This work aims to transfer the fast dissolution performances of drug nanosuspensions into the solid state via a carrier particle-mediated isolation method and explores the factors affecting the maximum achievable drug loading of the prepared nanocomposite microparticles. The solid composites of fast dissolving dalcetrapib (DCP) nanoparticles on larger montmorillonite (MMT) carrier microparticles have been prepared by an antisolvent precipitation method. The very high dissolution rate of the DCP nanoparticles is combined with the simple solid–liquid separation and drying of the MMT composite microparticles. The fast dissolution rate of DCP from the solid-state nanocomposite microparticles was maintained up to a drug loading of 20.9%, and the formulation was stable for a minimum of 10 weeks in the solid state. Surface functionalization of the MMT particles was not needed for a high and uniform attachment of nanoparticles. Addition of soluble surfactant and polymeric additives, generally used for stabilization of nanosuspensions, was not required and even decreased the DCP nanoparticle attachment and thus limited drug loading.

中文翻译：

---

Dalcetrapib–蒙脱土纳米复合微粒的载药量和溶解特性

这项工作旨在通过载体颗粒介导的分离方法将药物纳米混悬剂的快速溶解性能转化为固态，并探讨影响制备的纳米复合微粒可达到的最大载药量的因素。通过反溶剂沉淀法制备了在较大的蒙脱土（MMT）载体微粒上快速溶解的达西替尼（DCP）纳米颗粒的固体复合物。DCP纳米颗粒的极高溶解速率与MMT复合微粒的简单固液分离和干燥相结合。DCP从固态纳米复合微粒的快速溶出速率保持到20.9％的载药量，并且该制剂在固态下至少可稳定10周。MMT颗粒的表面功能化对于纳米颗粒的高而均匀的附着是不需要的。不需要添加通常用于稳定纳米悬浮液的可溶性表面活性剂和聚合物添加剂，甚至可以减少DCP纳米颗粒的附着，从而限制了药物的负载。