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FbD directed fabrication and investigation of luliconazole based SLN gel for the amelioration of candidal vulvovaginitis: a 2 T (thermosensitive & transvaginal) approach
Saudi Journal of Biological Sciences Pub Date : 2020-10-16 , DOI: 10.1016/j.sjbs.2020.10.005
Salma Firdaus , Nazia Hassan , Mohd. Aamir Mirza , Tabasum Ara , Hamed A. El-Serehy , Fahad A. Al-Misned , Zeenat Iqbal

Candidal vulvovaginitis (CVV), is the second most leading vaginal infection (global prevalence > 75%), caused due to excessive growth of Candida spp., predominantly Candida albicans (>95% cases). The current treatment regimens for CVV are marred with the challenges of fungal resistance & infection recurrence, subsequently leading to the compromised therapeutic efficacy of anti-fungal drugs, prolonged treatment and low patient compliance. The core of the present research was the fabrication & investigation of 2 T-SLN (solid lipid nanoparticles) gel carrying luliconazole for the amelioration of CVV. ‘2T’ symbolizes transvaginal & thermosensitive attributes of the present formulation. SLNs were prepared by a modified melt emulsification-ultra sonication method using a combination of solid lipids (Gelucire 50/13 & Precirol ATO 5), surfactant (Tween 80) and co-surfactant (Kolliphor). Formulation by design (FbD) approach was adopted to obtain appropriately screened and tailored SLNs. The optimized SLNs yielded a particle size, polydispersity index & entrapment efficiency of 62.18 nm, 0.263 & 81.5% respectively. To formulate the 2 T-gel, the final SLNs were loaded into Carbopol 971P-NF and Triethanolamine based gel. The 2 T-SLN gel was found to be easily spreadable and homogenous with mean extrudability (15 ± 0.4 g/cm2), viscosity (696.42 ± 2.34 Pa·s) and %drug content (93.24 ± 0.73%) values.. The pH of the prepared 2 T-SLN gel (4.5 ± 0.5) was in concordance with the vaginal pH (normal conditions). For in-vitro characterization of an optimized 2 T-SLN gel the release kinetics & anticandidal activity were assessed which offers a %cumulative drug release of 62 ± 0.5% in 72 h and 37.3 ± 1.5 mm zone of inhibition in 48 h. The visual appearance & dimensions were determined using fluorescent microscopy (spherical shape) & transmission electron microscopy (90–120 nm) respectively. The optimized 2 T-SLN gel showcases a skin-friendly profile with no significant signs of erythema and oedema and was found to be stable at room temperature for 2 months without any visual non-uniformity/cracking/breaking. In conclusion, the current research serves a new therapeutic perspective in assessing the activity of luliconazole for vaginal drug delivery using a 2 T-SLN gel system.



中文翻译:

FbD指导的基于卢立康唑的SLN凝胶的制备和研究,以改善念珠菌性外阴阴道炎:2 T(热敏和经阴道)方法

念珠菌性外阴阴道炎(CVV)是第二大最主要的阴道感染(全球患病率> 75%),是由于假丝酵母菌过度生长引起的。主要是白色念珠菌(> 95%的情况)。当前的CVV治疗方案充满了真菌抗药性和感染复发的挑战,随后导致抗真菌药的治疗功效下降,治疗时间延长和患者依从性降低。本研究的核心是制造和研究2种带有卢立康​​唑的T-SLN(固体脂质纳米颗粒)凝胶,以改善CVV。“ 2T”象征本制剂的经阴道和热敏特性。SLN通过改良的熔融乳化-超音波方法,结合使用固体脂质(Gelucire 50/13和Precirol ATO 5),表面活性剂(Tween 80)和助表面活性剂(Kolliphor)来制备。采用设计配方(FbD)方法来获得经过适当筛选和定制的SLN。优化的SLNs的粒径,多分散指数和截留效率分别为62.18 nm,0.263和81.5%。为了配制2 T-凝胶,将最终的SLN装入Carbopol 971P-NF和三乙醇胺基凝胶中。发现2 T-SLN凝胶易于铺展且均匀,平均可挤出性(15±0.4 g / cm2),粘度(696.42±2.34 Pa·s)和%药物含量(93.24±0.73%)值。制备的2 T-SLN凝胶的pH(4.5±0.5)与阴道pH(正常条件)一致)。对于体外对优化的2 T-SLN凝胶的表征,评估了其释放动力学和抗candidal活性,可在72小时内提供62±0.5%的累积药物释放百分比,并在48小时内提供37.3±1.5 mm的抑制区域。视觉外观和尺寸分别使用荧光显微镜(球形)和透射电子显微镜(90-120 nm)确定。经过优化的2 T-SLN凝胶具有皮肤亲和性,没有明显的红斑和浮肿迹象,并且在室温下可稳定放置2个月,没有任何视觉上的不均匀/开裂/破裂现象。总之,当前的研究为使用2 T-SLN凝胶系统评估卢立康唑用于阴道给药的活性提供了新的治疗方法。

更新日期:2020-12-25
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