Novel Intravaginal Drug Delivery System Based on Molecularly PEGylated Lipid Matrices for Improved Antifungal Activity of Miconazole Nitrate.
Novel Intravaginal Drug Delivery System Based on Molecularly PEGylated Lipid Matrices for Improved Antifungal Activity of Miconazole Nitrate.
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DOI：
10.1155/2018/3714329
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发表时间：
2018
影响因子：
--
通讯作者：
Ozioko AC
中科院分区：
文献类型：
--
作者：
Kenechukwu FC;Attama AA;Ibezim EC;Nnamani PO;Umeyor CE;Uronnachi EM;Momoh MA;Akpa PA;Ozioko AC
本研究的目的是研究基于生物相容性植物脂[Softisan® 154（SF）（氢化棕榈油）和超精制葵花籽油（SO）]和聚乙二醇-（PEG-）4000的微粒改善硝酸咪康唑（MN）阴道内给药的潜力，以有效治疗外阴阴道念珠菌病（VVC）。脂质基质（LM）的SF和SO的合理的混合物与或没有PEG-4000的融合制备和表征，并采用熔融均质化配制MN负载的固体脂质微粒（SLM）。SLMs的理化性质，anticandidal活性，和稳定性进行了表征。获得了具有良好理化性质和平均粒径的球形分散微粒，适合于阴道给药。基于SO：SF（1：9）并含有最高浓度的PEG-4000（4%w/w）和MN（3.0%w/w）的制剂是稳定的，并且与MN的商业局部溶液（Fungusol®）（8.00 x 10−3 min−1）和纯MN样品（5.160 x 10−3 min−1）相比，具有最高的包封效率（83.05-87.75%）和抑制圈直径（25.87±0.94-26.33±0.94 mm）以及显著（p<0.05）更快和更强的杀真菌活性（关于杀灭速率常数值（7.10 x 10 − 3-1.09 x 10− 2 min−1）。这项研究表明，基于分子聚乙二醇化脂质基质的MN负载SLM可以提供更好的选择来处理VVC。
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 10−3–1.09 x 10−2 min−1) than commercial topical solution of MN (Fungusol®) (8.00 x 10−3 min−1) and pure MN sample (5.160 x 10−3 min−1). This study has shown that MN-loaded SLMs based on molecularly PEGylated lipid matrices could provide a better option to deal with VVC.
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影响因子：
6
作者：
Attama, A. A.;Okafor, C. E.;Okorie, O.
通讯作者：
Okorie, O.
影响因子：
8
作者：
Aljaeid BM;Hosny KM
通讯作者：
Hosny KM
影响因子：
3.3
作者：
Elmoslemany, Riham M.;Abdallah, Ossama Y.;Khalafallah, Nawal M.
通讯作者：
Khalafallah, Nawal M.
影响因子：
3
作者：
Dorgan, Eileen;Denning, David W.;McMullan, Ronan
通讯作者：
McMullan, Ronan
影响因子：
8
作者：
Bonifácio BV;Ramos MA;da Silva PB;Negri KM;de Oliveira Lopes É;de Souza LP;Vilegas W;Pavan FR;Chorilli M;Bauab TM
通讯作者：
Bauab TM