Candesartan Cilexetil (CC) is a prodrug of candesartan and an angiotensin II receptor antagonist. It is used as a drug for different diseases like myocardial infarction, hypertension, and heart failure. The applicability of CC is impeded due to its poor water solubility, low permeability, and low bioavailability. This study is targeted to improve the efficacy and bioavailability of CC by its delivery through MeO‐PEO_5K‐PCL micelles. The effect of length of hydrophobic block (PCL) on size of the micelles, drug encapsulation efficiency, and drug release behavior is evaluated. MeO‐PEO_5K‐PCL based micelles were prepared by solvent evaporation method. The size of PMs was determined by dynamic light scattering, morphology by atomic force microscopy, and critical micelles concentration by fluorescence method. Encapsulation efficiency and drug release behaviors of MeO‐PEO_5K‐PCL based PMs were evaluated by UV‐visible spectroscopy and dispersion method, respectively. The size of micelles increased and drug release rate decreased with increase in the length of PCL block. Maximum encapsulation efficiency of 96.42 % for CC is achieved with ABCs having equal PEO and PCL block lengths. A comparison of antibacterial activity of CC in pure form and encapsulated in PMs against MRSA is conducted. The MIC₅₀ for CC loaded PMs has decreased to more than half in comparison to pure drug. AFM based morphological analysis also confirmed the decrease in MIC₅₀ by delivery through PMs.

中文翻译：

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通过聚合胶束递送增强非抗菌药物坎地沙坦Cilexetil的抗菌活性

Candesartan Cilexetil（CC）是坎地沙坦的前药和血管紧张素II受体拮抗剂。它被用作治疗各种疾病的药物，例如心肌梗塞，高血压和心力衰竭。由于CC的水溶性差，低渗透性和低生物利用度，因此阻碍了CC的适用性。这项研究旨在通过通过MeO-PEO _5K - PCL胶束递送CC来提高CC的功效和生物利用度。评估了疏水嵌段（PCL）的长度对胶束大小，药物封装效率和药物释放行为的影响。MeO-PEO _5K‐基于PCL的胶束通过溶剂蒸发法制备。通过动态光散射，通过原子力显微镜检查的形态以及通过荧光法测定的临界胶束浓度来确定颗粒物的大小。基于MeO-PEO _5K - PCL的PMs的包封效率和药物释放行为分别通过紫外可见光谱和分散法进行评估。随着PCL嵌段长度的增加，胶束的大小增加，药物释放速率降低。使用具有相同PEO和PCL块长度的ABC，可实现CC的96.42％的最大封装效率。进行了纯形式的CC和封装在PM中的CC对MRSA的抗菌活性的比较。MIC ₅₀与纯药物相比，CC装载的PMs减少了一半以上。基于AFM的形态学分析还证实了通过PM递送使MIC ₅₀降低。