Anastrozole (A) is an anti-cancer drug (an effective aromatase inhibitor) for the treatment of breast cancer in post-menopausal women. As it undergoes extensive first pass metabolism and has side effects like hot flashes, stomach pain, vomiting, loss of appetite, constipation, diarrhoea, stomach ache, weight gain swelling, warmth in hands or arms, blurred vision or vision changes, ulcers or blisters etc. and to overcome these side effects, an attempt has been made to develop anastrozole invasomes.
Objective: The objective of this work was to prepare and characterise invasosomal gel carrier for anastrozole, and to evaluate its optimized formulation.
Materials and methods: Invasomes were prepared by thin layer film hydration method using phospholipon 80H, fenchone (terpene) and ethanol. The optimised invasomes were incorporated in sodium carboxy methyl cellulose gel. Prepared formulations were characterized for size, size distribution, entrapment efficiency and ex-vivo drug release and cytotoxic study on MCF-7 breast cancer cell line.
Results and discussions: Optimized formulations were evaluated for particle size, drug entrapment, zeta potential and release efficiency. Morphological assessment (SEM) of the optimized formulation showed uniform size and spherical shaped vesicles. The ability of anastrozole loaded invasomes to deliver anastrozole through the skin was studied using ex-vivo studies and skin deposition studies using male Wistar rat skin. Cell line studies were performed using MCF-7 cells which showed cytotoxic effect of optimized formulation.
Conclusion: It was concluded that the developed anastrozole invasomes enhanced the transdermal flux penetration and the results obtained encouraged the use of the anastrozole invasomal gel as the formulation for the potential treatment of breast cancer in post-menopausal women.
Key words: Anastrozole, breast cancer, invasomes, full factorial design, cell line study.
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