Nayak Kritika, Misra Manju
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research, Opposite AirForce Station, Palaj Basan Road, Village Palaj, Gandhinagar, Gujarat 382355, India.
ACS Omega. 2020 Apr 6;5(14):7928-7939. doi: 10.1021/acsomega.9b04244. eCollection 2020 Apr 14.
Present work investigates the possibility of a polyethyleneglycolylated (PEGylated) microemulsion (ME) to deliver drug to the posterior segment of eye. Triamcinolone acetonide (TA), a widely used drug in intraocular diseases, was selected as the model drug. Based on solubility and emulsification capacity, components of microemulsion were selected and optimum formulation was obtained using a pseudoternary phase diagram. The optimized ratio of Capmul MCM C8 (oil): AccononMC8-2 (surfactant): Transcutol (cosurfactant): deionized water was 5:35.5:4.5:55. This was further PEGylated using 1,2-distearoylphosphatylethanolamine-polyethyleneglycol 2000 (DSPE-PEG 2000). This PEGylated ME loaded with TA was characterized and evaluated , , and for topical ocular use. The developed PEGylated ME loaded with TA was homogenous, stable, and nonirritable to eye and had the ability to reach the posterior segment of eye on topical instillation.
目前的工作研究了聚乙二醇化（PEG化）微乳（ME）将药物递送至眼后段的可能性。选择眼内疾病中广泛使用的药物曲安奈德（TA）作为模型药物。基于溶解度和乳化能力，选择微乳的成分，并使用伪三元相图获得最佳配方。Capmul MCM C8（油）：AccononMC8 - 2（表面活性剂）：Transcutol（助表面活性剂）：去离子水的优化比例为5:35.5:4.5:55。使用1,2 - 二硬脂酰磷脂酰乙醇胺 - 聚乙二醇2000（DSPE - PEG 2000）对其进行进一步PEG化。对负载TA的这种PEG化微乳进行了表征，并评估了其用于眼部局部给药的情况。所制备的负载TA的PEG化微乳均匀、稳定且对眼睛无刺激性，并且在局部滴注时具有到达眼后段的能力。
