Gandhi Arijit, Jana Sougata, Sen Kalyan Kumar
Department of Pharmaceutics, Gupta College of Technological Sciences, Ashram More, G.T. Road, Asansol-713301, West Bengal, India.
Department of Pharmaceutics, Gupta College of Technological Sciences, Ashram More, G.T. Road, Asansol-713301, West Bengal, India.
Int J Biol Macromol. 2014 Jun;67:478-82. doi: 10.1016/j.ijbiomac.2014.04.019. Epub 2014 Apr 19.
In this present study the possibility to develop Eudragit RLPO(®) based nanoparticles of acyclovir was investigated in order to increase its efficacy because acyclovir has oral bioavailability of only 10-20% thus showing erratic absorption and bioavailability behaviour. The nanoparticles were prepared by nanoprecipitation technique. Pluronic F68 was used as stabilizer. The nanoparticles were characterized by particle size, entrapment efficiency, DSC, SEM, FTIR and in-vitro drug release. It was found that as drug:polymer (Acyclovir:Eudragit RLPO(®)) ratio increased from 1:1.5 to 1:2, particle size was increased significantly and drug entrapment also increased but thereafter, further increase in drug: polymer ratio showed reduced or insignificant change in the drug entrapment efficiency. DSC results showed that in the prepared nanoaprticles, the drug was present in the amorphous phase and may have been homogeneously dispersed in the polymer matrix. In vitro drug release study of formulations showed release in 24h in the range 71.62±1.72 to 93.25±1.02%. The release was found to follow Higuchi model with non-Fickian diffusion mechanism for all batches. These preliminary results indicate that acyclovir loaded Eudragit RLPO(®) nanoparticles could be effective in sustaining drug release for a prolonged period.
在本研究中，为提高阿昔洛韦的疗效，对基于Eudragit RLPO（®）开发阿昔洛韦纳米颗粒的可能性进行了研究，因为阿昔洛韦的口服生物利用度仅为10%-20%，表现出吸收和生物利用度不稳定的行为。纳米颗粒采用纳米沉淀技术制备。普朗尼克F68用作稳定剂。通过粒径、包封率、差示扫描量热法（DSC）、扫描电子显微镜（SEM）、傅里叶变换红外光谱（FTIR）和体外药物释放对纳米颗粒进行了表征。结果发现，随着药物与聚合物（阿昔洛韦：Eudragit RLPO（®））的比例从1:1.5增加到1:2，粒径显著增加，药物包封率也增加，但此后，药物与聚合物比例的进一步增加显示药物包封效率降低或变化不显著。DSC结果表明，在制备的纳米颗粒中，药物以非晶态存在，可能已均匀分散在聚合物基质中。制剂的体外药物释放研究表明，在24小时内的释放范围为71.62±1.72%至93.25±1.02%。发现所有批次的释放均符合Higuchi模型，具有非菲克扩散机制。这些初步结果表明，负载阿昔洛韦的Eudragit RLPO（®）纳米颗粒可能有效地延长药物释放时间。
