Kasetvatin Chawankorn, Rujivipat Soravoot, Tiyaboonchai Waree
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok 65000, Thailand.
Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok 65000, Thailand; The Center of Excellence for Innovation in Chemistry (PERCH-CIC), Commission on High Education, Ministry of Education, Thailand; The Center of Excellence in Medical Biotechnology, Naresuan University, Phitsanulok 65000, Thailand.
Colloids Surf B Biointerfaces. 2015 Nov 1;135:458-464. doi: 10.1016/j.colsurfb.2015.07.078. Epub 2015 Jul 31.
The synergistic approach of using elastic liposomes (ELs) and low frequency ultrasound (LFU) was developed to enhance transepidermal delivery of hydrophilic macromolecules, hyaluronic acid (HA).
HA loaded ELs were prepared with varying cholesterol contents by reverse phase evaporation technique. Their mean sizes were evaluated using dynamic light scattering. Entrapment efficacy (%EE) was determined by UV-vis spectrophotometry. In vitro permeation studies using porcine ear epidermis were investigated. In addition, skin barrier disruption was assessed by transepidermal water loss and histology.
The HA loaded ELs showed mostly elliptical shaped with a mean size of ∼ 700 nm and a zeta potential of ∼-40 mV. Up to 77% drug entrapment efficiency was achieved. As ELs cholesterol content decreased, vesicle size, elasticity of liposomes and HA permeation profile increased. The in vitro permeation studies demonstrated that HA solution cannot permeate through the porcine epidermis. The combination of ELs/LFU showed greater HA permeation than ELs and HA/LFU, 2.1 times and 6.4 times, respectively. Increased LFU exposure times augmented HA permeation, but greater skin disruption was observed. Nevertheless, no skin damage was observed at the optimized 1 min exposure time. This ELs/LFU combination provides an efficacious protocol for transcutaneous drug delivery.
开发了使用弹性脂质体（ELs）和低频超声（LFU）的协同方法，以增强亲水性大分子透明质酸（HA）的经皮递送。
通过反相蒸发技术制备了具有不同胆固醇含量的载HA的ELs。使用动态光散射评估其平均尺寸。通过紫外可见分光光度法测定包封率（%EE）。研究了使用猪耳表皮的体外渗透研究。此外，通过经皮水分流失和组织学评估皮肤屏障破坏情况。
载HA的ELs大多呈椭圆形，平均尺寸约为700nm，ζ电位约为-40mV。实现了高达77%的药物包封效率。随着ELs胆固醇含量的降低，囊泡尺寸、脂质体弹性和HA渗透曲线增加。体外渗透研究表明，HA溶液不能透过猪表皮。ELs/LFU组合显示出比ELs和HA/LFU更大的HA渗透，分别为2.1倍和6.4倍。增加LFU暴露时间可增强HA渗透，但观察到更大的皮肤破坏。然而，在优化的1分钟暴露时间下未观察到皮肤损伤。这种ELs/LFU组合为经皮给药提供了一种有效的方案。
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