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Crosslinked casein-based micelles as a dually responsive drug delivery system†
Polymer Chemistry ( IF 4.1 ) Pub Date : 2018-06-04 00:00:00 , DOI: 10.1039/c8py00600h Matias Luis Picchio 1, 2, 3, 4, 5 , Julio César Cuggino 6, 7, 8, 9 , Gregor Nagel 10, 11, 12, 13 , Stefanie Wedepohl 10, 11, 12, 13 , Roque Javier Minari 6, 7, 8, 9 , Cecilia Inés Alvarez Igarzabal 1, 2, 3, 4, 5 , Luis Marcelino Gugliotta 6, 7, 8, 9 , Marcelo Calderón 10, 11, 12, 13
Polymer Chemistry ( IF 4.1 ) Pub Date : 2018-06-04 00:00:00 , DOI: 10.1039/c8py00600h Matias Luis Picchio 1, 2, 3, 4, 5 , Julio César Cuggino 6, 7, 8, 9 , Gregor Nagel 10, 11, 12, 13 , Stefanie Wedepohl 10, 11, 12, 13 , Roque Javier Minari 6, 7, 8, 9 , Cecilia Inés Alvarez Igarzabal 1, 2, 3, 4, 5 , Luis Marcelino Gugliotta 6, 7, 8, 9 , Marcelo Calderón 10, 11, 12, 13
Affiliation
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New types of biodegradable nanocarriers for drug delivery were prepared using casein (CAS) micelles as particle templates and glyceraldehyde (GAL) as a crosslinking agent. We found that highly crosslinked casein micelles (CCM) maintained their structural integrity at pH 7.4 (plasma conditions) but were easily degraded in the presence of proteases at pH 5 (lysosomal conditions). Nile red (NR) was chosen as a hydrophobic model drug inspired by the natural role of casein as lipophilic nutrient nanotransporter. The cumulative release of the NR-loaded micelles showed marginal dye leakage at pH 7.4 but was significantly accelerated by protease and pH-mediated degradation of the nanocarriers in a dual-responsive fashion. The prepared nanocarriers possess many favorable features for drug delivery: excellent biocompatibility and biodegradability, high stability in physiological conditions, remarkable capacity for the encapsulation of hydrophobic drugs, minimal drug leakage under extracellular conditions, and rapid drug release in response to the endo-lysosomal levels of pH and proteases. In this regard, the prepared CCM represent a promising candidate for the delivery and triggered release of anti-cancer drugs in lysosomal environments.
中文翻译：
基于交联酪蛋白的胶束作为双重响应的药物输送系统†
使用酪蛋白（CAS）胶束作为颗粒模板和甘油醛（GAL）作为交联剂制备了新型的可生物降解的纳米药物载体。我们发现高度交联的酪蛋白胶束（CCM）在pH 7.4（血浆条件）下保持其结构完整性，但在pH 5（溶酶体条件）下存在蛋白酶时很容易降解。由于酪蛋白作为亲脂性营养素纳米转运蛋白的天然作用，尼罗河红（NR）被选作疏水性模型药物。负载NR的胶束的累积释放在pH 7.4时显示出少量的染料泄漏，但是被蛋白酶和pH介导的纳米载体降解以双重响应方式显着加速了泄漏。制备的纳米载体具有许多良好的药物传递特性：出色的生物相容性和生物降解性，在生理条件下具有很高的稳定性，疏水性药物的封装能力显着，在细胞外条件下的药物泄漏最少，并且响应于溶酶体的内在pH和蛋白酶水平而迅速释放药物。在这方面，制备的CCM代表了在溶酶体环境中抗癌药物的递送和触发释放的有希望的候选者。
更新日期：2018-06-04
中文翻译：
基于交联酪蛋白的胶束作为双重响应的药物输送系统†
使用酪蛋白（CAS）胶束作为颗粒模板和甘油醛（GAL）作为交联剂制备了新型的可生物降解的纳米药物载体。我们发现高度交联的酪蛋白胶束（CCM）在pH 7.4（血浆条件）下保持其结构完整性，但在pH 5（溶酶体条件）下存在蛋白酶时很容易降解。由于酪蛋白作为亲脂性营养素纳米转运蛋白的天然作用，尼罗河红（NR）被选作疏水性模型药物。负载NR的胶束的累积释放在pH 7.4时显示出少量的染料泄漏，但是被蛋白酶和pH介导的纳米载体降解以双重响应方式显着加速了泄漏。制备的纳米载体具有许多良好的药物传递特性：出色的生物相容性和生物降解性，在生理条件下具有很高的稳定性，疏水性药物的封装能力显着，在细胞外条件下的药物泄漏最少，并且响应于溶酶体的内在pH和蛋白酶水平而迅速释放药物。在这方面，制备的CCM代表了在溶酶体环境中抗癌药物的递送和触发释放的有希望的候选者。
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