Formulation and Evaluation of Liquid Loaded Tablets Containing Docetaxel-Self Nano Emulsifying Drug Delivery Systems
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
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