Pitta Shravan Kumar, Dudhipala Narendar, Narala Arjun, Veerabrahma Kishan
a Laboratory of Nanotechnology , University College of Pharmaceutical Sciences, Kakatiya University , Warangal , India.
Drug Dev Ind Pharm. 2018 Mar;44(3):484-492. doi: 10.1080/03639045.2017.1402918. Epub 2017 Nov 29.
The aim was to prepare an optimized zolmitriptan (ZT)-loaded transfersome formulation using Box-Behnken design for improving the bioavailability by nasal route for quick relief of migraine and further to compare with a marketed nasal spray. Here, three factors were evaluated at three levels. Independent variables include: amount of soya lecithin (X), amount of drug (X) and amount of tween 80 (X). The dependent responses were vesicle size (Y), flexibility index (Y) and regression coefficient of drug release kinetics (Y). Prepared formulations were evaluated for physical characters and an optimal system was identified. Further, in vivo pharmacokinetic study was performed in male wistar rats to compare the amount of drug in systemic circulation after intranasal administration. Optimized ZT-transfersome formulation containing 82.74 mg of lecithin (X), 98.37 mg of zolmitriptan (X) and 32.2 mg of Tween 80 (X) and had vesicle size of 93.3 nm, flexibility index of 20.25 and drug release regression coefficient of 0.992. SEM picture analysis revealed that the vesicles were spherical in morphology and had a size more than 1 µm. The formulations were found to be physically stable upon storage at room temperature up to 2 months period, as there were no significant changes noticed in size and ZP. The nasal bioavailability of optimized transfersome formulation was found to be increased by 1.72 times than that of marketed nasal spray (Zolmist). The design and development of zolmitriptan as transfersome provided improved nasal delivery over a conventional nasal spray for a better therapeutic effect.
目的是使用Box-Behnken设计制备一种优化的载佐米曲普坦（ZT）传递体剂型，以通过鼻腔途径提高生物利用度，从而快速缓解偏头痛，并进一步与市售鼻喷雾剂进行比较。在此，在三个水平上评估了三个因素。自变量包括：大豆卵磷脂的量（X1）、药物的量（X2）和吐温80的量（X3）。因变量响应为囊泡大小（Y1）、柔性指数（Y2）和药物释放动力学的回归系数（Y3）。对制备的剂型进行物理特性评估，并确定最佳体系。此外，在雄性Wistar大鼠中进行体内药代动力学研究，以比较鼻内给药后体循环中的药物量。优化的ZT传递体剂型含有82.74 mg卵磷脂（X1）、98.37 mg佐米曲普坦（X2）和32.2 mg吐温80（X3），囊泡大小为93.3 nm，柔性指数为20.25，药物释放回归系数为0.992。扫描电子显微镜图片分析显示，囊泡形态为球形，大小超过1 µm。发现这些剂型在室温下储存长达2个月期间物理稳定，因为在大小和ζ电位方面未观察到显著变化。发现优化的传递体剂型的鼻腔生物利用度比市售鼻喷雾剂（佐米曲普坦鼻喷雾剂）提高了1.72倍。将佐米曲普坦设计开发为传递体剂型，与传统鼻喷雾剂相比，提供了更好的鼻腔给药效果，以实现更好地治疗效果。
