Assessment of nano lipid carrier loaded transdermal patch of rizatriptan benzoate.

Sayani Bhattacharyya, Lavanya Nanjareddy
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Abstract

Background: Migraine is a neurological disorder and is accompanied by different painful episodes. Hence the maintenance of a steady-state concentration of drug can be beneficial for the patients suffering with migraine. The present investigation focuses on the development of nano lipid carriers (NLCs) loaded transdermal patch of rizatriptan benzoate to sustain the effect of the drug for the enhancement of therapeutic effects.

Method: Stearic acid and peanut oil were used to make the NLCs. A central composite design was employed to observe the effect of formulation factors like solid lipid ratio, phase volume ratio, and concentration of surfactants on the formation of nanoparticles. The effects were evaluated for the responses like particle size and entrapment of the drug in the nanocarriers. The optimized formulation was subjected to compatibility, thermal, surface characteristics, and surface morphology studies. The optimized formulation was dispersed in HPMC 15CPS and PVP K30 polymer matrix and the transdermal patch was evaluated for its mechanical properties, drug release study, and skin irritation study.

Results: The experimental design was suitable to produce nanosized stable lipid carriers of the drug with high drug entrapment. The drug and excipients were found to be compatible. The thermal and surface characteristics study proved the high loading of drug in the nanoparticles. The surface morphology study showed the formation of irregular-shaped NLCs. The transdermal patch had good mechanical properties. The ex vivo study of the formulated patch showed a sustained release of the drug over 24h. No skin irritation was reported from the transdermal patch.

Conclusion: Therefore, it can be concluded that the nanoparticles loaded transdermal patch of rizatriptan benzoate can be promising in controlling the divergent phases of migraine.

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苯甲酸利扎曲普坦纳米脂质载体透皮贴片的评估。
背景:偏头痛是一种神经系统疾病,会伴随不同的疼痛发作。因此,维持药物的稳态浓度对偏头痛患者有益。本研究的重点是开发纳米脂质载体(NLCs)负载的苯甲酸利扎曲普坦透皮贴片,以维持药物的作用,提高治疗效果:方法:使用硬脂酸和花生油制作 NLCs。方法:用硬脂酸和花生油制成 NLCs,采用中心复合设计法观察固脂比、相体积比和表面活性剂浓度等配方因素对纳米颗粒形成的影响。对纳米载体的粒度和药物包埋等反应进行了评估。对优化配方进行了相容性、热学、表面特征和表面形态学研究。将优化配方分散在 HPMC 15CPS 和 PVP K30 聚合物基质中,并对透皮贴片的机械性能、药物释放研究和皮肤刺激性研究进行了评估:结果:实验设计适用于制备药物的纳米级稳定脂质载体,并具有较高的药物夹持率。药物和辅料的相容性良好。热学和表面特征研究证明纳米颗粒中药物的负载量很高。表面形态研究表明,纳米颗粒形成了不规则形状。透皮贴片具有良好的机械性能。对配制的贴片进行的体内外研究表明,药物可在 24 小时内持续释放。结论:透皮贴片对皮肤没有刺激:因此,可以得出结论,纳米粒子负载的苯甲酸利扎曲普坦透皮贴片在控制偏头痛的不同阶段方面具有良好的前景。
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