Assessing the physical-chemical properties and stability of dapivirine-loaded polymeric nanoparticles

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• 作者：Jos¨¦ das Neves ; Mansoor Amiji ; Maria Fern ; a Bahia ; Bruno Sarmento
• 关键词：HIV/AIDS ; Microbicides ; Poly(epsilon-caprolactone) ; Colloidal stability ; Drug release
• 刊名：International Journal of Pharmaceutics
• 出版年：2013
• 出版时间：18 November, 2013
• 年：2013
• 卷：456
• 期：2
• 页码：307-314
• 全文大小：1536 K

文摘

Nanocarriers may provide interesting delivery platforms for microbicide drugs and their characterization should be addressed early in development. Differently surface-engineered dapivirine-loaded, poly(epsilon-caprolactone) (PCL)-based nanoparticles (NPs) were obtained by nanoprecipitation using polyethylene oxide (PEO), sodium lauryl sulfate (SLS), or cetyltrimethylammonium bromide (CTAB) as surface modifiers. Physical-chemical properties of NP aqueous dispersions were evaluated upon storage at ?20-40 ¡ãC for one year. NPs presented 170-200 nm in diameter, roundish-shape, low polydispersity index (¡Ü0.18), and high drug association efficiency (¡Ý97 % ) and loading (¡Ý12.7 % ). NPs differed in zeta potential, depending on surface modifier (PEO: ?27.9 mV; SLS: ?54.7 mV; CTAB: +42.4 mV). No interactions among formulation components were detected by differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR), except for SLS-PCL NPs. Colloidal properties of NPs were lost at ?20 ¡ãC storage. Negatively charged NPs were stable up to one year at 5-40 ¡ãC; as for CTAB-PCL NPs, particle aggregation was observed from 30 to 90 days of storage depending on temperature. Colloidal instability affected the in vitro drug release of CTAB-PCL NPs after 360 days. In any case, no degradation of dapivirine was apparent. Overall, PEO-PCL and SLS-PCL NPs presented suitable properties as nanocarriers for dapivirine. Conversely, CTAB-PCL NPs require additional strategies in order to increase stability.