Docetaxel-loaded thermosensitive liquid suppository: optimization of rheological properties

Yeo, Woo Hyun; Ramasamy, Thiruganesh; Kim, Dong-Wuk; Cho, Hyuk Jun; Kim, Yong‐Il; Cho, Kwan Hyung; Yong, Chul Soon; Kim, Jong Oh; Choi, Han‐Gon

doi:10.1007/s12272-013-0175-6

Cited by 22 publications

(25 citation statements)

References 33 publications

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“…12 In brief, a weighed quantity of liquid suppository was placed in a glass vial which was in turn placed in an automated water bath containing a magnetic stirrer and a digital thermometer. A magnetic bar was allowed to rotate (~100 rpm) in the liquid suppository and the temperature was gradually increased from 20°C to 40°C at a rate of 1°C.…”

Section: Viscoelastic Property Gelation Temperaturementioning

confidence: 99%

“…Recently, various process and formulation related variables were optimized in order to adjust the thermogelling and mucoadhesive properties for effective rectal administration (Table 1). 12 The rate and extent of nanoparticle internalization is highly dependent on the particle size and size distribution of DCT-loaded nanomicelles. In this regard, results of dynamic light scattering analysis showed that micelles were nanosized with an average size around ~15 nm with a narrow poly dispersity index (0.2) (Figure 2A).…”

Section: Physicochemical Characterization Of Dct-loaded Nanomicellesmentioning

confidence: 99%

“…[1][2][3] However, critical drawbacks, including low aqueous solubility (5 µg/mL, highly lipophilic nature) and poor oral bioavailability (~5%, high first pass metabolism and p-glycoprotein efflux transporter/Rectal administration of the drug in a suitable dosage form remains a viable alternative to oral and intravenous (IV) administration in order to effectively counter the drawbacks and increase the therapeutic profile of DCT. 12,13 We recently reported enhanced bioavailability and anti-tumor potential of DCT by incorporation of thermosensitive and bioadhesive nanomicelles. Owing to appreciable bioadhesive interaction with rectal mucosa, the liquid suppository substantially increased the therapeutic concentration of the drug in the blood circulation and remarkable tumor regression was observed with no overt signs of drug or carrier related toxicity.…”

Section: Introductionmentioning

confidence: 99%

“…Due to its reverse gelation property, polaxamer remains in liquid state at room temperature (~25°C), while gelifying at physiological body temperature (~37°C). 12,14 We designed two delivery systems; DCT/P407/P188/Tween 80 (0.25%/11%/15%/10% by weight, respectively) and DCT/P407/P188/Tween 80/ NaTC (0.25%/11%/15%/10%/0.1% by weight, respectively) . Viscoelastic parameters were studied in terms of gel strength, gelation time, gelation temperature, and mucoadhesive force.…”

Section: Introductionmentioning

confidence: 99%

“…Previously, we have optimized the appropriate concentration of P407 and P188 such that the thermosensitive micelles formed a gel below the physiological body temperature. 12 The addition of NaTC caused a slight increase in the gelation temperature.…”

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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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Section: Viscoelastic Property Gelation Temperaturementioning

confidence: 99%

Section: Physicochemical Characterization Of Dct-loaded Nanomicellesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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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Preparation and pharmaceutical evaluation of new tacrolimus-loaded solid self-emulsifying drug delivery system

et al. 2014

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The purpose of this study was to develop a novel tacrolimus-loaded solid self-emulsifying drug delivery system (SEDDS) using Labrafac as an oil phase. The ternary phase diagram was plotted with Labrafac, Labrasol and Lauroglycol used as an oil, surfactant and co-surfactant, respectively. The liquid SEDDS formulated with Labrasol, Lauroglycol and Labrafac (70:15:15, volume ratio) furnished the smallest emulsion globule size. The solid SEDDS was obtained by spray-drying the liquid mixture containing the liquid SEDDS with 5 % tacrolimus and silicon dioxide. Furthermore, dissolution of tacrolimus from the solid SEDDS and pharmacokinetics in rats was studied compared to the commercial product. The solid SEDDS produced relatively larger emulsion globule size than that exhibited by the corresponding liquid SEDDS. However, this size variation was not significantly different. The solid SEDDS with approximately 280 nm emulsion droplet size improved the dissolution of the drug compared to drug power and the commercial product. It resulted in significantly higher plasma concentration, AUC and Cmax, and shorter Tmax values than did the commercial product (p < 0.05). The enormously enhanced oral bioavailability of tacrolimus in rats was attributed to relatively faster absorption due to accelerated dissolution of the drug from the solid SEDDS. Therefore, this novel solid SEDDS prepared with Labrafac as an oil phase is an excellent way to achieve better bioavailability of tacrolimus given via the oral route.

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Glycerosomal thermosensitive in situ gel of duloxetine HCl as a novel nanoplatform for rectal delivery: in vitro optimization and in vivo appraisal

Salem

Ali

Rabea

et al. 2022

Drug Deliv. and Transl. Res.

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Duloxetine HCl (DXH) is a reuptake inhibitor of serotonin and norepinephrine used to treat the major depressive disorder. Following its extensive hepatic metabolism, acid-labile nature, and limited aqueous solubility, DXH has poor oral bioavailability (40%). The rectal route has been suggested as another route of administration to surmount such challenges. The present study aimed to prepare DXH-loaded glycerosomal (DXH-GLYS) in situ gel for rectal administration to increase DXH permeability and improve its bioavailability. Box–Behnken design (BBD) was adopted to prepare and optimize nanoglycerosomes. The impact of Phospholipon 90G (PL90G), Tween 80 concentrations, and glycerol percentage on encapsulation efficiency, nanoglycerosomal size, % cumulative DXH released, and the cumulative DXH permeated per unit area after 24 h were studied by the design. The pharmacokinetic and pharmacodynamic behavior of optimized formulation was investigated in rats. The formulated DXH-GLYS had a vesicle size ranging between 135.9 and 430.6 nm and an entrapment efficiency between 69.11 and 98.12%. The permeation experiment revealed that the optimized DXH-GLYS in situ gel increased DXH permeation by 2.62-fold compared to DXH solution. Pharmacokinetics studies disclosed that the DXH-GLYS in situ rectal gel exhibited 2.24-times increment in DXH bioavailability relative to oral DXH solution. The pharmacodynamic study revealed that the DXH-GLYS rectal treatment significantly improved the behavioral analysis parameters and was more efficacious as an antidepressant than the oral DXH solution. Collectively, these findings demonstrate that GLYS can be considered a potentially valuable rectal nanocarrier that could boost the DXH efficacy. Graphical abstract

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Docetaxel-loaded thermosensitive liquid suppository: optimization of rheological properties

Cited by 22 publications

References 33 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

Preparation and pharmaceutical evaluation of new tacrolimus-loaded solid self-emulsifying drug delivery system

Glycerosomal thermosensitive in situ gel of duloxetine HCl as a novel nanoplatform for rectal delivery: in vitro optimization and in vivo appraisal

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