Abudoleh Suha M, Abu Ershaid Juhaina M, Lafi Dima, Dahshan Nisreen A, Talhouni Ahmad, Abuirmeileh Amjad
Department of Basic Pharmaceutical Sciences, Faculty of Pharmacy, Middle East University, Amman 11831, Jordan.
Department of Applied Pharmaceutical Sciences and Clinical Pharmacy, Faculty of Pharmacy, Isra University, Amman 11622, Jordan.
Pharmaceutics. 2025 May 31;17(6):727. doi: 10.3390/pharmaceutics17060727.
Acne vulgaris is a chronic skin infection characterized by high sebum secretion, keratosis around hair follicles, inflammation, and imbalance in androgen levels. Acne vulgaris causes permanent scars or skin pigmentation in cases of improper treatment. Oral or topical isotretinoin, contraceptives, and antibiotics are used to treat acne. Minocycline is one of the widely used tetracyclines for this purpose; it inhibits the synthesis of proteins in bacterial ribosomes. Commonly, minocycline is prescribed daily for several months for acne vulgaris. Systemic minocycline is highly distributed into body fluids, and it is associated with several side effects and antibiotic resistance. Additionally, minocycline is highly metabolized in the liver, leading to reduced bioavailability upon systemic delivery. This study aims to develop and characterize minocycline nanocrystals for targeted skin delivery and evaluate their antimicrobial efficacy in treating acne vulgaris. : Minocycline nanocrystals were synthesized using milling or solvent evaporation techniques. Nanocrystals were characterized in terms of particle size, particle distribution index (PDI), zeta potential, and morphology. The antibacterial efficacy against , , and was evaluated using a minimum inhibitory concentration assay (MIC) and agar well diffusion test in comparison to coarse minocycline. : Minocycline nanocrystals had a particle size of 147.4 ± 7.8 nm and 0.27 ± 0.017 of PDI. The nanocrystals exhibited a loading efficiency of 86.19 ± 16.7%. Antimicrobial testing showed no significant difference in activity between minocycline and its nanoparticle formulation. In terms of skin deposition, the nanocrystals were able to deliver minocycline topically to rat skin significantly more than free minocycline. The nanocrystal solution deposited 554.56 ± 24.13 μg of minocycline into rat skin, whereas free minocycline solution deposited 373.99 ± 23.32 μg. : Minocycline nanocrystals represent a promising strategy for targeted skin delivery in the treatment of acne vulgaris, potentially reducing systemic side effects and antibiotic resistance and improving patient outcomes.
寻常痤疮是一种慢性皮肤感染，其特征为皮脂分泌过多、毛囊周围角化、炎症以及雄激素水平失衡。若治疗不当，寻常痤疮会导致永久性疤痕或皮肤色素沉着。口服或外用异维甲酸、避孕药及抗生素可用于治疗痤疮。米诺环素是为此目的广泛使用的四环素类药物之一；它抑制细菌核糖体中的蛋白质合成。通常，米诺环素每日给药用于治疗寻常痤疮，疗程数月。全身性米诺环素在体液中分布广泛，且与多种副作用及抗生素耐药性有关。此外，米诺环素在肝脏中高度代谢，导致全身给药后生物利用度降低。本研究旨在开发米诺环素纳米晶体并对其进行表征以实现靶向皮肤给药，并评估其治疗寻常痤疮的抗菌疗效。：采用研磨或溶剂蒸发技术合成米诺环素纳米晶体。从粒径、粒度分布指数（PDI）、ζ电位和形态方面对纳米晶体进行表征。与粗品米诺环素相比，使用最低抑菌浓度测定法（MIC）和琼脂孔扩散试验评估对痤疮丙酸杆菌、金黄色葡萄球菌和表皮葡萄球菌的抗菌疗效。：米诺环素纳米晶体的粒径为147.4±7.8nm，PDI为0.27±0.017。纳米晶体的载药效率为86.19±16.7%。抗菌测试表明米诺环素及其纳米颗粒制剂之间的活性无显著差异。在皮肤沉积方面，纳米晶体能够比游离米诺环素更显著地将米诺环素局部递送至大鼠皮肤。纳米晶体溶液向大鼠皮肤沉积了554.56±24.13μg米诺环素，而游离米诺环素溶液沉积了373.99±23.32μg。：米诺环素纳米晶体是治疗寻常痤疮靶向皮肤给药的一种有前景的策略，可能减少全身副作用和抗生素耐药性并改善患者预后。
