Tamoxifen Citrate Containing Topical Nanoemulgel Prepared by Ultrasonication Technique: Formulation Design and In Vitro Evaluation

Abstract

The present study aims to design and develop a nanoemulgel formulation of Tamoxifen citrate (TAM), a water-insoluble, potent anticancer drug, using the spontaneous emulsification method to improve topical delivery, achieve high accumulation at the tumour site, and spare the healthy tissues. The oil-based selection was related to the TAM solubility, while the surfactant and co-surfactant were chosen based on the droplets’ thermodynamic stability and size. Afterwards, a pseudo-ternary phase diagram was built for the most promising formulation using two oils, olive and sesame, with a varied mix of Tween 40 as the surfactant and Trascutol HP as the co-surfactant (Smix), by the optimisation of experiments. The nanoemulsion (NE) formulations that were prepared were found to have an average droplet size of 41.77 ± 1.23 nm and 188.37 ± 3.53 nm, with suitable thermodynamic stability and physicochemical properties. Both olive and sesame oils are natural food additives due to their associated antioxidant effects; therefore, they showed no toxicity profile on breast cell lines (MCF-7, ATCC number HTB-22). The TAM-NE preparations revealed a prolonged and doublings superior cumulative percentage of in vitro release of TAM compared to TAM plain gel suspension over 24 h. The release data suggested that the Higuchi model was the best fitting kinetical model for the developed formulations of NE1, NE9, and NE18. The extended release of the drug as well as an acceptable amount of the drug permeated TAM via nanogel preparations suggested that nanoemulgel (NEG) is suitable for the topical delivery of TAM in breast cancer management. Thus, this work suggests that a nanogel of TAM can improve anticancer properties and reduce systemic adverse effects compared to a suspension preparation of TAM when applied in the treatment of breast cancer.

Efficacy of topical Omega-3 emulgel in preventing radiation-induced oral mucositis: A randomized clinical trial

“…Using direct emulsification, fish oil emulsion was prepared. In brief, the aqueous phase that contains Tween 80 (El Gomhouria Co. Alexandria, Egypt) was added to the oily phase which contains Fish oil and Span 80 (sigma Aldrich, UK)) (22). The ratio of water: oil was 6:4 and the ratio of the used surfactant was 7:3 for Tween 80 and Span 80 respectively.…”

Omega-3 nanoemulgel in prevention of radiation-induced oral mucositis and its associated effect on microbiome: a randomized clinical trial

“…Fish oil nano emulsion was developed using direct emulsification method. Briefly, the aqueous phase containing Tween 80 (El Gomhouria Co. Alexandria, Egypt) was added to the oily phase (Fish oil and Span 80 (sigma Aldrich, UK)) [51,52]. The ratio of water: oil was 6:4 and the ratio of the used surfactant was 7:3 for Tween 80 and Span 80 respectively.…”

“…4. Stability Test: The stability of the prepared (NE) systems was assessed by applying centrifugation stress; 1 mL of the system was added to 100 mL distilled water and centrifuged for 30 min (5000× rpm), and phase separation was inspected visually using ultra cooling centrifuge (Sigma laborzentrifugen GmbH, Osterode, Germany) [51].…”