a Department of Pharmacy, College of Chemical Engineering , Qingdao University of Science and Technology , Qingdao , China.
b Qingdao Women and Children's Hospital , Pharmacy Intravenous Admixture Services , Qingdao , China.
Drug Deliv. 2019 Dec;26(1):481-489. doi: 10.1080/10717544.2019.1600077.
Ginsenosides Rb1 (Rb1) could form micelles in aqueous solutions. Self-assembled Rb1 micelles could potentially be utilized as ocular drug delivery system, and it was postulated that the encapsulation of a medicine within Rb1 micelles might strengthen the drug's therapeutic action and reduce side effects.
Diclofenac-loaded Rb1 micelles (Rb1-Dic micelles) were formulated, optimized, and then further evaluated for in vitro cytotoxicity/in vivo ocular irritation, in vivo corneal permeation, and in vivo anti-inflammatory efficacy.
Rb1 self-assembled into micelles with ultra-small particle size (<8 nm) in a homogeneous distribution state (polydispersity index [PDI] < 0.3). Diclofenac was highly encapsulated into the micelles according to the weight ratios of Rb1 to diclofenac. The ophthalmic solution of Rb1-Dic micelle was simple to prepare. Rb1 had good cellular tolerance, and it also improved the cellular tolerance of the encapsulated diclofenac. Rb1-Dic micelles also showed non-irritants to the rabbit eyes. The use of Rb1 micelles significantly improved the in vivo corneal permeation as well as the anti-inflammatory efficacy of diclofenac when compared to commercial diclofenac eye drops.
Rb1 micelle formulations have great potential as a novel ocular drug delivery system to improve the bioavailability of drugs such as diclofenac.
人参皂苷 Rb1（Rb1）可在水溶液中形成胶束。自组装的 Rb1 胶束可潜在地用作眼部药物传递系统，据推测，将药物封装在 Rb1 胶束内可能会增强药物的治疗作用并减少副作用。
制备并优化了载双氯芬酸钠的 Rb1 胶束（Rb1-Dic 胶束），然后进一步评估其体外细胞毒性/体内眼刺激性、体内角膜透过性和体内抗炎功效。
Rb1 自组装成具有超小粒径（<8nm）的胶束，呈均匀分布状态（多分散指数[PDI] <0.3）。根据 Rb1 与双氯芬酸钠的重量比，双氯芬酸钠高度包封在胶束中。Rb1-Dic 胶束的滴眼剂易于制备。Rb1 具有良好的细胞耐受性，并且还提高了包封的双氯芬酸钠的细胞耐受性。Rb1 胶束对兔眼也无刺激性。与市售双氯芬酸钠滴眼液相比，Rb1 胶束显著提高了双氯芬酸钠的体内角膜透过性和抗炎功效。
Rb1 胶束制剂具有作为改善双氯芬酸钠等药物生物利用度的新型眼部药物传递系统的巨大潜力。
