Liposomal gels for vaginal drug delivery
Liposomal gels for vaginal drug delivery
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DOI：
10.1016/s0378-5173(01)00637-8
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发表时间：
2001-05-21
影响因子：
5.8
通讯作者：
Schubert, R
中科院分区：
文献类型：
--
作者：
Pavelic, Z;Skalko-Basnet, N;Schubert, R
本研究的目的是开发一种脂质体药物载体系统，能够为阴道局部治疗提供适当的药物的持续和控制释放。为了优化脂质体制备的大小和包封率，通过五种不同的方法制备含有钙黄绿素的脂质体。测试了两种最佳脂质体制剂（前体脂质体和多元醇稀释脂质体）在模拟人阴道条件的培养基（缓冲液，pH 4.5）中的体外稳定性。为了更接近脂质体的体内应用并实现其稳定性的进一步改善，将脂质体掺入适合于阴道自我施用的媒介物中。选择聚丙烯酸酯凝胶作为脂质体制剂的载体。由于它们的亲水性和生物粘附性，可以达到与生理条件相对应的适当pH值以及所需的粘度。掺入这些凝胶（Carbopol 974 P NF或Carbopol 980 NF）中的脂质体的体外释放研究证实了它们作为阴道给药中新型药物载体系统的适用性。无论使用何种凝胶，即使在pH 4.5的缓冲液中孵育脂质体凝胶24小时后，仍保留了80%以上的原始截留物质。(C)2001 Elsevier Science B.V.保留所有权利。
The aim of our study was to develop a liposomal drug carrier system, able to provide sustained and controlled release of appropriate drug for local vaginal therapy. To optimise the preparation of liposomes with regards to size and entrapment efficiency, liposomes containing calcein were prepared by five different methods. Two optimal liposomal preparations (proliposomes and polyol dilution liposomes) were tested for their in vitro stability in media that simulate human vaginal conditions (buffer, pH 4.5). To be closer to in vivo application of liposomes and to achieve further improvement of their stability, liposomes were incorporated in vehicles suitable for vaginal self-administration. Gels of polyacrylate were chosen as vehicles for liposomal preparations. Due to their hydrophilic nature and bioadhesive properties, it was possible to achieve an adequate pH value corresponding to physiological conditions as well as desirable viscosity. In vitro release studies of liposomes incorporated in these gels (Carbopol 974P NF or Carbopol 980 NF) confirmed their applicability as a novel drug carrier system in vaginal delivery. Regardless of the gel used, even 24 h after the incubation of liposomal gel in the buffer pH 4.5 more than 80% of the originally entrapped substance was still retained. (C) 2001 Elsevier Science B.V. All rights reserved.