Section of Pharmacology, Department of Biomedical and Biotechnological Sciences, School of Medicine, University of Catania, 95123 Catania, Italy.
Center for Research in Ocular Pharmacology-CERFO University of Catania, 95123 Catania, Italy.
Int J Mol Sci. 2017 Sep 30;18(10):2076. doi: 10.3390/ijms18102076.
Dysregulation of the transforming growth factor-β1 (TGF-β1)/selected small mother against decapentaplegic (SMAD) pathway can be implicated in development of age-related macular degeneration (AMD), and the delivery of TGF-β1 could be beneficial for AMD. We developed a new ophthalmic formulation of TGF-β1 assessing the ocular pharmacokinetic profile of TGF-β1 in the rabbit eye. Small unilamellar vesicles (SUV) loaded with TGF-β1 were complemented with Annexin V and Ca, and the vitreous bioavailability of TGF-β1 was assessed after topical ocular administration by a commercial ELISA kit. We detected high levels of TGF-β1 (C 114.7 ± 12.40 pg/mL) in the vitreous after 60 min (T) from the topical application of the liposomal suspension. Ocular tolerability was also assessed by a modified Draize's test. The new formulation was well tolerated. In conclusion, we demonstrated that the novel formulation was able to deliver remarkable levels of TGF-β1 into the back of the eye after topical administration. Indeed, this TGF-β1 delivery system may be useful in clinical practice to manage ophthalmic conditions such as age-related macular degeneration, skipping invasive intraocular injections.
转化生长因子-β1（TGF-β1）/选择的小母体对抗颅面发育不全（SMAD）途径的失调可能与年龄相关性黄斑变性（AMD）的发生有关，而 TGF-β1 的传递可能对 AMD 有益。我们开发了一种新的 TGF-β1 眼科制剂，评估了 TGF-β1 在兔眼的眼内药代动力学特征。装载有 TGF-β1 的小单层囊泡（SUV）用 Annexin V 和 Ca 补充，并通过商业 ELISA 试剂盒评估 TGF-β1 在局部眼用后玻璃体内的生物利用度。我们在局部应用脂质体混悬液 60 分钟（T）后检测到玻璃体内 TGF-β1 水平很高（C 114.7 ± 12.40 pg/mL）。还通过改良的 Draize 试验评估了眼部耐受性。新制剂具有良好的耐受性。总之，我们证明了这种新的制剂能够在局部给药后将显著水平的 TGF-β1 递送到眼睛的后部。实际上，这种 TGF-β1 传递系统可能在临床实践中有用，可用于治疗眼部疾病，如年龄相关性黄斑变性，避免侵入性眼内注射。
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