a Chongqing Research Center for Pharmaceutical Engineering , Chongqing Medical University , Chongqing , China.
b Nursing College, Chongqing Medical University , Chongqing , China.
Drug Deliv. 2018 Nov;25(1):1426-1437. doi: 10.1080/10717544.2018.1474970.
Most antitumor ingredients found in nature have poor solubility. These ingredients are expected to have much better absorption and higher bioavailability than synthetic antitumor agents. Woody oil emulsive nanosystems carrying poorly soluble natural alkaloids were fabricated (evodiamine (EA) carried by fructus bruceae oil-based emulsive nanosystems, or EFEN). Fructus bruceae oil has two excipient-like properties (oil phase and stabilizer) that contribute to the formulation and one drug-like property (antitumor effects) that synergizes with the antitumor effect of EA. The properties of EFEN were compared with free EA, a blank nanoemulsion, an EA-loaded emulsive nanosystem, and a fructus bruceae oil-loaded emulsive nanosystem. For the first time, this suggests that increases in the sensitivity of lung cancer cells to poorly soluble natural alkaloids can be achieved by delivering drugs using woody oil-based emulsive nanosystems. In this study, woody oil-based emulsive nanosystems efficiently deliver poorly soluble natural alkaloids.
天然存在的大多数抗肿瘤成分溶解度都较差。这些成分有望比合成抗肿瘤剂具有更好的吸收和更高的生物利用度。本研究制备了携带难溶性天然生物碱的 Woody 油乳状纳米系统(由鸦胆子油基乳状纳米系统携带的吴茱萸碱(EA),或 EFEN)。鸦胆子油具有两种赋形剂特性(油相和稳定剂),有助于制剂,并具有一种类似药物的特性(抗肿瘤作用),与 EA 的抗肿瘤作用协同。将 EFEN 的性质与游离 EA、空白纳米乳、载 EA 的乳状纳米系统和载鸦胆子油的乳状纳米系统进行了比较。首次表明,通过使用 Woody 油基乳状纳米系统递送药物,可以提高肺癌细胞对难溶性天然生物碱的敏感性。在本研究中, Woody 油基乳状纳米系统有效地传递了难溶性天然生物碱。