新型蒙脱土壳聚糖眼部给药载体的制备与表征

Dongzhi Hou, Ruyi Gui, Sheng Hu, Yi Huang, Zu-yong Feng, Q. Ping
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引用次数: 47

摘要

本研究的目的是研究蒙脱土作为长期眼部应用的载药纳米颗粒制备的持续载体的潜力。采用三聚磷酸钠离子凝胶法制备了壳聚糖纳米颗粒。盐酸倍他洛尔(BH)作为模型药物。采用TG、FT-IR、TEM、DLS和XRD对壳聚糖-蒙脱土/TPP药物包封纳米颗粒(CS-MMT/TPP NPs)进行了表征。TEM图像显示,颗粒呈球形,表面粗糙。纳米颗粒的粒径范围为338 ~ 585 nm, zeta电位值为24 ~ 36 mV,包封效率为12.27% ~ 50.92%。载bh纳米颗粒在人工泪液(pH 7.4)中有体外缓释作用。FT-IR、TG和XRD结果表明,CSMMT/ TPP NPs包被药物。在黏附研究中,发现载药CSMMT/ TPP NPs与粘蛋白相互作用,可延长角膜前停留时间,从而促进有效的持续释放。经改良德来兹试验确定优化后的配方无刺激性、耐受性好。因此,所开发的装载bh的CS-MMT/TPP NPs是一种很有前途的眼睛药物递送载体。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and Characterization of Novel Drug-Inserted-Montmorillonite Chitosan Carriers for Ocular Drug Delivery
The objective of the study was to investigate the potential of montmorillonite as a sustained carrier in the preparation of drug-loaded nanoparticles for prolonged ocular application. Nanoparticles were prepared by ionic gelation of chitosan with sodium tripolyphosphate (TPP). Betaxolol hydrochloride (BH) was applied as a model drug. TG, FT-IR, TEM, DLS and XRD have been employed in the characterization of drug-encapsulated chitosan-montmorillonite/TPP nanoparticles (CS-MMT/TPP NPs). TEM images showed that the particles were spherical in shape and had a rough surface. The size range of the nanoparticles was between 338 and 585 nm with positive zeta potential values from 24 mV to 36 mV and encapsulation efficiency values ranging from 12.27% to 50.92%. In vitro sustained drug release was observed with the BH-loaded nanoparticles in artificial tears (pH 7.4). The results of FT-IR, TG and XRD showed that the drug was coated with CSMMT/ TPP NPs. In the mucoadhesion studies, an interaction was found between drug-loaded CSMMT/ TPP NPs and mucin, which could enhance precorneal residence time and hence facilitate an effective sustained release. The optimized formulation was determined to be non-irritant and tolerable by modified Draize test. Therefore, the BH-loading CS-MMT/TPP NPs developed are a promising carrier for controlled drug delivery to the eye.
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