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Abstract：
BACKGROUND: This work proposes the development of new vesicular systems based on anesthetic compounds (lidocaine (LID) and capsaicin (CA)) and antimicrobial agents (amino acid-based surfactants from phenylalanine), with a focus on physicochemical characterization and the evaluation of antimicrobial and cytotoxic properties.
METHODS: Phenylalanine surfactants were characterized via high-performance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR). Different niosomal systems based on capsaicin, lidocaine, cationic phenylalanine surfactants, and dipalmitoyl phosphatidylcholine (DPPC) were characterized in terms of size, polydispersion index (PI), zeta potential, and encapsulation efficiency using dynamic light scattering (DLS), transmitted light microscopy (TEM), and small-angle X-ray scattering (SAXS). Furthermore, the interaction of the pure compounds used to prepare the niosomal formulations with DPPC monolayers was determined using a Langmuir balance. The antibacterial activity of the vesicular systems and their biocompatibility were evaluated, and molecular docking studies were carried out to obtain information about the mechanism by which these compounds interact with bacteria.
RESULTS: The stability and reduced size of the analyzed niosomal formulations demonstrate their potential in pharmaceutical applications. The nanosystems exhibit promising antimicrobial activity, marking a significant advancement in pharmaceutical delivery systems with dual therapeutic properties. The biocompatibility of some formulations underscores their viability.
CONCLUSIONS: The proposed niosomal formulations could constitute an important advance in the pharmaceutical field, offering delivery systems for combined therapies thanks to the pharmacological properties of the individual components.
METHODS: Phenylalanine surfactants were characterized via high-performance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR). Different niosomal systems based on capsaicin, lidocaine, cationic phenylalanine surfactants, and dipalmitoyl phosphatidylcholine (DPPC) were characterized in terms of size, polydispersion index (PI), zeta potential, and encapsulation efficiency using dynamic light scattering (DLS), transmitted light microscopy (TEM), and small-angle X-ray scattering (SAXS). Furthermore, the interaction of the pure compounds used to prepare the niosomal formulations with DPPC monolayers was determined using a Langmuir balance. The antibacterial activity of the vesicular systems and their biocompatibility were evaluated, and molecular docking studies were carried out to obtain information about the mechanism by which these compounds interact with bacteria.
RESULTS: The stability and reduced size of the analyzed niosomal formulations demonstrate their potential in pharmaceutical applications. The nanosystems exhibit promising antimicrobial activity, marking a significant advancement in pharmaceutical delivery systems with dual therapeutic properties. The biocompatibility of some formulations underscores their viability.
CONCLUSIONS: The proposed niosomal formulations could constitute an important advance in the pharmaceutical field, offering delivery systems for combined therapies thanks to the pharmacological properties of the individual components.
摘要：
背景：这项工作提出了基于麻醉化合物（利多卡因（LID）和辣椒素（CA））和抗微生物剂（来自苯丙氨酸的基于氨基酸的表面活性剂）的新型囊泡系统的开发，专注于物理化学表征以及抗菌和细胞毒性的评估。
方法：通过高效液相色谱（HPLC）和核磁共振（NMR）表征苯丙氨酸表面活性剂。基于辣椒素的不同的脂质体系统，利多卡因,阳离子苯丙氨酸表面活性剂，和二棕榈酰磷脂酰胆碱（DPPC）在大小方面进行了表征，多分散指数(PI)，zeta电位,使用动态光散射(DLS)和封装效率，透射光学显微镜（TEM），和小角度X射线散射（SAXS）。此外，使用Langmuir天平测定用于制备脂质体制剂的纯化合物与DPPC单层的相互作用。评估了囊泡系统的抗菌活性及其生物相容性，和分子对接研究，以获得有关这些化合物与细菌相互作用机制的信息。
结果：所分析的脂质体制剂的稳定性和减小的尺寸证明了它们在药物应用中的潜力。纳米系统表现出有希望的抗菌活性，标志着具有双重治疗特性的药物递送系统的显著进步。一些制剂的生物相容性强调了它们的生存力。
结论：提出的脂质体制剂可以构成制药领域的重要进展，由于各个成分的药理特性，为联合治疗提供输送系统。
方法：通过高效液相色谱（HPLC）和核磁共振（NMR）表征苯丙氨酸表面活性剂。基于辣椒素的不同的脂质体系统，利多卡因,阳离子苯丙氨酸表面活性剂，和二棕榈酰磷脂酰胆碱（DPPC）在大小方面进行了表征，多分散指数(PI)，zeta电位,使用动态光散射(DLS)和封装效率，透射光学显微镜（TEM），和小角度X射线散射（SAXS）。此外，使用Langmuir天平测定用于制备脂质体制剂的纯化合物与DPPC单层的相互作用。评估了囊泡系统的抗菌活性及其生物相容性，和分子对接研究，以获得有关这些化合物与细菌相互作用机制的信息。
结果：所分析的脂质体制剂的稳定性和减小的尺寸证明了它们在药物应用中的潜力。纳米系统表现出有希望的抗菌活性，标志着具有双重治疗特性的药物递送系统的显著进步。一些制剂的生物相容性强调了它们的生存力。
结论：提出的脂质体制剂可以构成制药领域的重要进展，由于各个成分的药理特性，为联合治疗提供输送系统。
