Design, Characterization, and Biopharmaceutical Behavior of Nanoparticles Loaded with an HIV-1 Fusion Inhibitor Peptide,Molecular Pharmaceutics

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Design, Characterization, and Biopharmaceutical Behavior of Nanoparticles Loaded with an HIV-1 Fusion Inhibitor Peptide
Molecular Pharmaceutics ( IF 4.5 ) Pub Date : 2018-09-18 00:00:00 , DOI: 10.1021/acs.molpharmaceut.8b00609
Martha Ariza-Sáenz _{1,

2} , Marta Espina ₁ , Ana Calpena ₁ , María J. Gómara ₂ , Ignacio Pérez-Pomeda ₂ , Isabel Haro ₂ , María Luisa García ₁

Affiliation

New therapeutic alternatives to fight against the spread of HIV-1 are based on peptides designed to inhibit the early steps of HIV-1 fusion in target cells. However, drawbacks, such as bioavailability, short half-life, rapid clearance, and poor ability to cross the physiological barriers, make such peptides unattractive for the pharmaceutical industry. Here we developed, optimized, and characterized polymeric nanoparticles (NPs) coated with glycol chitosan to incorporate and release an HIV-1 fusion inhibitor peptide (E1) inside the vaginal mucosa. The NPs were prepared by a modified double emulsion method, and optimization was carried out by a factorial design. In vitro, ex vivo, and in vivo studies were carried out to evaluate the optimized formulation. The results indicate that the physicochemical features of these NPs enable them to incorporate and release HIV fusion inhibitor peptides to the vaginal mucosa before the fusion step takes place.

中文翻译：

载有HIV-1融合抑制剂肽的纳米粒子的设计，表征和生物制药行为。

对抗HIV-1传播的新的治疗选择是基于旨在抑制HIV-1在靶细胞中融合的早期步骤的肽。但是，诸如生物利用度，半衰期短，清除快和克服生理屏障的能力差等缺点使此类肽对制药业没有吸引力。在这里，我们开发，优化和表征了涂有乙二醇壳聚糖的聚合物纳米颗粒（NPs），以在阴道粘膜内部掺入并释放HIV-1融合抑制剂肽（E1）。通过改进的双乳化法制备NP，并通过析因设计进行优化。进行了体外，离体和体内研究以评估优化的制剂。

更新日期：2018-09-18

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