Drug Delivery and Nanomedicines Research Group, Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Enugu State, Nigeria.
Nanomedicines and Drug Delivery Unit, Department of Pharmaceutics and Pharmaceutical Technology, Nnamdi Azikiwe University, Awka, Anambra State, Nigeria.
Biomed Res Int. 2018 Jun 6;2018:3714329. doi: 10.1155/2018/3714329. eCollection 2018.
The aim of this study was to investigate the potential of microparticles based on biocompatible phytolipids [Softisan® 154 (SF) (hydrogenated palm oil) and super-refined sunseed oil (SO)] and polyethylene glycol- (PEG-) 4000 to improve intravaginal delivery of miconazole nitrate (MN) for effective treatment of vulvovaginal candidiasis (VVC). Lipid matrices (LMs) consisting of rational blends of SF and SO with or without PEG-4000 were prepared by fusion and characterized and employed to formulate MN-loaded solid lipid microparticles (SLMs) by melt-homogenization. The SLMs were characterized for physicochemical properties, anticandidal activity, and stability. Spherical discrete microparticles with good physicochemical properties and mean diameters suitable for vaginal drug delivery were obtained. Formulations based on SO:SF (1:9) and containing highest concentrations of PEG-4000 (4 %w/w) and MN (3.0 %w/w) were stable and gave highest encapsulation efficiency (83.05-87.75%) and inhibition zone diameter (25.87±0.94-26.33±0.94 mm) and significantly (p<0.05) faster and more powerful fungicidal activity regarding killing rate constant values (7.10 x 10-1.09 x 10 min) than commercial topical solution of MN (Fungusol®) (8.00 x 10 min) and pure MN sample (5.160 x 10 min). This study has shown that MN-loaded SLMs based on molecularly PEGylated lipid matrices could provide a better option to deal with VVC.
本研究旨在探讨基于生物相容的植物脂质[Softisan® 154（SF）（氢化棕榈油）和精炼葵花籽油（SO）]和聚乙二醇-（PEG-）4000 的微粒，以提高米康唑硝酸盐（MN）的阴道内传递，从而有效治疗外阴阴道念珠菌病（VVC）。由 SF 和 SO 与或不与 PEG-4000 合理混合的脂质基质（LM）通过熔融混合制备，并对其进行了表征，用于通过熔融匀化来制备载有米康唑的固体脂质微球（SLM）。对 SLM 的理化性质、抗真菌活性和稳定性进行了表征。得到了具有良好理化性质和适合阴道给药的平均粒径的球形离散微球。基于 SO：SF（1：9）的制剂，含有最高浓度的 PEG-4000（4%w/w）和 MN（3.0%w/w），是稳定的，并具有最高的包封效率（83.05-87.75%）和抑菌圈直径（25.87±0.94-26.33±0.94mm），并且在杀菌率常数值（7.10×10-1.09×10-1 min）方面比商用 MN 局部溶液（Fungusol®）（8.00×10-1 min）和纯 MN 样品（5.160×10-1 min）更快、更有效。本研究表明，基于分子 PEG 化脂质基质的载 MN SLM 可为治疗 VVC 提供更好的选择。
