Aburayan Walaa S, Alajmi Areej M, Alfahad Ahmed J, Alsharif Wijdan K, Alshehri Abdullah A, Booq Rayan Y, Alsudir Samar A, Alsulaihem Fatemah M, Bukhary Haitham A, Badr Moutaz Y, Alyamani Essam J, Tawfik Essam A
National Center of Biotechnology, Life Science and Environment Research Institute, King Abdulaziz City for Science and Technology (KACST), Riyadh 11442, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, Umm Al-Qura University, Makkah 24381, Saudi Arabia.
Pharmaceutics. 2022 Mar 28;14(4):725. doi: 10.3390/pharmaceutics14040725.
Skin infection compromises the body's natural defenses. Several antibiotics are no longer effective owing to the evolution of antimicrobial-resistant (AMR) bacteria, hence, the constant development of novel antibacterial agents. Naturally occurring antibacterial agents may be potential candidates for AMR bacterial infection treatments; however, caution should be taken when administering such agents due to the high incidence of toxicity. A fibrous material system from a biocompatible polymer that could be used as a skin patch for skin infections treatment caused by AMR bacteria is proposed in this study. Bee venom's active ingredient, melittin, was fabricated using electrospinning technology. Scanning electron microscopy showed that melittin-loaded fibers had smooth surfaces with no signs of beads or pores. The average diameter of this fibrous system was measured to be 1030 ± 160 nm, indicating its successful preparation. The melittin fibers' drug loading and entrapment efficiency (EE%) were 49 ± 3 µg/mg and 84 ± 5%, respectively. This high EE% can be another successful preparatory criterion. An in vitro release study demonstrated that 40% of melittin was released after 5 min and achieved complete release after 120 min owing to the hydrophilic nature of the PVP polymer. A concentration of ≤10 µg/mL was shown to be safe for use on human dermal fibroblasts HFF-1 after 24-h exposure, while an antibacterial MIC study found that 5 μg/mL was the effective antimicrobial concentration for , , and yeast. A melittin-loaded fibrous system demonstrated an antibacterial zone of inhibition equivalent to the control (melittin discs), suggesting its potential use as a wound dressing patch for skin infections.
皮肤感染会损害人体的自然防御能力。由于抗菌耐药（AMR）细菌的进化，几种抗生素已不再有效，因此，新型抗菌剂不断涌现。天然存在的抗菌剂可能是治疗AMR细菌感染的潜在候选药物；然而，由于其高毒性发生率，在使用此类药物时应谨慎。本研究提出了一种由生物相容性聚合物制成的纤维材料系统，可作为治疗AMR细菌引起的皮肤感染的皮肤贴片。利用静电纺丝技术制备了蜂毒的活性成分蜂毒肽。扫描电子显微镜显示，负载蜂毒肽的纤维表面光滑，没有珠子或孔隙的迹象。该纤维系统的平均直径测量为1030±160nm，表明其制备成功。蜂毒肽纤维的载药量和包封率（EE%）分别为49±3μg/mg和84±5%。这种高EE%可以作为另一个成功的制备标准。体外释放研究表明，由于PVP聚合物的亲水性，5分钟后40%的蜂毒肽被释放，120分钟后实现完全释放。在24小时暴露后，≤10μg/mL的浓度对人皮肤成纤维细胞HFF-1使用是安全的，而抗菌MIC研究发现，5μg/mL是对金黄色葡萄球菌、大肠杆菌、白色念珠菌和热带念珠菌酵母的有效抗菌浓度。负载蜂毒肽的纤维系统显示出与对照（蜂毒肽圆盘）相当的抑菌圈，表明其作为皮肤感染伤口敷料贴片的潜在用途。
