We report here on ion-exchange polymeric nanoparticles from a linear copolymer of maleic anhydride methyl vinyl ether esterified with 30% octadecanol. The side chains for the polymer structure were optimized through metadynamics simulations, which revealed the use of octadecanol esters generates ideal free energy surfaces for drug encapsulation and release. Nanoparticles were synthesized using a solvent evaporation-precipitation method by mixing the polymer solution in acetone into water; upon acetone evaporation, a nanodispersion with an average particle size of ∼150 nm was obtained. Gentamicin sulfate, possessing five amino groups, was spontaneously entrapped in the nanocarrier by ionic interactions. Encapsulation efficiency increases significantly with the increase in pH and ionic strength. In vivo results demonstrate high gentamicin (GM) content in the enteric chamber (AUC 8207 ± 1334 (μg min)/mL) compared to 3% GM solution (AUC 2024 ± 438 (μg min)/mL). The formulation was also able to significantly extend the release of gentamicin when applied to rabbit cornea. These anionic nanoparticles can be used for extended-release of other cationic drugs.

中文翻译：

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用于眼科药物递送的离子交换纳米粒子

我们在这里报道了由马来酸酐甲基乙烯基醚与30％十八醇酯化的线性共聚物的离子交换聚合物纳米颗粒。通过元动力学模拟对聚合物结构的侧链进行了优化，结果表明十八醇酯的使用可为药物封装和释放产生理想的自由能表面。使用溶剂蒸发沉淀法，通过将聚合物在丙酮中的溶液混合到水中来合成纳米颗粒。丙酮蒸发后，获得平均粒径约为150 nm的纳米分散体。具有五个氨基的硫酸庆大霉素通过离子相互作用自发截留在纳米载体中。随着pH和离子强度的增加，封装效率显着提高。体内结果表明与3％GM溶液（AUC 2024±438（μgmin）/ mL）相比，肠腔中的庆大霉素（GM）含量较高（AUC 8207±1334（μgmin）/ mL）。当应用于兔子角膜时，该制剂还能够显着延长庆大霉素的释放。这些阴离子纳米颗粒可用于其他阳离子药物的缓释。