Preparation and evaluation of biphenyl dimethyl dicarboxylate microemulsions for oral delivery

Kim, Chong‐Kook; Cho, Yeon-Ju; Gao, Zhong-Gao

doi:10.1016/s0168-3659(00)00343-6

Cited by 108 publications

(45 citation statements)

References 12 publications

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“…Current research is focused on developing nanoparticle formulations of widely used chemotherapeutics or newly discovered cancer agents, which are few in number. 3 Traditional self-assembled polyoxyethylene nonionic surfactants (PNS), including polysorbate 80, polyoxyl 35 castor oil, poloxamer, and poly(ethylene glycol), are a class of nanocarrier systems with potential application in tablets, 4 emulsions, 5 and especially in the preparation of injections. 6 PNS can dramatically improve the efficiency of anticancer drugs by enhancing their solubility in aqueous solution.…”

Section: Introductionmentioning

confidence: 99%

Novel designed polyoxyethylene nonionic surfactant with improved safety and efficiency for anticancer drug delivery

Sun

et al. 2014

IJN

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In order to limit the adverse reactions caused by polysorbate 80 in Taxotere ® , a widely used formulation of docetaxel, a safe and effective nanocarrier for this drug has been developed based on micelles formed by a new class of well-defined polyoxyethylene sorbitol oleate (PSO) with sorbitol as the matrix in aqueous solution. The physicochemical properties of the amphiphilic surfactant and the resulting micelles can be easily fine-tuned by the homogeneous sorbitol matrix and pure oleic acid. Composition, critical micelle concentration, and entrapment efficiency were investigated by ultraviolet visible spectroscopy, matrix-assisted laser desorption/ionization time-of-flight mass spectrometry, fluorospectrophotometry, and high-performance liquid chromatography. In vitro and in vivo evaluation revealed that PSO had exceptionally low hemolysis and histamine release rates compared with commercial polysorbate 80. Moreover, the tumor targeting delivery of PSO was investigated by in vivo imaging in S180 tumor-bearing mice. The results suggest that this novel delivery system, PSO, provides an acceptable alternative to polysorbate 80 for delivery of docetaxel. Further, due to the hypoallergenic nature of PSO, the mechanism of pseudoallergy caused by the polyoxyethylene nonionic surfactant was investigated. Based on in vitro cell analysis, it was assumed that the initial contact of polyoxyethylene nonionic surfactant with mast cells provoked pseudoallergy via polyamine receptor-mediated endocytosis.

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Section: Introductionmentioning

confidence: 99%

Novel designed polyoxyethylene nonionic surfactant with improved safety and efficiency for anticancer drug delivery

Sun

et al. 2014

IJN

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“…Therefore, SMEDDS is a potential strategy for enhancing the oral bioavailability of poorly water-soluble drugs. 18 However, SMEDDS are liquid formulations, which have several disadvantages, including low stability and portability during the manufacturing process and limited dosage forms, such as soft gelatin capsule. To overcome these problems, solid SMEDDSs have been investigated as alternatives.…”

Section: Introductionmentioning

confidence: 99%

Optimized formulation of solid self-microemulsifying sirolimus delivery systems

Cho

Kim

et al. 2013

IJN

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Background:The aim of this study was to develop an optimized solid self-microemulsifying drug delivery system (SMEDDS) formulation for sirolimus to enhance its solubility, stability, and bioavailability. Methods: Excipients used for enhancing the solubility and stability of sirolimus were screened. A phase-separation test, visual observation for emulsifying efficiency, and droplet size analysis were performed. Ternary phase diagrams were constructed to optimize the liquid SMEDDS formulation. The selected liquid SMEDDS formulations were prepared into solid form. The dissolution profiles and pharmacokinetic profiles in rats were analyzed. Results: In the results of the oil and cosolvent screening studies, Capryol™ Propylene glycol monocapry late (PGMC) and glycofurol exhibited the highest solubility of all oils and cosolvents, respectively. In the surfactant screening test, D-α-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) was determined to be the most effective stabilizer of sirolimus in pH 1.2 simulated gastric fluids. The optimal formulation determined by the construction of ternary phase diagrams was the T32 (Capryol™ PGMC:glycofurol:vitamin E TPGS = 30:30:40 weight ratio) formulation with a mean droplet size of 108.2 ± 11.4 nm. The solid SMEDDS formulations were prepared with Sucroester 15 and mannitol. The droplet size of the reconstituted solid SMEDDS showed no significant difference compared with the liquid SMEDDS. In the dissolution study, the release amounts of sirolimus from the SMEDDS formulation were significantly higher than the raw sirolimus powder. In addition, the solid SMEDDS formulation was in a more stable state than liquid SMEDDS in pH 1.2 simulated gastric fluids. The results of the pharmacokinetic study indicate that the SMEDDS formulation shows significantly greater bioavailability than the raw sirolimus powder or commercial product (Rapamune ® oral solution). Conclusion:The results of this study suggest the potential use of a solid SMEDDS formulation for the delivery of poorly water-soluble drugs, such as sirolimus, through oral administration.

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“…After oral administration, it rapidly disperses in stomach forming small droplets (<5 μm), which promotes wide distribution of the drug throughout the GI tract. In the past decade, we have developed lipophilic drugs microemulsion [6], hydrophobic drug emulsion [12], and thermal sensitive microemulsion [13] for enhancing water insoluble drugs bioavailability. In this chapter, we discuss on the enhancing bioavailability of the poorly water soluble drugs after oral administration by using microemulsion system.…”

Section: Introductionmentioning

confidence: 99%

Preparation and evaluation of biphenyl dimethyl dicarboxylate microemulsions for oral delivery

Cited by 108 publications

References 12 publications

Novel designed polyoxyethylene nonionic surfactant with improved safety and efficiency for anticancer drug delivery

Novel designed polyoxyethylene nonionic surfactant with improved safety and efficiency for anticancer drug delivery

Optimized formulation of solid self-microemulsifying sirolimus delivery systems

Thermal Reversible Microemulsion for Oral Delivery of Poorly Water-Soluble Drugs

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