Institute of Ocular Pharmacology, School of Ophthalmology and Optometry, Wenzhou Medical College, 270 Xueyuan Road, Wenzhou, 325027 Zhejiang, People's Republic of China.
Acta Biomater. 2014 Jan;10(1):126-33. doi: 10.1016/j.actbio.2013.09.022. Epub 2013 Sep 27.
A subtenon injection of triamcinolone acetonide (TA) is a widely used treatment modality for various chorio-retinal diseases. Although it is less invasive than intravitreal injection, it can produce dose-associated ocular complications and has the disadvantages associated with systemic TA exposure. In this study we have developed and evaluated an episcleral film consisting of TA and poly-ε-caprolactone (PCL). The films were prepared by spraying a mixture of PCL in dichloromethane and TA in acetone. The films were produced as 6mm wide and 12 mm long episcleral plaques. X-ray diffraction demonstrated an even distribution of TA crystals in PCL, although the TA was less crystalized than a native TA control. Fourier transform infrared spectroscopy revealed effective integration of TA within the PCL matrix. An in vitro study of the release of TA from the episcleral plaques showed that TA release rate was only 40-50% that of the equivalent native TA control. An in vivo study demonstrated that the plaques were well tolerated in rabbit eyes with significantly less systemic TA exposure. The episcleral plaques provided therapeutic vitreous TA levels for 3 months, while TA levels in the vitreous were detectable for only 1 month following an equivalent dose by subtenon TA injection. The PCL-TA 30-60 episcleral plaque may be further developed as a better alternative treatment for many chronic vitreo-retinal diseases, providing longer and controlled release and fewer drug-associated complications than those associated with a conventional subtenon injection of TA.
曲安奈德(TA)经巩膜注射是一种广泛应用于多种脉络膜视网膜疾病的治疗方法。虽然它比玻璃体内注射的侵入性小,但仍可能产生与剂量相关的眼部并发症,并且具有与全身 TA 暴露相关的缺点。在这项研究中,我们开发并评估了一种由 TA 和聚己内酯(PCL)组成的巩膜膜片。这些膜片是通过将 PCL 在二氯甲烷中的混合物和 TA 在丙酮中的混合物喷涂制成的。膜片制成 6mm 宽和 12mm 长的巩膜贴片。X 射线衍射表明 TA 晶体在 PCL 中的分布均匀,尽管 TA 的结晶度低于天然 TA 对照。傅里叶变换红外光谱显示 TA 有效地整合到 PCL 基质中。体外研究表明,从巩膜贴片释放的 TA 释放率仅为等效天然 TA 对照的 40-50%。体内研究表明,在兔子眼中,贴片具有良好的耐受性,全身 TA 暴露明显减少。巩膜贴片提供了 3 个月的治疗性玻璃体内 TA 水平,而在接受相当于经巩膜 TA 注射的剂量后,玻璃体内的 TA 水平仅可检测到 1 个月。PCL-TA 30-60 巩膜贴片可能进一步开发为许多慢性玻璃体内视网膜疾病的更好替代治疗方法,与传统的经巩膜 TA 注射相比,提供更长时间和更受控的释放以及更少的药物相关并发症。