马来酸氟伏沙明负载脂质纳米颗粒的制备及性能评价

A. P., Mancy S.P., M. K, S. V. Kulkarni, Jagadeesh R
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引用次数: 1

摘要

近年来,固体脂质纳米颗粒(SLN's)因其生物可降解性、生物利用度和将多种药物输送到靶向作用部位的能力而受到了研究人员的广泛关注。本研究的目的是开发和评价负载马来酸氟伏沙明的脂质纳米颗粒。采用三硬脂、甘醇、橄榄油、椰子油、芝麻油等不同脂质组合,采用热熔均质-超声法制备马来酸氟伏沙明脂质纳米颗粒。通过FTIR和DSC验证了相容性研究。对LN的粒径、PDI、zeta电位、包封效率和体外药物释放进行了评价。用固体脂质制备的马来酸氟伏沙明LN的粒径范围为98.58 ~ 152.43 nm。各配方的PDI在0.239 ~ 0.456之间,zeta电位在- 6.52 ~ -18.6 mV之间。捕集率为64.56% ~ 84.23%。不同LN对马来酸氟伏沙明的累积释放率为46.14% ~ 81.48%。固体脂质与液体脂质联合制备的马来酸氟伏沙明LN的粒径范围为63.22 ~ 263.8 nm。PDI范围为0.229 ~ 0.514,Zeta电位范围为- 5.01 ~ -9.30 mV。捕集率为71.02 ~ 90.51%。不同LN对马来酸氟伏沙明的累积释放百分比根据药物脂质比和所用脂质类型的不同,从63.71到85.41%不等。释放动力学研究表明,释放为一级释放,扩散控制,Korsmeyer-Peppa模型的n值表明释放机制为反常(非菲克)扩散型。
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Formulation and Evaluation of Fluvoxamine Maleate Loaded Lipid Nanoparticle
Recently solid lipid nanoparticles (SLN's) have been received much attention by the researchers owing to its biodegradability, bioavailability and the ability to deliver wide range of drugs to the targeted site of action. The purpose of the present study is to develop and evaluate the fluvoxamine maleate loaded lipid nanoparticles. The fluvoxamine maleate lipid nanoparticles (LN’s) were prepared by the hot melt homogenization followed by the sonication by using different combination of lipids like tristearin, compritol, olive oil, coconut oil, sesame oil. Compatibility study was confirmed by FTIR and DSC. The LN’s were evaluated for particle size, PDI, zeta potential, entrapment efficiency and in-vitro drug release. For the Fluvoxamine maleate LN’s prepared using the solid lipids, the particle size ranged from 98.58 to 152.43 nm. PDI of all formulations were good within the range of 0.239 to 0.456 with zeta potential from - 6.52 to -18.6 mV. Entrapment efficiency observed was in the range of 64.56 to 84.23 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 46.14 to 81.48%. For the formulations prepared using the combination of solid lipids and liquid lipids, Fluvoxamine maleate LN’s the particle size ranged from 63.22 to 263.8 nm. With good PDI range from 0.229 to 0.514 Zeta potential of all formulation is from - 5.01 to -9.30 mV. Entrapment efficiency observed was in the range of 71.02 to 90.51 %. The cumulative percentage release of fluvoxamine maleate from different LN’s varied from 63.71 to 85.41% depending upon the drug lipid ratio, the type of lipid used. The release kinetic studies showed that the release was first order, diffusion controlled, and the ‘n’ values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Anomalous (non-Fickian) diffusion type.
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