抗逆转录病毒药物的开发,表征和评价-二腺苷负载血清白蛋白纳米载体用于抗逆转录病毒治疗

Josephine Leno Jenita Joseph , Vijaya Chockalingam , Wilson Barnabas
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引用次数: 3

摘要

AimDidanosine是一种核苷类逆转录酶抑制剂,用于治疗有或无获得性免疫缺陷综合征患者的HIV感染。本研究的目的是通过脱溶技术制备负载二腺苷的牛血清白蛋白纳米颗粒,并包被1%聚山梨酸80,以改善抗逆转录病毒治疗。方法采用脱溶法制备牛血清白蛋白纳米粒,并与8% v/v的戊二醛交联。乙醇和甘露醇分别作为脱溶剂和冷冻保护剂。在三个月的时间里,对配制的纳米颗粒进行了表征、评估和稳定性研究。对最佳配方进行生物分布研究(D1)。结果纳米粒径平均小于270 nm, PDI为0.2,zeta电位范围为- 23.0 ~ - 36.6。包封率为66 ~ 85.71%,载药量为9.48 ~ 28.34 %。累积释药百分数在60 ~ 80%范围内,释放动力学表明药物释放受菲克氏扩散控制。为期3个月的稳定性研究证实了BSA纳米颗粒的稳定性。生物分布研究表明,1%聚山梨酯80包被纳米颗粒可提高巨噬细胞器官中的药物水平。结论该方法操作简单,可制备稳定的球形纳米颗粒,缓释效果好。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development, characterization and evaluation of antiretroviral drug – Didanosine loaded serum albumin nanocarriers for an antiretroviral therapy

Aim

Didanosine, a nucleoside reverse transcriptase inhibitor, is used to treat HIV infection in patients with or without acquired immunodeficiency syndrome. The objective of this study is to prepare didanosine loaded bovine serum albumin nanoparticles by desolvation technique and coated with 1% polysorbate 80 to improve antiretroviral therapy.

Method

Bovine serum albumin nanoparticles containing didanosine were prepared by desolvation technique and cross linked with 8% v/v glutaraldehyde solution. Ethanol and mannitol were used as a desolvating agent and cryoprotectant respectively. The formulated nanoparticles were characterized, evaluated and were subjected to stability studies over a period of three months. Biodistribution studies were investigated for the best formulation (D1).

Results

Nanoparticle size was averaged below 270 nm with 0.2 PDI and zeta potential was in the range of −23.0 to −36.6. Encapsulation efficiency ranges from 66 to 85.71% and % drug loading ranges from 9.48 to 28.34. Cumulative percent drug release was in range of 60–80% and release kinetics suggested that drug release was Fickian diffusion controlled. The stability studies over period of 3 months confirmed the stability of BSA nanoparticles. Biodistribution studies demonstrated that the drug level in macrophage organs can be enhanced by coating of nanoparticles with 1% polysorbate 80.

Conclusion

The method adopted is simple and able to prepare stable, spherical shaped nanoparticles which exhibit slow and sustained release.

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