Kaul Shreya, Nagaich Upendra, Verma Navneet
Department of Pharmaceutics, Faculty of Pharmacy, IFTM University, Moradabad, Uttar Pradesh, India.
Department of Pharmaceutics, Amity Institute of Pharmacy, Amity University, Noida, Uttar Pradesh, India.
J Adv Pharm Technol Res. 2021 Oct-Dec;12(4):356-361. doi: 10.4103/japtr.japtr_188_21. Epub 2021 Oct 20.
Tobramycin remains the anchor drug for bacterial keratitis treatment and management; however, unlike other aminoglycosides, it does not pass through the gastrointestinal tract. The aim of the current investigation was to formulate tobramycin-loaded nanostructured liquid crystalline particles as an ophthalmic drug delivery system to ameliorate its preocular residence duration and ophthalmic bioavailability. Tobramycin cubosomes were fabricated by liquid-lipid monoolein, water, and poloxamer 407 as a stabilizer. Corneal penetration studies exhibited that the apparent permeation coefficient of tobramycin cubosomes was nearly 3.6-fold greater than marketed tobramycin eye drops. Ocular analysis performed in rabbits' eyes manifested that the intensity of bacterial keratitis was reduced on day 3, and on day 5, the manifestations were considerably mitigated with tobramycin cubosomes as compared to marked eye drops. Pharmacokinetic study of rabbit aqueous humor demonstrated that the area under curve and the peak concentration of optimized cubosomes were 3.1-fold and 3.3-fold, respectively, which was significantly higher than marketed eye drops. Moreover, histopathological studies illustrated the existence of normal ocular structures, thus indicating that there was no damage to the corneal epithelium or stromal layer. Consequently, the results acquired demonstrated that tobramycin-loaded cubosomal formulation could be a propitious lipid-based nanodelivery system that would enhance retention time and corneal permeability contrast to commercial eye drops.
妥布霉素仍然是细菌性角膜炎治疗和管理的主要药物；然而，与其他氨基糖苷类药物不同，它不能通过胃肠道。本研究的目的是制备载有妥布霉素的纳米结构液晶颗粒作为眼科药物递送系统，以改善其在眼表的停留时间和眼部生物利用度。以液体脂质单油酸甘油酯、水和泊洛沙姆407作为稳定剂制备妥布霉素立方液晶纳米粒。角膜渗透研究表明，妥布霉素立方液晶纳米粒的表观渗透系数比市售妥布霉素滴眼液高近3.6倍。在兔眼中进行的眼部分析表明，在第3天细菌性角膜炎的强度降低，在第5天，与市售滴眼液相比，妥布霉素立方液晶纳米粒使症状明显减轻。兔房水的药代动力学研究表明，优化后的立方液晶纳米粒的曲线下面积和峰浓度分别是市售滴眼液的3.1倍和3.3倍，显著高于市售滴眼液。此外，组织病理学研究表明存在正常的眼部结构，因此表明角膜上皮或基质层没有损伤。因此，所获得的结果表明，载有妥布霉素的立方液晶纳米粒制剂可能是一种有利的基于脂质的纳米递送系统，与市售滴眼液相比，它可以提高药物的停留时间和角膜通透性。
