Abstract
Objective: The main objective of this study was to prepare and evaluate the nanocrystal formulation of docetaxel.
 Methods: Docetaxel nanocrystals were formulated to improve the water solubility. Docetaxel nanocrystals were prepared by nanoprecipitation method using Tween 80, egg lecithin, and povidone C-12 as stabilizers and poly(lactic-co-glycolic acid) (PLGA) as polymer in acceptable limits. A total of 16 formulations were prepared by changing stabilizer and polymer ratios. The prepared nanocrystals were characterized by particle size, zeta potential, crystalline structure, surface morphology, assay, saturation solubility, and in vitro drug release.
 Results: Based on particle size, polydispersity index, and zeta potential data, four formulations were optimized. The formulation containing Tween 80 as stabilizer has shown lowest particle size and better drug release than the formulations containing egg lecithin and povidone C-12 as stabilizers. The formulation containing Tween 80 and PLGA has shown still lower sized particles than the Tween 80 alone and exhibited prolonged sustained drug release. The release kinetics of formulations containing Tween 80 and PLGA followed zero-order release kinetics and formulations containing egg lecithin and povidone C-12 followed Higuchi diffusion (non-Fickian).
 Conclusion: From the study, we concluded that as the type and concentration of stabilizer changed the size and shape of the crystals were also changed and the formulations showed sustained drug release with non-Fickian diffusion.
Highlights
Cancer is the main cause of death worldwide
RTM injection concentrate, due to its poor water solubility docetaxel, is given in a vehicle containing high concentration of Tween 80 and the injection needs to be diluted with 13% ethanol in water for injection
Standard curve of docetaxel in UV spectrophotometer The UV absorbance of DTX standard solution is in the range of 10–40 μg/ml of drug in isopropyl alcohol (IPA) and buffer pH 7.4 (50:50) showed linearity at λ max 231 nm
Summary
Cancer is the main cause of death worldwide. Nanotechnology has a great approach to have a revolutionary impact on cancer diagnosis and therapy [1]. Docetaxel is used to treat a number of cancers such as breast, ovarian, lung, head, and neck cancer. It shows more affinity (1.9-fold) for microtubules when compared with paclitaxel [5,6,7,8]. Despite these advantages, clinical use of docetaxel is still limited due to its low water solubility. Clinical use of docetaxel is still limited due to its low water solubility The presence of high concentrations of Tween 80 and ethanol causes severe adverse effects like several hypersensitivity reactions and it shows incompatibility with common PVC intravenous administration sets [9,10]
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