Formulation and Characterization of Sertaconazole Nitrate Mucoadhesive Liposomes for Vaginal Candidiasis
Formulation and Characterization of Sertaconazole Nitrate Mucoadhesive Liposomes for Vaginal Candidiasis
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DOI：
10.2147/ijn.s250960
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发表时间：
2020-01-01
影响因子：
8
通讯作者：
Al-Mokaddem, Asmaa K.
中科院分区：
文献类型：
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作者：
Abdellatif, Menna M.;Khalil, Islam A.;Al-Mokaddem, Asmaa K.
目的：探讨硝酸舍他康唑局部治疗阴道念珠菌病的有效方法。方法：采用薄膜水合法制备硝酸塞他康唑阳离子脂质体，并包被不同浓度的果胶（0.05%、0.1%、0.2%）制成黏附脂质体。从形貌、包封效率、粒径、zeta值、黏附性能和药物释放等方面对所制备的黏附囊泡进行了表征。将选定的配方掺入凝胶基中，并与常规的舍他康唑凝胶进行体外渗透研究。同时，对舍他康唑黏附脂质体凝胶对阴道念珠菌病大鼠的治疗效果进行了体内研究。结果：黏附脂质体呈球形。与未包覆的囊泡相比，用果胶包覆脂质体可提高包覆效率和颗粒大小。相反，用果胶包覆脂质体后，zeta值降低，表明果胶包覆脂质体是有效的。黏附脂质体比未包被的脂质体具有更持久的药物释放。离体研究结果表明，黏附脂质体凝胶增加了舍他康唑的组织滞留，降低了药物的组织渗透。在体内研究中，与常规凝胶相比，黏附脂质体凝胶显示微生物计数显著减少，随后炎症反应减少，组织病理学变化最低。结论：本研究证实了黏附脂质体作为阴道给药载体的可行性。
Purpose: The aim of this study is to develop efficient localized therapy of sertaconazole nitrate for the treatment of vaginal candidiasis.Methods: Sertaconazole nitrate-loaded cationic liposomes were prepared by thin- film hydration method and coated with different concentrations of pectin (0.05%, 0.1% and 0.2%) to develop mucoadhesive liposomes. The formulated mucoadhesive vesicles were characterized in terms of morphology, entrapment efficiency, particle size, zeta value, mucoadhesive properties and drug release. The selected formula was incorporated into a gel base and further characterized by an ex vivo permeation study in comparison with conventional sertaconazole gel. Also, the in vivo study was performed to assess the efficacy of sertaconazole mucoadhesive liposomal gel in treating rats with vaginal candidiasis.Results: The mucoadhesive liposomes were spherical. Coating liposomes with pectin results in increased entrapment efficiency and particle size compared with uncoated vesicles. On the contrary, zeta values were reduced upon coating liposomes with pectin indicating efficient coating of liposomes with pectin. Mucoadhesive liposomes showed a more prolonged and sustained drug release compared with uncoated liposomes. Ex vivo study results showed that mucoadhesive liposomal gel increased sertaconazole tissue retention and reduced drug tissue penetration. In the invivo study, the mucoadhesive liposomal gel showed a significant reduction in the microbial count with a subsequent reduction in inflammatory responses with the lowest histopathological change compared with conventional gel.Conclusion: The study confirmed the potentiality of employing mucoadhesive liposomes as a successful carrier for the vaginal delivery of antifungal drugs.