Distearoyl phosphatidylglycerol and dioleoyl phosphatidylglycerol increase the retention and reduce the toxicity of amphotericin B-loaded in nanoemulsions.

Nanomedicine (London, England) Pub Date : 2024-02-01 Epub Date: 2024-01-31 DOI:10.2217/nnm-2023-0256

Gabriel Silva Marques Borges, Thais Tunes Santos, Cristiane Monteiro Pinto, Frédéric Frézard, Verônica Freitas Blanco, Roberta Ondei, Stephen Rumbelow, Lucas Antônio Miranda Ferreira, Marta Marques Gontijo de Aguiar, Gisele Assis Castro Goulart

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Abstract

Aim: To develop nanoemulsions (NEs) loading amphotericin B (AmB) and to evaluate the influence of different excipients on the stability and the supramolecular organization, retention and toxicity of AmB. Materials & methods: The NEs were developed from different oils, surfactants, external media and anionic lipids (disteaoryl phosphatidylglycerol [DSPG] and dioleoyl phosphatidylglycerol [DOPG]). Their impact on the size, pH, zeta potential, AmB encapsulation efficiency, AmB retention and hemolytic potential of the NEs was evaluated. Results & conclusion: The use of soybean oil (lipid matrix), Span 80 (surfactant), phosphate buffer (external phase) and DSPG or DOPG (hydrophobic ion pair) provided better NE stability, higher AmB retention within the NEs and a safer formulation profile in hemolysis tests.

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二硬脂酰基磷脂酰甘油和二油酰基磷脂酰甘油可提高纳米乳剂中两性霉素 B 的保留率并降低其毒性。

目的：开发负载两性霉素 B（AmB）的纳米乳剂（NEs），并评估不同辅料对 AmB 的稳定性、超分子组织、保留和毒性的影响。材料与方法：NEs 由不同的油、表面活性剂、外部介质和阴离子脂质（二乙基磷脂酰甘油 [DSPG] 和二油酰磷脂酰甘油 [DOPG]）制成。评估了它们对 NEs 的尺寸、pH 值、Zeta 电位、AmB 包封效率、AmB 保留率和溶血潜能的影响。结果与结论使用大豆油（脂质基质）、Span 80（表面活性剂）、磷酸盐缓冲液（外相）和 DSPG 或 DOPG（疏水离子对）可提高 NE 的稳定性，在 NE 中保留更多 AmB，并在溶血试验中提供更安全的制剂概况。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Nanomedicine (London, England)

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