Programa de Pós-Graduação em Ciências Biológicas: Farmacologia e Terapêutica, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil.
Programa de Pós-Graduação em Química, Instituto de Química, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil.
Drug Dev Ind Pharm. 2021 Jan;47(1):83-91. doi: 10.1080/03639045.2020.1862167. Epub 2020 Dec 28.
This study developed a novel child-friendly drug delivery system for pediatric HIV treatment: a liquid, taste-masked, and solvent-free monoolein-based nanoparticles formulation containing indinavir (0.1%).
Adherence to antiretroviral therapy by pediatric patients is difficult because of the lack of dosage forms adequate for children.
Monoolein-based nanoparticles were developed. The particle size, zeta potential, pH, drug content, small angle X-ray scattering, stability, drug release profile, biocompatibility, toxicity, and taste-masking properties were evaluated.
Monoolein-based formulations containing indinavir had nanosized particles with 155 ± 7 nm, unimodal particle size distribution, and polydispersity index of 0.16 ± 0.03. The zeta potential was negative (-31.3 ± 0.3 mV) and pH was neutral (7.78 ± 0.01). A 96% drug incorporation efficiency was achieved, and the indinavir concentration remained constant for 30 days. Polarized light microscopy revealed isotropic characteristics. Transmission electron microscopy images showed spherical shaped morphology. Small-angle X-ray scattering displayed a form factor broad peak. Indinavir had a sustained release from the nanoparticles. The system was nonirritant and was able to mask drug bitter taste.
Monoolein-based nanoparticles represent a suitable therapeutic strategy for antiretroviral treatment with the potential to reduce the frequency of drug administration and promote pediatric adherence.
本研究开发了一种新型儿童友好型药物递送系统，用于儿科 HIV 治疗：一种含有 0.1%茚地那韦的、无溶剂的、单油酸甘油酯基、口感掩蔽的纳米粒制剂。
由于缺乏适合儿童的剂型，儿科患者对抗逆转录病毒治疗的依从性较差。
开发了基于单油酸甘油酯的纳米粒。评估了粒径、Zeta 电位、pH 值、药物含量、小角 X 射线散射、稳定性、药物释放特性、生物相容性、毒性和口感掩蔽特性。
含有茚地那韦的单油酸甘油酯制剂具有纳米级颗粒，粒径为 155±7nm，呈单峰粒径分布，多分散指数为 0.16±0.03。Zeta 电位为负（-31.3±0.3mV），pH 值为中性（7.78±0.01）。实现了 96%的药物包封效率，茚地那韦浓度在 30 天内保持稳定。偏光显微镜显示各向同性特征。透射电子显微镜图像显示球形形态。小角 X 射线散射显示形态因子宽峰。纳米粒能持续释放茚地那韦。该系统无刺激性，能够掩盖药物的苦味。
基于单油酸甘油酯的纳米粒为抗逆转录病毒治疗提供了一种有前途的治疗策略，有可能减少药物给药频率，提高儿科患者的依从性。
