Nanobiofar Group, Department of Pharmacology, Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Santiago de Compostela, Campus Vida, E-15782, Santiago de Compostela, Spain; Drug Science Department, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
Drug Science Department, University of Pavia, Viale Taramelli 12, 27100 Pavia, Italy.
Carbohydr Polym. 2017 Aug 15;170:43-51. doi: 10.1016/j.carbpol.2017.04.051. Epub 2017 Apr 23.
Recently nanoparticle-based vaginal drug delivery formulations have been acquiring great attention for the administration of peptide based-vaccines or microbicides to prevent or treat sexually transmitted diseases. In this work, a straightforward and efficient strategy for the vaginal application and release of peptide-loaded mucoadhesive nanoparticles was developed. This essentially consists of chitosan nanoparticles encapsulated in suitable hydrophilic freeze-dried cylinders. Chitosan nanoparticles are responsible for carrying the peptide drug and allowing adhesion to the vaginal mucosal epithelium. Hydrophilic freeze-dried cylinders facilitate the application and quick release of the nanoparticles to the vaginal zone. Upon contact with the aqueous vaginal medium, the excipients constituting these sponge-like systems are quickly dissolved enabling the release of their content. In vitro release studies showed the ability of the sponge-like systems and chitosan nanoparticles to deliver the mucoadhesive nanoparticles and peptide respectively. CLSM micrographs proved the nanoparticles ability promoting the peptide penetration inside the vaginal mucosa.
最近，基于纳米粒子的阴道给药制剂在给药基于肽的疫苗或杀微生物剂以预防或治疗性传播疾病方面受到了极大关注。在这项工作中，开发了一种用于阴道应用和释放载肽的粘膜粘附性纳米粒子的简单有效的策略。这主要包括包封在合适的亲水性冷冻干燥圆柱体内的壳聚糖纳米粒子。壳聚糖纳米粒子负责携带肽药物并允许与阴道粘膜上皮粘附。亲水性冷冻干燥圆柱体能促进纳米粒子的应用和快速释放到阴道区域。与含水的阴道介质接触时，构成这些海绵状系统的赋形剂迅速溶解，使其中的内容物释放出来。体外释放研究表明，海绵状系统和壳聚糖纳米粒子具有分别输送粘膜粘附纳米粒子和肽的能力。CLSM 显微照片证明了纳米粒子促进肽穿透阴道粘膜的能力。
