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An investigation on parameters affecting the optimization of testosterone enanthate loaded solid nanoparticles for enhanced transdermal delivery
Colloids and Surfaces A: Physicochemical and Engineering Aspects ( IF 5.2 ) Pub Date : 2020-02-01 , DOI: 10.1016/j.colsurfa.2020.124437
Mahgol Tajbakhsh , Majid Saeedi , Jafar Akbari , Katayoun Morteza-Semnani , Ali Nokhodchi , Akbar Hedayatizadeh-Omran

Abstract The current research aimed to formulate and optimize testosterone enanthate-loaded solid lipid nanoparticles (TE-SLNs) for the enhanced TE transdermal delivery. To this end, TE-SLNs were prepared using ultrasound-assisted emulsification technique and their properties and permeation across the excised rat skin were investigated. Evaluation of lipid type as well as the ratio and contents of surfactant mixtures resulted in a polydispersity index, particle size, drug loading, drug encapsulation efficiency, and zeta potential of 0.317 ± 0.006, 87.66 ± 1.52 nm, 21.61 ± 0.45 %, 44.71 ± 1.14 % and -23.06 ± 0.50 mV, respectively. ATR-FTIR spectra of TE-SLNs exhibited the prominent functional groups of TE in the formulations, indicating a well-dispersion of TE in the lipid matrix without any chemical interaction with other components of the formulation. Differential scanning calorimetry (DSC) demonstrated that TE in SLNs is in an amorphous state. Transmission electron microscopy (TEM) confirmed that the prepared TE-SLNs have a stable size and maintained their sphericity. The results of TE permeation across the excised rat skin from SLNs displayed cumulative amounts of 110.61 ± 17.7 μg/cm2, which is 3.2 fold improvement in TE permeation in comparison with the testosterone enanthate solution in oleic acid (p

中文翻译:

影响优化载有庚酸睾酮的固体纳米颗粒以增强透皮给药的参数的研究

摘要 目前的研究旨在配制和优化装载庚酸睾酮的固体脂质纳米颗粒 (TE-SLN),以增强 TE 透皮给药。为此,使用超声辅助乳化技术制备了 TE-SLN,并研究了它们的特性和在离体大鼠皮肤上的渗透。脂质类型以及表面活性剂混合物的比例和含量的评估导致多分散指数、粒径、载药量、药物包封效率和 zeta 电位为 0.317 ± 0.006、87.66 ± 1.52 nm、21.61 ± 0.45 %、44.71 ±分别为 1.14 % 和 -23.06 ± 0.50 mV。TE-SLN 的 ATR-FTIR 光谱显示出配方中 TE 的显着官能团,表明 TE 在脂质基质中分散良好,与制剂的其他成分没有任何化学相互作用。差示扫描量热法 (DSC) 表明 SLN 中的 TE 处于无定形状态。透射电子显微镜 (TEM) 证实制备的 TE-SLN 具有稳定的尺寸并保持其球形度。TE 渗透从 SLNs 切除的大鼠皮肤的结果显示累积量为 110.61 ± 17.7 μg/cm2,与油酸中庚酸睾酮溶液相比,TE 渗透率提高了 3.2 倍(p
更新日期:2020-02-01
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