Menadione Sodium Bisulfite Loaded Rhamnolipid Based Solid Lipid Nanoparticle as Skin Lightener Formulation: A Green Production Beside In Vitro/In Vivo Safety Index Evaluation.

IF 3.1 Q2 PHARMACOLOGY & PHARMACY
Advanced pharmaceutical bulletin Pub Date : 2024-10-01 Epub Date: 2024-06-22 DOI:10.34172/apb.2024.047
Fatemeh Asadpour Panbehchouleh, Hossein Amani, Majid Saeedi
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Abstract

Purpose: In the current investigation, an ultrasonic approach was performed to produce menadione sodium bisulfite-loaded solid lipid nanoparticles (MSB-SLNs) with rhamnolipid as bio-surfactant, which aimed to increase the dermal delivery and anti-pigmentation effect.

Methods: To achieve optimum delivery for MSB, the impact of the ratio of two surfactants (rhamnolipid: Tween) on nanoparticle attributes and the respective functions were evaluated. In vitro diffusion process, in vitro cytotoxicity assay, determination of melanin content of melanoma cells, L-DOPA auto-oxidation inhibitory test, and skin irritation studies carried out to investigate the suitability of MSB formulation in dermal application.

Results: The optimized nanoparticles showed an average particle size, zeta potential, polydispersity index (PDI), and drug entrapment efficiency of 117.26±1.12 nm, -6.28±0.33 mV, 0.262±0.002, 83.34±0.75% respectively in hydrophilic-lipophilic balance (HLB) of 12. The in vitro diffusion process demonstrated that MSB-SLN gel had a prolonged release pattern. The levels of MSB in the cutaneous layers (52.192±2.730% or 961.59±50.313 μg/cm2 ) and the receiver compartment (23.721±1.803 % or 437.049± 33.236 μg/cm2 ) for the MSB-SLN gel was higher than MSB simple and showed no cutaneous irritancy and toxicity in rats. MSB-SLN inhibited melanin formation and was remarkably higher than free MSB. MSB-SLN inhibited L-3,4- dihydroxyphenylalanine (L-DOPA) auto-oxidation to a greater extent (95.14±1.46%) than MSB solution (72.28±0.83%).

Conclusion: This study's observations revealed that the produced MSB-SLN might be used as a potential nano-vehicle for MSB dermal administration, thereby opening up innovative options for the management of hyper-melanogenesis problems.

作为皮肤增白剂配方的亚硫酸氢钠美那二酮负载鼠李糖脂基固体脂质纳米粒子:体外/体内安全指数评估之外的绿色生产。
目的:本研究采用超声波方法制备了以鼠李糖脂作为生物表面活性剂的亚硫酸氢钠负载固体脂质纳米颗粒(MSB-SLNs),旨在提高其皮肤递送和抗色素沉着效果:为了实现 MSB 的最佳递送效果,我们评估了两种表面活性剂(鼠李糖脂:吐温)的比例对纳米粒子属性和各自功能的影响。此外,还进行了体外扩散过程、体外细胞毒性试验、黑色素瘤细胞黑色素含量测定、L-DOPA 自氧化抑制试验和皮肤刺激性研究,以考察 MSB 制剂在皮肤应用中的适用性:结果:在亲水-亲油平衡(HLB)为 12 的条件下,优化后的纳米颗粒的平均粒径、ZETA电位、多分散指数(PDI)和药物包埋效率分别为 117.26±1.12 nm、-6.28±0.33 mV、0.262±0.002、83.34±0.75%。体外扩散过程表明,MSB-SLN 凝胶具有延长释放模式。MSB-SLN凝胶在皮肤层(52.192±2.730%或961.59±50.313 μg/cm2)和接收层(23.721±1.803%或437.049±33.236 μg/cm2)的MSB含量高于单纯的MSB,且对大鼠无皮肤刺激性和毒性。MSB-SLN 对黑色素形成的抑制作用明显高于游离 MSB。MSB-SLN 对 L-3,4-二羟基苯丙氨酸(L-DOPA)自身氧化的抑制率(95.14±1.46%)高于 MSB 溶液(72.28±0.83%):本研究的观察结果表明,制备的 MSB-SLN 可用作 MSB 皮肤给药的潜在纳米载体,从而为治疗过度黑色素生成问题提供了创新选择。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Advanced pharmaceutical bulletin
Advanced pharmaceutical bulletin PHARMACOLOGY & PHARMACY-
CiteScore
6.80
自引率
2.80%
发文量
51
审稿时长
12 weeks
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