Self-nanoemulsifying drug delivery systems of tamoxifen citrate: design and optimization.
Tamoxifen citrate is an antiestrogen for peroral breast cancer treatment. The drug delivery encounters problems of poor water solubility and vulnerability to enzymatic degradation in both intestine and liver. In the current study, tamoxifen citrate self-nanoemulsifying drug delivery systems (SNEDDS) were prepared in an attempt to circumvent such obstacles. Preliminary screening was carried out to select proper ingredient combinations. All surfactants screened were recognized for their bioactive aspects. Ternary phase diagrams were then constructed and an optimum system was designated. Three tamoxifen SNEDDS were then compared for optimization. The systems were assessed for robustness to dilution, globule size, cloud point, surface morphology and drug release. An optimum system composed of tamoxifen citrate (1.6%), Maisine 35-1 (16.4%), Caproyl 90 (32.8%), Cremophor RH40 (32.8%) and propylene glycol (16.4%) was selected. The system was robust to different dilution volumes and types. It possessed a mean globule size of 150 nm and a cloud point of 80 degrees C. Transmission electron microscopy demonstrated spherical particle morphology. The drug release from the selected formulation was significantly higher than other SNEDDS and drug suspension, as well. Realizing drug incorporation into an optimized nano-sized SNEDD system that encompasses a bioactive surfactant, our results proposed that the prepared system could be promising to improve oral efficacy of the tamoxifen citrate.
Elnaggar
Yosra S R
YS
Department of Pharmaceutics, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt. yosra pharm@yahoo.com.
El-Massik
Magda A
MA
Abdallah
Ossama Y
OY
D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems / Q000379:methods*; D004355:Drug Stability; D004655:Emulsions / Q000138:chemical synthesis / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry; D036103:Nanotechnology / Q000379:methods*; D010316:Particle Size; D044367:Phase Transition; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry; D013629:Tamoxifen / Q000737:chemistry / Q000493:pharmacokinetics
D004655:Emulsions; D005079:Excipients; D013501:Surface-Active Agents; D013629:Tamoxifen