Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka, India.
AAPS PharmSciTech. 2023 Nov 21;24(8):238. doi: 10.1208/s12249-023-02696-4.
Vesicular drug delivery systems have revolutionized the pharmaceutical field, offering a promising path for achieving targeted and sustained drug delivery. The oral, transdermal, and ocular routes of administration offer optimal ease in attaining desired therapeutic outcomes. However, conventional treatment strategies are all plagued with several challenges, such as poor skin permeability, ocular barriers, and gastrointestinal (GIT) degradation leading to vesicular disruption with the release of the encapsulated drug before reaching the targeted site of action. In recent years, bilosomes-stabilized nanovesicles containing bile salts have received considerable attention due to their versatility and adaptability for diverse applications. These bilayered vesicles enhance the solubility of lipophilic drugs and improve formulation stability in the gastrointestinal tract. They exhibit ultra-deformable properties, improving stratum corneum permeability, making them ideal candidates for oral and transdermal drug delivery. In addition, bilosomes find utility in topical drug delivery, making them applicable for ocular administration. Over the past decade, extensive research has highlighted bilosomes' potential as superior vesicular carriers surpassing liposomes and niosomes. Advances in this field have led to the development of modified bilosomes, such as probilosomes and surface-modified bilosomes, further enhancing their capabilities and therapeutic potential. Thus, the present review provides a comprehensive summary of bilosomes, modified bilosomes, surface modifications with their mechanism of action, formulation components, preparation methods, patents, and a wide array of recent pharmaceutical applications in oral, transdermal, and ocular drug delivery. The enhanced properties of bilosomes offer promising prospects for targeted and effective drug delivery, providing potential solutions for addressing various therapeutic challenges.
囊泡给药系统彻底改变了制药领域,为实现靶向和持续药物输送提供了有前途的途径。口服、透皮和眼部给药途径为实现所需的治疗效果提供了最佳的简便性。然而,传统的治疗策略都存在几个挑战,例如皮肤渗透性差、眼部屏障和胃肠道 (GIT) 降解,导致囊泡在到达靶向作用部位之前破裂,释放包裹的药物。近年来,由于其多功能性和对各种应用的适应性,含有胆汁盐的双分子层囊泡(bilosomes)稳定的纳米囊泡受到了相当大的关注。这些双层囊泡提高了亲脂性药物的溶解度,并提高了在胃肠道中的制剂稳定性。它们具有超可变形的特性,可改善角质层的通透性,使其成为口服和透皮药物输送的理想候选物。此外,bilosomes 在局部药物输送中也有应用,使其适用于眼部给药。在过去的十年中,广泛的研究强调了 bilosomes 作为优于脂质体和非离子囊泡的卓越囊泡载体的潜力。该领域的进展导致了改良的 bilosomes 的发展,如 probilosomes 和表面修饰的 bilosomes,进一步增强了它们的能力和治疗潜力。因此,本综述全面总结了 bilosomes、改良的 bilosomes、表面修饰及其作用机制、制剂成分、制备方法、专利以及在口服、透皮和眼部药物输送方面的广泛的最新药物应用。bilosomes 的增强特性为靶向和有效药物输送提供了有前途的前景,为解决各种治疗挑战提供了潜在的解决方案。