增溶表面活性剂以及抗病毒、抗菌和抗真菌药物负载量对其从乙烯-醋酸乙烯酯共聚物中释放速率的影响。

Effects of solubilizing surfactants and loading of antiviral, antimicrobial, and antifungal drugs on their release rates from ethylene vinyl acetate copolymer.

作者信息

Tallury Padmavathy, Randall Marcus K, Thaw Khin L, Preisser John S, Kalachandra Sid

机构信息

Center for Oral and Systemic Diseases, Department of Periodontology, School of Dentistry, University of North Carolina, Chapel Hill, NC 27599-7455, USA.

出版信息

Dent Mater. 2007 Aug;23(8):977-82. doi: 10.1016/j.dental.2006.08.005. Epub 2006 Oct 17.

DOI:10.1016/j.dental.2006.08.005

PMID:17049593

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3881552/

Abstract

OBJECTIVES

This study investigates the effects of surfactants and drug loading on the drug release rate from ethylene vinyl acetate (EVA) copolymer. The release rate of nystatin from EVA was studied with addition of non-ionic surfactants Tween 60 and Cremophor RH 40. In addition, the effect of increasing drug load on the release rates of nystatin, chlorhexidine diacetate and acyclovir is also presented.

METHOD

Polymer casting solutions were prepared by stirring EVA copolymer and nystatin (2.5wt.%) in dichloromethane. Nystatin and surfactants were added in ratios of (1:1), (1:2) and (1:3). Drug loading was studied with 2.5, 5.0, 7.5, and 10.0wt.% proportions of nystatin, chlorhexidine diacetate and acyclovir incorporated into a separate polymer. Three drug loaded polymer square films (3cmx3cmx0.08cm) were cut from dry films to follow the kinetics of drug release at 37 degrees C. Ten milliliters of either distilled water or PBS was used as the extracting medium that was replaced daily. PBS was used for nystatin release with addition of surfactants and water was used for the study on drug loading and surfactant release. The rate of drug release was measured by UV-spectrophotometer. The amount of surfactant released was determined by HPLC.

RESULTS

The release of nystatin was low in PBS and its release rate increased with the addition of surfactants. Also, increasing surfactant concentrations resulted in increased drug release rates. The release rates of chlorhexidine diacetate (p<0.0001), acyclovir (p<0.0003) and nystatin (p<0.0017) linearly increased with increasing drug loads. The amount of surfactants released was above the CMC.

SIGNIFICANCE

This study demonstrates that the three therapeutic agents show a sustained rate of drug release from EVA copolymer over extended periods of time. Nystatin release in PBS is low owing to its poor solubility. Its release rate is enhanced by addition of surfactants and increasing the drug load as well.

摘要

目的

本研究调查表面活性剂和药物负载量对药物从乙烯-醋酸乙烯酯（EVA）共聚物中释放速率的影响。研究了添加非离子表面活性剂吐温60和聚氧乙烯蓖麻油RH 40时制霉菌素从EVA中的释放速率。此外，还展示了增加药物负载量对制霉菌素、醋酸氯己定和阿昔洛韦释放速率的影响。

方法

通过在二氯甲烷中搅拌EVA共聚物和制霉菌素（2.5wt.%）制备聚合物浇铸溶液。制霉菌素和表面活性剂按（1:1）、（1:2）和（1:3）的比例添加。研究了将2.5、5.0、7.5和10.0wt.%的制霉菌素、醋酸氯己定和阿昔洛韦掺入单独聚合物中的药物负载情况。从干膜上切下三片载药聚合物方形薄膜（3cm×3cm×0.08cm），以跟踪37℃下的药物释放动力学。使用10毫升蒸馏水或磷酸盐缓冲液（PBS）作为提取介质，每天更换。添加表面活性剂时，使用PBS研究制霉菌素的释放，使用水研究药物负载和表面活性剂释放。通过紫外分光光度计测量药物释放速率。通过高效液相色谱法测定释放的表面活性剂的量。