Perspectives of nanoemulsion assisted oral delivery of docetaxel for improved chemotherapy of cancer

Abstract

Context: Nanoemulsions (NE) are one of the robust delivery tools for drugs due to their higher stability and efficacy. Objectives: The purpose of present investigation is to develop stable, effective and safe NE of docetaxel (DTX). Methods: Soybean oil, lecithin, Pluronic F68, PEG 4000 and ethanol were employed as excipients and NEs were prepared by hot homogenization followed by ultra-sonication. NEs were optimized and investigated for different in vitro and in vivo parameters viz. droplet size, poly dispersity index, charge; zeta potential, drug content and in vitro drug release, in vitro cytotoxicity, in vitro cell uptake and acute toxicity. Transmission electron microscopy was performed to study morphology and structure of NEs. Stability studies of the optimized formulation were performed. Results: Droplet size, poly dispersity index, zeta potential, drug content and in vitro drug release were found to be 233.23 ± 4.3 nm, 0.24 ± 0.010, À43.66 ± 1.9 mV, 96.76 ± 1.5%, 96.25 ± 2.1%, respectively. NE F11 exhibited higher cell uptake (2.83 times than control) and strong cytotoxic activity against MCF-7 cancer cells (IC 50 ; 13.55 ± 0.21 mg/mL at 72 h) whereas no toxicity or necrosis was observed with liver and kidney tissues of mice at a dose of 20 mg/kg. Transmission electron microscopy ensured formation of poly-dispersed and spherical droplets in nanometer range. NE F11 (values indicated above) was selected as the optimized formulation based on the aforesaid parameters. Conclusion: Conclusively, stable, effective and safe NE was developed which might be used as an alternative DTX therapy.

Development of docetaxel nanocapsules for improvingin vitrocytotoxicity and cellular uptake in MCF-7 cells

“…The extent of NCs uptake in vitro was examined by flow cytometry (BD Biosciences, FACS Aria, Germany). The data are presented as the mean fluorescence obtained from a population of 10 000 cells 27,28 .…”

“…The limit of detection (LOD) and quantification (LOQ) were found to be 36 and 156 ng/ml, respectively. Following formula was used to calculate the entrapment efficiency 16,[25][26][27][28] .…”

Design and evaluation of oral nanoemulsion drug delivery system of mebudipine

“…In recent years, nanoemulsion systems have received increasing attention as an appropriate carrier system for insoluble active compounds to increase their bioavailability and modify drug release characteristics (Han et al, 2009;Kotta et al, 2013;Sharma et al, 2014;Verma et al, 2014). For instance, improved oral bioavailability of amlodipine (Chhabra et al, 2011) and felodipine (Veerareddy et al, 2012) nanoemulsions in comparison with the conventional preparations has been reported.…”

Influence of Polysorbate 60 on Formulation Properties and Bioavailability of Morin-Loaded Nanoemulsions with and without Low-Saponification-Degree Polyvinyl Alcohol

“…Nanoemulsion systems have received increasing attention as appropriate carriers for insoluble active compounds to increase bioavailability and modify drug release characteristics. [13][14][15] Improvements in the solubility of drugs into nanoemulsion components such as the oil phase and surfactants represent an effective strategy for drugs for which low water solubility dissolution is the rate limiting step in absorption and bioavailability. However, non-ionic surfactants are inhibitors of intestinal P-gp.…”