Abstract
Purpose: To prepare and characterize tablets loaded with self-nanoemulsifying drug delivery system (SNEDDS) containing docetaxel (DTL).Method: SNEDDS of docetaxel were prepared using various oils, surfactants, co-surfactant and solvents to improve the dissolution rate and bioavailability of the poorly water-soluble chemotherapeutic agent. The SNEDDS components were preliminarily screened for the solubility of the drug in various vehicles, miscibility of excipients, rate of emulsification and ternary phase diagrams. The tablets were prepared by direct compression process with a porous carrier, magnesium alumino-metasilicate, and subsequently loaded with SNEDDS by a simple absorption method. The tablets were then characterized for physical parameters, including tablet hardness, weight variation, disintegration, drug content and invitro drug release.Results: Cremophor-EL, polysorbate-80 and dehydrated alcohol mixture in the ratio 85:10:5 yielded docetaxel SNEDDS with droplet size of 12.16 nm and polydispersity (PDI) of 0.039. Tablets with high porosity suitable for loading with SNEDDS and containg the super-disintegrants, crosscarmellose sodium and sodium starch glycolate, in a concentration of 3, 4 and 5 %, achieved complete dissolution of docetaxel from the tablets. In vitro release of docetaxel from SNEDDS and the tablets was similar (p < 0.05).Conclusion: SNEDDS of docetaxel is a promising approach to achieving a solid dosage form of the liquid-loaded drug delivery systems for enhancing the solubility and dissolution rate of the drug, and hence also its bioavailability.Keywords: Docetaxel, Drug carrier, SNEDDS, Self-nanoemulsifying, Solubility, Drug release, Anicancer, Surfactant, Co-surfactant
Highlights
High levels of insolubility in the formulation of anticancer injections pose serious problems and challenges to formulation scientists and physicians in terms of emulsifying and suspending injectable formulations
Docetaxel injection is available as self-nanoemulsifying drug delivery system (SNEDDS) formulation with polysorbate-80, which accommodates effective therapeutic amount in smaller amount of surfactant mix
The concentration of docetaxel was quantified by high performance liquid chromatography (HPLC)
Summary
High levels of insolubility in the formulation of anticancer injections pose serious problems and challenges to formulation scientists and physicians in terms of emulsifying and suspending injectable formulations. Docetaxel injection is available as SNEDDS formulation with polysorbate-80, which accommodates effective therapeutic amount in smaller amount of surfactant mix. Formulation development in these areas using SNEDDS is feasible to have pharmaceutical equivalent dosage form. Some formulators have focused on solid formulation of lipid systems and in particular formulation of liquids and semi-solid selfemulsifying drug delivery systems (SEDDS) [3]. Lipid-based formulation systems have become increasingly important in the formulation of lipophilic drug substances as they can facilitate the dispersion of a drug in the gastrointestinal tract resulting in enhanced oral bioavailability [4]. Self-nanoemulsifying mixture is an advanced form of nanoemulsion drug delivery systems, because water is not used and so the drug leaching from the nanosized oily droplets to the aqueous medium of the formulation during storage is minimized [6]
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