Preparation and Optimization of Fexofenadine HCl Solid lipid Nanoparticles

Ashwini Gunjote, Heramb Shahane, Rani Ghosalkar, Kedar Bavaskar, Ashish Jain
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Abstract

Solid lipid nanoparticles (SLNs) are introduced as an efficient carrier method for correcting dynamic medicine and water-soluble medication. Fexofenadine HCl is a long-acting selective histamine (H1) receptor antagonist with anti-inflammatory properties of the second generation. Allergic rhinitis, angioedema, and chronic urticaria are treated with fexofenadine HCl. Solid lipid nanoparticles were prepared by hot homogenization method using a solid lipid of and different polymers. A solid lipid nanoparticle created by drug and polymer poloxamer 188 in ratio showed highest entrapment efficiency as well as drug release of the medication from the solid lipid nanoparticle formulation. The prepared nanoparticles were used to formulate the nanogel using Carbopol 934. The nano-drug delivery system developed by the hot homogenization method has demonstrated their suitability for a topical route for the treatment of skin allergy. Thus, the studies revealed that the developed system has a great appeal for the convenient treatment of dermatological allergy that may overcome in improving the limitations of the existing drug delivery system. Fexofenadine HCl is a white colored powder. It is practically insoluble in water and soluble in methanol. The melting point was found to be 194.1-195.2. The FTIR spectra of Fexofenadine HCl and the mixture of drug and excipients used in the formulation of nanoparticles reveal that there was no significant interaction between the drug and polymer and other excipients used in the formulation. The optimized batches (F2) showed highest entrapment efficiency. It was observed that as there is increase in concentration of surfactant increases the entrapment efficiency. The optimized solid lipid nanoparticle formulation showed maximum drug release within 6 hr. This showed that the increase in the concentration of surfactant there was increase in drug release from the SLN.
非非那定盐酸固体脂质纳米颗粒的制备与优化
固体脂质纳米颗粒(SLNs)是一种有效的动态药物和水溶性药物校正载体。非索非那定HCl是一种长效选择性组胺(H1)受体拮抗剂,具有第二代抗炎特性。非索非那定盐酸治疗过敏性鼻炎、血管性水肿和慢性荨麻疹。以固体脂质和不同的聚合物为原料,采用热均质法制备固体脂质纳米颗粒。由药物和聚合物poloxam188按比例制成的固体脂质纳米颗粒显示出最高的包封效率以及固体脂质纳米颗粒制剂中药物的药物释放。将制备的纳米颗粒用Carbopol 934配制成纳米凝胶。通过热均质方法开发的纳米药物递送系统已经证明它们适合局部途径治疗皮肤过敏。因此,研究表明,所开发的系统在克服现有给药系统的局限性方面,对皮肤过敏的便捷治疗具有很大的吸引力。盐酸非索非那定是白色粉末。它几乎不溶于水,可溶于甲醇。熔点为194.1-195.2。对盐酸非索非那定及纳米颗粒制剂中所用的药物和辅料混合物的FTIR光谱分析表明,药物与聚合物及制剂中所用的辅料之间没有明显的相互作用。优化后的批(F2)包封效率最高。结果表明,随着表面活性剂浓度的增加,捕集效率也随之提高。优化后的固体脂质纳米颗粒在6小时内释放最大。结果表明,随着表面活性剂浓度的增加,SLN的药物释放量增加。
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