Abstract
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.
Highlights
Over the past two decades, there has been a dramatic increase in the rate of vulvovaginal candidiasis (VVC), a common fungal infection caused by abnormal growth of yeast-like fungi (Candida albicans) on the female genital tract mucosa [1] and often characterized by painful and uncomfortable manifestations such as intense itching, irritation, vaginal discharge, erythema, and dysuria [2,3,4], with associated diminished quality of life of many women, considerable morbidity, and high and escalating healthcare cost to the society [5]
The use of miconazole nitrate (MN) for localized treatment of VVC is limited by low bioavailability, requirement for multiple daily doses, difficulty in reaching the target site due to the low penetration capacity to treat deep-seated recurrent VVC, and drug resistance
The potential of intravaginal PEGylated solid lipid microparticles (SLMs) in prolonged localized vaginal delivery of MN was investigated for improved treatment of VVC
Summary
Over the past two decades, there has been a dramatic increase in the rate of vulvovaginal candidiasis (VVC), a common fungal infection caused by abnormal growth of yeast-like fungi (Candida albicans) on the female genital tract mucosa [1] and often characterized by painful and uncomfortable manifestations such as intense itching, irritation, vaginal discharge, erythema, and dysuria [2,3,4], with associated diminished quality of life of many women, considerable morbidity, and high and escalating healthcare cost to the society [5]. The infection most often reoccurs; patients receive therapy over a long time [1, 10]. It has been suggested that the cause of relapse in women
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