Docetaxel microemulsion for enhanced oral bioavailability: Preparation and in vitro and in vivo evaluation

Yin, Yongmei; Cui, Fude; Mu, Chaofeng; Choi, Min‐Koo; Kim, Jung Sun; Chung, Suk‐Jae; Shim, Chang‐Koo; Kim, Dae‐Duk

doi:10.1016/j.jconrel.2009.08.015

Cited by 270 publications

(148 citation statements)

References 29 publications

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“…21 In brief, aliquots of DTX-loaded micelles were introduced into a dialysis bag (MWCO = 3500 Da, Greenbird Inc, Shanghai, China), the sealed end of which was immersed fully into 50 mL of a release medium at 37°C; this medium was stirred at 100 rpm for 24 hours. At fixed time intervals, 0.5-mL aliquots were withdrawn and replaced with an equal volume of fresh medium.…”

Section: In Vitro Dtx Releasementioning

confidence: 99%

Pluronic P105/F127 mixed micelles for the delivery of docetaxel against Taxol-resistant non-small cell lung cancer: optimization and in vitro, in vivo evaluation

Chen¹,

Sha²,

Jiang³

et al. 2013

IJN

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Abstract:The aim of this work was to establish a novel polymeric mixed micelle composed of Pluronic P105 and F127 copolymers loaded with the poorly soluble antitumor drug docetaxel (DTX) against Taxol-resistant non-small cell lung cancer. A central composite design was utilized to optimize the preparation process, helping to improve drug solubilization efficiency and micelle stability. Prepared by a thin-film hydration method, the average size of the optimized mixed micelle was 23 nm, with a 92.40% encapsulation ratio and a 1.81% drug-loading efficiency. The optimized formulation showed high storage stability in lyophilized form, with 95.7% of the drug content remaining after 6 months' storage at 4°C. The in vitro cytotoxicity assay showed that the IC50 values for Taxotere ® and mixed micelles were similar for A549, while on A549/Taxol cell lines, DTX-loaded P105/F127 mixed micelles showed a superior hypersensitizing effect; their IC50 value (0.059 µg/mL) was greatly reduced compared to those of Taxotere injections (0.593 µg/mL). The in vivo pharmacokinetic study showed that the mixed-micelle formulation achieved a 1.85-fold longer mean residence time in circulation and a 3.82-fold larger area under the plasma concentration-time curve than Taxotere. In addition, therapeutic improvement of mixed micelles in vivo against A549/Taxol was obtained. The tumor inhibition rate of the micelles was 69.05%, versus 34.43% for Taxotere (P , 0.01). Therefore, it could be concluded from the results that DTX-loaded P105/F127 mixed micelles might serve as a potential antitumor drug delivery system to overcome multidrug resistance in lung cancer.

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Section: In Vitro Dtx Releasementioning

confidence: 99%

Pluronic P105/F127 mixed micelles for the delivery of docetaxel against Taxol-resistant non-small cell lung cancer: optimization and in vitro, in vivo evaluation

Chen¹,

Sha²,

Jiang³

et al. 2013

IJN

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“…The polydispersity values of all formulations were very low which indicates uniformity of droplets within the formulation. The Zeta potential of the formulation was also measured in order to determine the interaction between colloidal particles, where large positive or negative values suggesting high inclination of emulsion repulsion and hence, stability [17].…”

Section: Discussionmentioning

confidence: 99%

Topical nano-delivery of 5-fluorouracil: Preparation and characterization of water-in-oil nanoemulsion

Siddalingam¹,

Chidambaram²

2016

Trop. J. Pharm Res

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“…The condition used for the in vitro lipolysis study was modified from Yin et al [21]. The tested formulations containing MSE (250 mg) were dispersed in 9 ml of the digestive buffer (50 mmol trizma ® maleate, 150 mmol NaCl, 5 mmol CaCl2·2H2O, pH 7.5) containing 5 mmol NaTc and 1.25 mmol L-α-phosphatidylcholine in order to simulate the fasted intestinal conditions.…”

Section: In Vitro Intestinal Lipolysis Studymentioning

confidence: 99%

Enhancement of Stability, Release and in Vitro Digestibility of Mulberry Stem Extract Using Microemulsions

Soonthornsit

Hemstapat

Pitaksutheepong

et al. 2017

Int J Pharm Pharm Sci

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Objective: This study was aimed to develop oral microemulsions and to evaluate their ability to enhance stability, release and intestinal digestion of mulberry stem extract (MSE). Methods:The pseudoternary phase diagrams were constructed using caprylic/capric triglyceride (oil), PEG-8 caprylic/capric glycerides (S), polyglyceryl-3 diisostearate (CoS) and an aqueous phase. The effects of S/CoS (Km) ratio and a cosolvent, i.e. polyethene glycol 400 or propylene glycol (PG), were investigated. The optimized formulations were selected and incorporated with MSE. Then, they were then subjected to stability, release and lipolysis studies. The control solution consisted of 50% PG and 50% water. Results:The formation and characteristics of the microemulsions were influenced by Km and cosolvents. The two optimized formulations (F3 and F4) consisted of 10% oil, 70% S/CoS mixture and 20% aqueous phase were chosen. The Km ratios of F3 and F4 were 4:1 and 3:1. The aqueous phase of F3 and F4 was water and water mixed with PG, respectively. These formulations could improve the stability of MSE better than the control solution. The accumulated release of MSE from F3, F4 and the control solution reached 100% while that of unformulated crude extract reached only 70% after 6 h. The lipolysis study showed that MSE incorporated in both F3 and F4 was digested more than double the percentage compared to that of MSE incorporated in the control solution.Conclusion: MSE was successfully developed in microemulsions. They are shown to be promising vehicles for oral delivery of MSE. Further animal trials are suggested.

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Docetaxel microemulsion for enhanced oral bioavailability: Preparation and in vitro and in vivo evaluation

Cited by 270 publications

References 29 publications

Pluronic P105/F127 mixed micelles for the delivery of docetaxel against Taxol-resistant non-small cell lung cancer: optimization and in vitro, in vivo evaluation

Pluronic P105/F127 mixed micelles for the delivery of docetaxel against Taxol-resistant non-small cell lung cancer: optimization and in vitro, in vivo evaluation

Topical nano-delivery of 5-fluorouracil: Preparation and characterization of water-in-oil nanoemulsion

Enhancement of Stability, Release and in Vitro Digestibility of Mulberry Stem Extract Using Microemulsions

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