使用三元相体系在载氯己定有机凝胶中制备姜黄素包封脂质体用于治疗婴儿脐炎

Development of Curcumin Encapsulated Liposomes in Chlorhexidine-Loaded Organogel Using Ternary Phase Systems for Treatment of Omphalitis in Infants.

作者信息

Cardoso-Daodu Ibilola Mary, Ilomuanya Margaret Okonawan

机构信息

Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, University of Lagos, PMB 12003, Lagos, Nigeria.

出版信息

Adv Pharmacol Pharm Sci. 2025 Jan 30;2025:6828052. doi: 10.1155/adpp/6828052. eCollection 2025.

Abstract

Infections in infants, after childbirth, remain a leading cause of neonatal morbidity and mortality, globally. A soaring percentage of these infections arise from bacterial colonization of the umbilicus. Current therapy for omphalitis includes the topical application of chlorhexidine on the umbilicus. Bacteria such as which are the key causative organisms of omphalitis, are resistant to chlorhexidine. In this study, curcumin-loaded liposomes were prepared using the "thin film hydration" method. Liposomes were characterized by particle size analysis, light microscopy, encapsulation efficiency, and flux. Stable organogels were formed via a high-speed homogenization method and stabilized by an emulsifier mix. They were evaluated for stability over a period by observing for phase separation. Four gels F1 (curcumin-loaded liposomes in chlorhexidine organogel), F2 (curcumin-loaded liposomes in organogel), F3 (chlorhexidine in organogel), and control (plain organogel) were prepared. Physicochemical properties of all gels were evaluated such as organoleptic tests, gel-to-sol transition, rheological studies, pH, skin irritancy, spreadability, accelerated stability, and antibacterial activity studies. Liposomes were spherical with an average size of 7 μm and an encapsulation efficiency of 97%. The release profile best fits the Higuchi mathematical model implying that curcumin release was by diffusion and dissolution mechanism. release was also higher at pH 5.5. F1 had the highest spreadability of 63 mmg and the lowest viscosity of 184,400 MPas at a shear rate of 10 rotations per minute with a pH of 6.5. Formulation F1 also displayed the highest antibacterial activity against all three bacteria. It can be concluded that the synergistic interaction between curcumin and chlorhexidine may be responsible for the significant antibacterial potency exhibited in formulation F1. Curcumin-loaded liposomes in chlorhexidine organogel (F1) can serve as a prototype for the development of an antibacterial topical formulation having intrinsic activity and enhanced potency to combat omphalitis.

摘要

在全球范围内,婴儿产后感染仍然是新生儿发病和死亡的主要原因。这些感染中,脐部细菌定植导致的感染比例正在飙升。目前治疗脐炎的方法包括在脐部局部应用氯己定。诸如引起脐炎的关键病原体等细菌对氯己定具有耐药性。在本研究中,采用“薄膜水化”法制备了载姜黄素脂质体。通过粒度分析、光学显微镜、包封率和通量对脂质体进行表征。通过高速均质法形成稳定的有机凝胶,并用乳化剂混合物进行稳定。通过观察相分离情况,对其在一段时间内的稳定性进行评估。制备了四种凝胶F1(氯己定有机凝胶中的载姜黄素脂质体)、F2(有机凝胶中的载姜黄素脂质体)、F3(有机凝胶中的氯己定)和对照(普通有机凝胶)。对所有凝胶的物理化学性质进行了评估,如感官测试、凝胶-溶胶转变、流变学研究、pH值、皮肤刺激性、铺展性、加速稳定性和抗菌活性研究。脂质体呈球形,平均大小为7μm,包封率为97%。姜黄素释放曲线最符合Higuchi数学模型,这意味着姜黄素的释放是通过扩散和溶解机制进行的。在pH 5.5时姜黄素的释放量也更高。在pH值为6.5、剪切速率为每分钟10转的情况下,F1的铺展性最高,为63 mm/g,粘度最低,为184400 mPa·s。制剂F1对所有三种细菌也表现出最高的抗菌活性。可以得出结论,姜黄素和氯己定之间的协同相互作用可能是制剂F1中显著抗菌效力的原因。氯己定有机凝胶中的载姜黄素脂质体(F1)可作为开发具有内在活性和增强效力以对抗脐炎的抗菌局部制剂的原型。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/54b3/11824790/27f69e2f87b5/APS2025-6828052.001.jpg

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