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首页> 外文期刊>Journal of Pharmacy and Pharmaceutical Sciences >Design and Pharmaceutical Evaluation of a Nano-Enabled Crosslinked Multipolymeric Scaffold for Prolonged Intracranial Release of Zidovudine
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Design and Pharmaceutical Evaluation of a Nano-Enabled Crosslinked Multipolymeric Scaffold for Prolonged Intracranial Release of Zidovudine

机译：齐多夫定延长颅内释放的纳米功能交联的多聚支架的设计和药物评价。

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Purpose. Nanomedicine explores and allows for the development of drug delivery devices with superior drug uptake, controlled release and fewer drug side-effects. This study explored the use of nanosystems to formulate an implantable drug delivery device capable of sustained zidovudine release over a prolonged period. Methods. Pectin and alginate nanoparticles were prepared by applying a salting out and controlled gelification approach, respectively. The nanoparticles were characterized by attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and dynamic light scattering (DLS) and were further evaluated for zidovudine (AZT) entrapment efficiency. Multipolymeric scaffolds were prepared by crosslinking carboxymethyl cellulose, polyethylene oxide and epsilon caprolactone for entrapment of zidovudine-loaded alginate nanoparticles to impart enhanced controlled release of zidovudine over the time period. Swelling and textural analysis were conducted on the scaffolds. Prepared scaffolds were treated with hydrochloric acid (HCl) to reduce the swelling of matrix in the hydrated environment thereby further controlling the drug release. Drug release studies in phosphate buffered saline (pH 7.4, 37°C) were undertaken on both zidovudine-loaded nanoparticles and native scaffolds containing alginate nanoparticles. Results. A higher AZT entrapment efficiency was observed in alginate nanoparticles. Biphasic release was observed with both nanoparticle formulations, exhibiting an initial burst release of drug within hours of exposure to PBS, followed by a constant release rate of AZT over the remaining 30 days of nanoparticle analysis. Exposure of the scaffolds to HCl served to reduce the drug release rate from the entrapped alginate nanoparticles and extended the AZT release up to 30 days. Conclusions. The crosslinked multipolymeric scaffold loaded with alginate nanoparticles and treated with 1% HCl showed the potential for prolonged delivery of zidovudine over a period of 30 days and therefore may be a potential candidate for use as an implantable device in treating Aids Dementia Complex. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.
机译：目的。纳米医学探索并允许开发具有优异的药物吸收，控释和更少的药物副作用的药物递送装置。这项研究探索了使用纳米系统来配制能够长时间持续释放齐多夫定的植入式药物输送装置。方法。果胶和藻酸盐纳米颗粒分别通过应用盐析法和受控胶凝法制备。通过衰减全反射-傅立叶变换红外光谱（ATR-FTIR），扫描电子显微镜（SEM），透射电子显微镜（TEM）和动态光散射（DLS）表征纳米颗粒，并进一步评估齐多夫定（AZT）的包封效率。通过交联羧甲基纤维素，聚环氧乙烷和ε-己内酯来制备载有齐多夫定的藻酸盐纳米颗粒，从而在一定时间内增强齐多夫定的受控释放，从而制备了多聚支架。在支架上进行溶胀和质地分析。将制备的支架用盐酸（HCl）处理以减少基质在水合环境中的溶胀，从而进一步控制药物的释放。在载有齐多夫定的纳米颗粒和含有藻酸盐纳米颗粒的天然支架上进行了磷酸盐缓冲液（pH 7.4，37°C）中的药物释放研究。结果。在藻酸盐纳米颗粒中观察到较高的AZT截留效率。在两种纳米颗粒制剂中均观察到双相释放，在暴露于PBS数小时内显示出药物的爆发性释放，随后在剩余的30天纳米颗粒分析中，AZT的释放速率恒定。将支架暴露于HCl可以降低药物从截留的藻酸盐纳米颗粒中的释放速率，并将AZT释放延长至30天。结论。负载有藻酸盐纳米颗粒并用1％HCl处理的交联的多聚支架显示出齐多夫定在30天内延长递送的潜力，因此可能是潜在的候选药物，可用于治疗艾滋病痴呆症。本文对发布后审查开放。已注册的读者（请参阅“针对读者”）可以通过在问题目录页面上单击摘要来发表评论。

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