Alternative drug formulations of docetaxel: a review

Engels, Frederike K.; Mathôt, Ron A. A.; Verweij, Jaap

doi:10.1097/cad.0b013e3280113338

Cited by 190 publications

(130 citation statements)

References 59 publications

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“…In its commercial formulation (Taxotere ® , Sanofi-Aventix, Bridgewater, NJ, USA), nonionic surfactant Tween 80 (polysorbate 80) and 13% ethanol in saline have been used to dissolve DCT, due to its poor solubility in water; 19 however, this formulation is associated with unpredictable hypersensitivity reactions and other side effects. 20 Thus, many new systems -including micelles, emulsions, and conjugates with other polymers -have been developed to deliver DCT to tumor sites with minimal adverse reactions. [21][22][23] Heparin is a biocompatible, biodegradable, water-soluble natural polysaccharide coupled with various biological activities, including anticoagulation, anti-inflammatory, and antiangiogenesis effects.…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel

Kim¹,

Termsarasab²,

Cho³

et al. 2014

IJN

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Low-molecular-weight heparin (LMWH)–stearylamine (SA) conjugates (LHSA)-based self-assembled nanoparticles were prepared for intravenous delivery of docetaxel (DCT). 1-Ethyl-3-(3-dimethylaminopropyl) carbodiimide and N -hydroxysuccinimide were used as coupling agents for synthesis of LHSA conjugates. The physicochemical properties, in vitro antitumor efficacy, in vitro cellular uptake efficiency, in vivo antitumor efficacy, and in vivo pharmacokinetics of LHSA nanoparticles were investigated. The LHSA nanoparticles exhibited a spherical shape with a mean diameter of 140–180 nm and a negative surface charge. According to in vitro release and in vivo pharmacokinetic test results, the docetaxel-loaded LHSA5 (LMWH:SA =1:5) nanoparticles exhibited sustained drug release profiles. The blank LHSA nanoparticles demonstrated only an insignificant cytotoxicity in MCF-7 and MDAMB 231 human breast cancer cells; additionally, higher cellular uptake of coumarin 6 (C6) in MCF-7 and MDAMB 231 cells was observed in the LHSA5 nanoparticles group than that in the C6 solution group. The in vivo tumor growth inhibition efficacy of docetaxel-loaded LHSA5 nanoparticles was also significantly higher than the Taxotere ® -treated group in the MDAMB 231 tumor-xenografted mouse model. These results indicated that the LHSA5-based nanoparticles could be a promising anticancer drug delivery system.

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Section: Introductionmentioning

confidence: 99%

Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel

Kim¹,

Termsarasab²,

Cho³

et al. 2014

IJN

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“…The H22 hepatic cancer cells (2 × 10 6 cells/ mouse) were subcutaneously transplanted into the right axilla of mice. When the tumor volume reached a size of about 150 mm 3 , the mice were injected with physiological saline, DIR-loaded PLGA, and PLA-TPGS nanoparticles at a dose of DIR 0.1/kg body weight via the tail vein. The animals were anesthetized by isoflurane inhalation.…”

Section: In Vivo Biodistributionmentioning

confidence: 99%

“…1,2 However, its poor water solubility limits its clinical use. 3 The currently available dosage formulation is as an injection with Tween 80 and anhydrous ethanol as the cosolvents, which have been proved to cause some severe side effects. 1,4 It is essential to develop a drug-delivery system (DDS) that will reduce the side effects and improve its therapeutic efficiency.…”

Section: Introductionmentioning

confidence: 99%

“…Many nanosized DTX formulations, such as liposomes, prodrugs, polymeric nanoparticles, and micelles, have been investigated and shown improved therapeutic efficiency. 3,[6][7][8][9][10][11][12] Among these, polymeric nanoparticles have been found to offer better stability, high drug-loading efficiency (DLE), small particle size, and preferable in vivo pharmacokinetics/pharmacodynamics. 13,14 Poly(lactic acid) (PLA) and poly(lactide-co-glycolide) (PLGA) have been widely used in DDS because they are approved as good biodegradability and biocompatibility agents by the US Food and Drug Administration (FDA).…”

Section: Introductionmentioning

confidence: 99%

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Antitumor activity of docetaxel-loaded polymeric nanoparticles fabricated by Shirasu porous glass membrane-emulsification technique

Yu¹,

Tan²,

Zhao³

et al. 2013

IJN

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Docetaxel (DTX) has excellent efficiency against a wide spectrum of cancers. However, the current clinical formulation has limited its usage, as it causes some severe side effects. Various polymeric nanoparticles have thus been developed as alternative formulations of DTX, but they have been mostly fabricated on a laboratory scale. Previously, we synthesized a novel copolymer, poly(lactide)-d-α-tocopheryl polyethylene glycol 1000 succinate (PLA-TPGS), and found that it exhibited great potential in drug delivery with improved properties. In this study, we applied the Shirasu porous glass (SPG) membrane-emulsification technique to prepare the DTX-loaded PLA-TPGS nanoparticles on a pilot scale. The effect of several formulation variables on the DTX-loaded nanoparticle properties, including particle size, zeta potential, and drug-encapsulation efficiency, were investigated based on surfactant type and concentration in the aqueous phase, organic/aqueous phase volumetric ratio, membrane-pore size, transmembrane cycles, and operation pressure. The DTX-loaded nanoparticles were obtained with sizes of 306.8 ± 5.5 nm and 334.1 ± 2.7 nm (mean value ± standard deviation), and drugencapsulation efficiency of 81.8% ± 4.5% and 64.5% ± 2.7% for PLA-TPGS and poly(lacticco-glycolic acid) (PLGA) nanoparticles, respectively. In vivo pharmacokinetic study exhibited a significant advantage of PLA-TPGS nanoparticles over PLGA nanoparticles and Taxotere. Drug-loaded PLA-TPGS nanoparticles exhibited 1.78-, 6.34-and 3.35-fold higher values for area under the curve, half-life, and mean residence time, respectively, compared with those of PLGA nanoparticles, and 2.23-, 13.2-, 8.51-fold higher than those of Taxotere, respectively. In vivo real-time distribution of nanoparticles was measured on tumor-bearing mice by near-infrared fluorescence imaging, which demonstrated that the PLA-TPGS nanoparticles achieved much higher concentration and longer retention in tumors than PLGA nanoparticles after intravenous injection. This is consistent with the pharmacokinetic behavior of the nanoparticles. The tumorinhibitory effect of DTX-loaded nanoparticles was observed in vivo in an H22 tumor-bearing mice model via intravenous administration. This indicated that PLA-TPGS nanoparticles are a feasible drug-delivery formulation with a pilot fabrication technique and have superior pharmacokinetic and anticancer effects compared to the commercially available Taxotere.

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“…However, due to the high content of Tween 80, acute hypersensitivity reactions have been found in the majority of patients treated in the clinical trials, sometimes even leading to death. 14) To avoid and/or alleviate these side effects, some new preparations including liposomes 15) and nanoparticles 16) have been developed. Another attractive approach to overcome the drawbacks of the above intravenous dosage is to develop oral formulations that have advantages in reducing the potential toxicity and improving compli-ance.…”

mentioning

confidence: 99%

Development of a Solid Supersaturatable Self-Emulsifying Drug Delivery System of Docetaxel with Improved Dissolution and Bioavailability

Chen

Zheng

et al. 2011

Biological & Pharmaceutical Bulletin

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Self-emulsifying drug delivery systems (SEDDS) are defined as isotropic mixtures of oils, surfactants, and co-solvents. The systems can form fine oil in water (o/w) emulsions (SEDDS) with a droplet size between 100 and 1000 nm or in microemulsions (SMEDDS) with a droplet size of less than 100 nm when meeting with aqueous media. SEDDS/ SMEDDSs may offer a new strategy for enhancing the oral bioavailability of poorly water soluble and lipophilic drugs. [1][2][3][4] However, recent studies suggest that there are some shortcomings in the stability and safety of SEDDS/ SMEDDSs. First of all, SEDDS/SMEDDSs are normally in liquid or semi-solid form and are encapsulated in soft gelatin capsules with high manufacturing costs. 5) Some of the alcohol or other cosolvents in the SEDDSs possibly move into the shells of the capsule, which results in the precipitation of the drug.1,6) Therefore, a new SEDDS called the solid selfemulsifying drug delivery system (S-SEDDS) was prepared by incorporating a liquid self-emulsifying formulation into a solid dosage form.5-8) S-SEDDSs have the advantages of higher stability, longer storage time, lower irritation of gastrointestinal tract and lower production costs compared with conventional SEDDS. Secondly, plenty of surfactants and cosolvents are added into the formulations of SEDDS/SMEDDSs to prevent precipitation of the drug when diluted by gastrointestinal (GI) fluids. However, more surfactants may cause gastrointestinal side effects 9,10) ; therefore, a new thermodynamically stable formulation called the supersaturatable self-emulsifying drug delivery system (sSEDDS) was designed to contain a reduced amount of surfactant and watersoluble polymers as a supersaturated promoter to prevent precipitation of the drug by generating and maintaining a supersaturated state in vivo. In comparison with conventional SEDDSs, sSEDDS formulations can result in enhanced stability and lower side effects. 10)This study combines the advantages of S-SEDDSs with those of sSEDDSs by incorporating a supersaturatable liquid self-emulsifying formulation into a solid dosage form. This can possibly overcome the disadvantages of liquid SEDDSs and the high surfactant levels in conventional SEDDS formulations described above. Although increasing studies have focused on the area of S-SEDDSs or sSEDDSs, related reports are limited. There has been no previous work that was carried out to investigate the combination of SEDDS and S-SEDDS technology with sSEDDSs. Docetaxel (DTX) is an antineoplastic agent belonging to the second generation of the taxoid family. It was identified in 1986 as an alternative to paclitaxel. It has become one of the most important chemotherapeutic agents and is widely used against ovarian carcinoma, advanced breast cancer, lung cancer, and head/neck cancer.11-13) Docetaxel is practically insoluble in water and is often dissolved in polysorbate 80 (Tween 80). However, due to the high content of Tween 80, acute hypersensitivity reactions have been found in the majority of patients treated in t...

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Alternative drug formulations of docetaxel: a review

Cited by 190 publications

References 59 publications

Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel

Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel

Antitumor activity of docetaxel-loaded polymeric nanoparticles fabricated by Shirasu porous glass membrane-emulsification technique

Development of a Solid Supersaturatable Self-Emulsifying Drug Delivery System of Docetaxel with Improved Dissolution and Bioavailability

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