or in vitro.…”

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confidence: 99%

Silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation

Yang

Hwang²,

Yousaf³

et al. 2013

IJN

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Development of docetaxel-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) for enhanced chemotherapeutic effect

Cited by 144 publications

References 49 publications

The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles

The influence of bile salt on the chemotherapeutic response of docetaxel-loaded thermosensitive nanomicelles

Tumor-targeting, pH-sensitive nanoparticles for docetaxel delivery to drug-resistant cancer cells

Silymarin-loaded solid nanoparticles provide excellent hepatic protection: physicochemical characterization and in vivo evaluation

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