Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Future University in Egypt, New Cairo, Cairo, 11835, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, 11562, Egypt.
Int J Nanomedicine. 2022 Jun 25;17:2753-2776. doi: 10.2147/IJN.S370192. eCollection 2022.
The low entrapment efficiency of the hydrophilic drugs such as brimonidine tartrate (BRT) in liposomes represents a challenge that requires interventions. Gelatinized core liposomes (GCLs) were fabricated to increase the drug entrapment, corneal penetration, and physical stability of the investigated molecule.
GCLs encapsulating BRT were prepared and optimized utilizing D-optimal design (DOD). The effect of plasticizer incorporation on the physicochemical characteristics and on the in vivo performance was studied. The optimized formulations were investigated for pH, rheological properties, morphological characteristics, in vitro release profiles, biological performance, safety profile. The effects of storage and gamma sterilization were also investigated.
The results revealed the great success of the prepared formulations to achieve high entrapment efficiency reaching 98% after a maturation period of 10 days. The addition of glycerol as plasticizer significantly minimized the particle size and shortened the maturation period to 7 days. The selected formulations were stable for 3 months after gamma sterilization. The formulations showed significant lowering of intra-ocular pressure (IOP) in glaucomatous rabbits with sustainment of the pharmacological effect for 24 hours compared to drug solution.
Enhanced in vitro and in vivo profiles of brimonidine tartrate loaded gelatinized-core-liposomes were obtained.
亲水药物如酒石酸溴莫尼定（BRT）在脂质体中的包封效率低，这是一个需要干预的挑战。本研究制备了明胶化核心脂质体（GCL）以提高所研究分子的药物包封率、角膜穿透率和物理稳定性。
利用 D 最优设计（DOD）制备和优化了包封 BRT 的 GCL。研究了增塑剂的加入对理化性质和体内性能的影响。对优化的配方进行了 pH 值、流变特性、形态特征、体外释放曲线、生物学性能、安全性特征的研究。还研究了储存和γ射线灭菌的影响。
结果表明，所制备的制剂非常成功，可实现高达 98%的包封效率，在 10 天的成熟期后达到。添加甘油作为增塑剂可显著减小粒径并将成熟时间缩短至 7 天。选择的配方在γ射线灭菌后 3 个月内稳定。与药物溶液相比，载有酒石酸溴莫尼定的明胶化核心脂质体在青光眼兔中表现出显著降低眼压（IOP）的作用，其药效可持续 24 小时。
获得了增强的酒石酸溴莫尼定载明胶化核心脂质体的体外和体内特性。
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