Abdallah Marwa H, Shahien Mona M, Alshammari Alia, Ibrahim Somaia, Ahmed Enas Haridy, Atia Hanan Abdelmawgoud, Elariny Hemat A
Department of Pharmaceutics, College of Pharmacy, University of Ha'il, Ha'il 81442, Saudi Arabia.
Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt.
Gels. 2024 Mar 31;10(4):239. doi: 10.3390/gels10040239.
The present study explored the effectiveness of bile-salt-based nano-vesicular carriers (bilosomes) for delivering anti-psychotic medication, Sulpiride (Su), via the skin. A response surface methodology (RSM), using a 3 Box-Behnken design (BBD) in particular, was employed to develop and optimize drug-loaded bilosomal vesicles. The optimized bilosomes were assessed based on their vesicle size, entrapment efficiency (% EE), and the amount of Sulpiride released. The Sulpiride-loaded bilosomal gel was generated by incorporating the optimized Su-BLs into a hydroxypropyl methylcellulose polymer. The obtained gel was examined for its physical properties, ex vivo permeability, and in vivo pharmacokinetic performance. The optimum Su-BLs exhibited a vesicle size of 211.26 ± 10.84 nm, an encapsulation efficiency of 80.08 ± 1.88% and a drug loading capacity of 26.69 ± 0.63%. Furthermore, the use of bilosomal vesicles effectively prolonged the release of Su over a period of twelve hours. In addition, the bilosomal gel loaded with Su exhibited a three-fold increase in the rate at which Su transferred through the skin, in comparison to oral-free Sulpiride. The relative bioavailability of Su-BL gel was almost four times as high as that of the plain Su suspension and approximately two times as high as that of the Su gel. Overall, bilosomes could potentially serve as an effective technique for delivering drugs through the skin, specifically enhancing the anti-psychotic effects of Sulpiride by increasing its ability to penetrate the skin and its systemic bioavailability, with few adverse effects.
本研究探讨了基于胆盐的纳米囊泡载体（双分子层脂质体）经皮递送抗精神病药物舒必利（Su）的有效性。采用响应面法（RSM），特别是使用三因素Box-Behnken设计（BBD）来制备和优化载药双分子层脂质体。根据其囊泡大小、包封率（%EE）和舒必利释放量对优化后的双分子层脂质体进行评估。通过将优化后的舒必利-双分子层脂质体（Su-BLs）掺入羟丙基甲基纤维素聚合物中来制备载舒必利的双分子层凝胶。对所得凝胶的物理性质、离体渗透率和体内药代动力学性能进行了研究。最佳的Su-BLs囊泡大小为211.26±10.84 nm，包封效率为80.08±1.88%，载药量为26.69±0.63%。此外，双分子层脂质体的使用有效地延长了舒必利在12小时内的释放。此外，与游离口服舒必利相比，载舒必利的双分子层凝胶中舒必利透过皮肤的速率提高了两倍。Su-BL凝胶的相对生物利用度几乎是普通舒必利混悬液的四倍，约为舒必利凝胶的两倍。总体而言，双分子层脂质体可能是一种有效的经皮给药技术，特别是通过提高舒必利的皮肤穿透能力及其全身生物利用度来增强其抗精神病作用，且副作用较少。
