Zafar Ameeduzzafar, Imam Syed Sarim, Alruwaili Nabil K, Yasir Mohd, Alsaidan Omar Awad, Alshehri Sultan, Ghoneim Mohammed M, Khalid Mohammad, Alquraini Ali, Alharthi Salman S
Department of Pharmaceutics, College of Pharmacy, Jouf University, Sakaka 72341, Al-Jouf, Saudi Arabia.
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
Gels. 2022 Feb 18;8(2):133. doi: 10.3390/gels8020133.
The present research work was designed to prepare butenafine (BN)-loaded bilosomes (BSs) by the thin-film hydration method. BN is a sparingly water-soluble drug having low permeability and bioavailability. BSs are lipid-based nanovesicles used to entrap water-insoluble drugs for enhanced permeation across the skin. BSs were prepared by the thin-film hydration method and optimized by the Box-Behnken design (BBD) using lipid (A), span 60 (B), and sodium deoxycholate (C) as independent variables. The selected formulation (BN-BSo) was converted into the gel using Carbopol 940 as a gelling agent. The prepared optimized gel (BN-BS-og) was further evaluated for the gel characterization, drug release, drug permeation, irritation, and anti-fungal study. The optimized bilosomes (BN-BSo) showed a mean vesicle size of 215 ± 6.5 nm and an entrapment efficiency of 89.2 ± 1.5%. The DSC study showed that BN was completely encapsulated in the BS lipid matrix. BN-BSog showed good viscosity, consistency, spreadability, and pH. A significantly ( < 0.05) high release (81.09 ± 4.01%) was achieved from BN-BSo compared to BN-BSog (65.85 ± 4.87%) and pure BN (17.54 ± 1.37 %). The permeation study results revealed that BN-BSo, BN-BSog, and pure BN exhibited 56.2 ± 2.7%, 39.2 ± 2.9%, and 16.6 ± 2.3%. The enhancement ratio of permeation flux was found to be 1.4-fold and 3.4-fold for the BN-BS-og and pure BN dispersion. The HET-CAM study showed that BN-BSog was found to be nonirritant as the score was found within the limit. The antifungal study revealed a significant ( < 0.05) enhanced antifungal activity against and . The findings of the study revealed that BS is an important drug delivery system for transdermal delivery.
本研究旨在通过薄膜水化法制备载有布替萘芬（BN）的双分子层脂质体（BSs）。BN是一种水溶性差、渗透性和生物利用度低的药物。BSs是基于脂质的纳米囊泡，用于包裹水不溶性药物以增强其经皮渗透。采用薄膜水化法制备BSs，并以脂质（A）、司盘60（B）和脱氧胆酸钠（C）作为自变量，通过Box-Behnken设计（BBD）进行优化。选用的制剂（BN-BSo）以卡波姆940作为胶凝剂制成凝胶。对制备的优化凝胶（BN-BS-og）进行凝胶特性、药物释放、药物渗透、刺激性和抗真菌研究等进一步评估。优化后的双分子层脂质体（BN-BSo）平均囊泡大小为215±6.5nm，包封率为89.2±1.5%。差示扫描量热法（DSC）研究表明，BN完全包裹在BS脂质基质中。BN-BSog表现出良好的粘度、稠度、铺展性和pH值。与BN-BSog（65.85±4.87%）和纯BN（17.54±1.37%）相比，BN-BSo的释放率显著较高（<0.05），达到81.09±4.01%。渗透研究结果显示，BN-BSo、BN-BSog和纯BN的渗透率分别为56.2±2.7%、39.2±2.9%和16.6±2.3%。BN-BS-og和纯BN分散体的渗透通量增强率分别为1.4倍和3.4倍。鸡胚绒毛尿囊膜（HET-CAM）研究表明，BN-BSog得分在限值范围内，无刺激性。抗真菌研究显示，其对 和 的抗真菌活性显著增强（<0.05）。该研究结果表明，BS是一种重要的经皮给药系统。
