Rezigue Meriem, Mashaqbeh Hadeia, Aljabali Alaa A A, Mansour Randa Sh, Hamzeh Iyad
Pharmaceutics and Pharmaceutical Technology Department, Faculty of Pharmacy, Yarmouk University, Irbid 21163, Jordan.
Pharmaceutics and Pharmaceutical Technology Department, Faculty of Pharmacy, Zarqa University, Zarqa 13110, Jordan.
Pharmaceutics. 2025 Mar 21;17(4):400. doi: 10.3390/pharmaceutics17040400.
: The topical delivery of antibiotics through transethosomes shows promise for enhancing its dermal delivery for the treatment of skin infections. This study aimed to develop and characterize azithromycin-loaded transethosomes to enhance topical drug delivery and improve the antibacterial activity of azithromycin. : The prepared azithromycin formulations underwent assessment for various characteristics, including their vesicle dimensions, size distribution, zeta potential, encapsulation efficiency, and morphological features (via TEM analysis). Additionally, their thermal properties were examined through DSC analysis, and their stability was monitored over six months under refrigerated storage conditions. The sequential tape-stripping technique was employed to conduct ex vivo penetration studies on human skin. Interactions between transethosomes and stratum corneum lipids were examined using attenuated total reflectance Fourier-transform infrared spectroscopy (ATR-FTIR). Additionally, the formulations were tested for their in vitro antibacterial efficacy against . : The findings revealed that AZ 1 and AZ 2 had vesicle sizes of 108.44 ± 5.72 nm and 70.42 ± 6.02 nm, zeta potential measurements of -11.897 ± 1.820 mV and -34.575 ± 4.535 mV, and high entrapment efficiencies of 99.259 ± 0.086% and 99.560 ± 0.014%, respectively. Transmission electron microscopy (TEM) analysis confirmed the spherical nature of the vesicles, whereas differential scanning calorimetry (DSC) confirmed the successful encapsulation of azithromycin in transethosomes. The formulations exhibited acceptable physical stability at 4 °C for six months. Ex vivo studies revealed a significantly higher deposition of azithromycin in the skin by both transethosome formulations than by the drug solution ( < 0.05), with low systemic absorption. Among the formulations, AZ 2 resulted in much deeper skin penetration, with deeper dermal and epidermal layer deposition (1.388 ± 0.242 µg/cm) compared to AZ 1 (four-fold higher, < 0.05) and to the control drug solution (12 times more, < 0.05). Analysis using ATR-FTIR suggested that azithromycin-loaded transethosomes improve the drug penetration by increasing the lipid fluidity and extracting lipids from the stratum corneum. Moreover, the transethosomes loaded with azithromycin demonstrated enhanced antibacterial efficacy against , with minimum inhibitory concentration (MIC) values that were lower than those of the free drug solution. : The results highlight the promising potential of transethosomes as a novel topical drug delivery system for azithromycin that offers improved therapeutic effects against skin infections.
通过转质体进行抗生素的局部给药显示出增强其皮肤给药用于治疗皮肤感染的前景。本研究旨在开发和表征载阿奇霉素的转质体，以增强局部药物递送并提高阿奇霉素的抗菌活性。：对制备的阿奇霉素制剂进行了各种特性评估，包括其囊泡尺寸、大小分布、zeta电位、包封效率和形态特征（通过透射电子显微镜分析）。此外，通过差示扫描量热法分析检查了它们的热性质，并在冷藏储存条件下监测其六个月的稳定性。采用连续胶带剥离技术对人皮肤进行离体渗透研究。使用衰减全反射傅里叶变换红外光谱（ATR-FTIR）检查转质体与角质层脂质之间的相互作用。此外，测试了制剂对……的体外抗菌功效。：研究结果表明，AZ 1和AZ 2的囊泡尺寸分别为108.44±5.72 nm和70.42±6.02 nm，zeta电位测量值分别为-11.897±1.820 mV和-34.575±4.535 mV，包封效率分别为99.259±0.086%和99.560±0.014%，均较高。透射电子显微镜（TEM）分析证实了囊泡的球形性质，而差示扫描量热法（DSC）证实了阿奇霉素成功包封在转质体中。制剂在4℃下六个月表现出可接受的物理稳定性。离体研究表明，两种转质体制剂在皮肤中的阿奇霉素沉积均明显高于药物溶液（P<0.05），全身吸收较低。在制剂中，AZ 2导致皮肤渗透更深，与AZ 1相比，真皮和表皮层沉积更深（1.388±0.242μg/cm）（高四倍，P<0.05），与对照药物溶液相比（高12倍，P<0.05）。使用ATR-FTIR的分析表明，载阿奇霉素的转质体通过增加脂质流动性和从角质层中提取脂质来改善药物渗透。此外，载阿奇霉素的转质体对……表现出增强的抗菌功效，其最低抑菌浓度（MIC）值低于游离药物溶液。：结果突出了转质体作为阿奇霉素新型局部药物递送系统的潜在前景，其对皮肤感染具有改善的治疗效果。
