Abstract
The strategy using nonionic microemulsion as a solubilizer for hydrophobic drugs was studied and is demonstrated in this work. The aqueous phase behaviors of mixed nonionic surfactants with various oils at 37 °C are firstly constructed to give the optimal formulations of nonionic microemulsions with applications in the enhanced solubilization of the model hydrophobic drug, paclitaxel, at 37 °C. Briefly, the suitable oil phase with paclitaxel significantly dissolved is microemulsified with appropriate surfactants. Surfactants utilized include Tween 80, Cremophor EL, and polyethylene glycol (4.3) cocoyl ether, while various kinds of edible oils and fatty esters are used as the oil phase. On average, the apparent solubility of paclitaxel is increased to ca. 70–100 ppm in the prepared microemulsions at 37 °C using tributyrin or ethyl caproate as the oil phases. The sizes of the microemulsions attained are mostly from ca. 60 nm to ca. 200 nm. The cytotoxicity of the microemulsion formulations is assessed with the cellular viability of 3T3 cells. In general, the cell viability is above 55% after 24 h of cultivation in media containing these microemulsion formulations diluted to a concentration of total surfactants equal to 50 ppm and 200 ppm.
Highlights
Nowadays, the development of new drugs often encounters great difficulty during tests of drug efficacy and cytotoxicity owing to the low aqueous solubility of the newly discovered entities of drugs [1,2,3]
Selection of an appropriate oil phase was mainly based on the combined contribution from the higher solubility of paclitaxel in these oils and the possibly larger solubilization capacity of oils by surfactant solutions
Solubilizers for the model hydrophobic drug, paclitaxel, were successfully demonstrated using nonionic microemulsions at 37 ◦ C prepared from mixed surfactants and proper oil phases in this work
Summary
The development of new drugs often encounters great difficulty during tests of drug efficacy and cytotoxicity owing to the low aqueous solubility of the newly discovered entities of drugs [1,2,3]. The micellar solubilization as well as the encapsulation by microemulsion/liposome account for most mechanisms of action in surfactant-based solubilizers hydrophobic drugs. The micellar solubilization was known earlier to formulation scientists and work well in small molecular drugs, while microemulsion/liposomes are often applied to the encapsulation of larger drug molecules [1,3,4,5,6,7,9,10]. Microemulsion has recently drawn considerable interests in drug delivery systems and as a drug solubilizer, owing to advantages such as an easy preparation [11] and a good solubilization power of hydrophobic drugs [1,3,4]
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