In situ gelling systems based on Pluronic F127/Pluronic F68 formulations for ocular drug delivery

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• 作者：Kosai Al Khateb^a ; Elvira K. Ozhmukhametova^b ; Marat N. Mussin^b ; Serzhan K. Seilkhanov^b ; Tolebai K. Rakhypbekov^b ; Wing Man Lau^a ; ^{w.lau@reading.ac.uk" class="auth_mail" title="E-mail the corresponding author} ; Vitaliy V. Khutoryanskiy^a ; ^{v.khutoryanskiy@reading.ac.uk" class="auth_mail" title="E-mail the corresponding author}
• 关键词：In situ gelling systems ; Ocular drug delivery ; Pluronics ; Gelation ; Mucoadhesion
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：11 April 2016
• 年：2016
• 卷：502
• 期：1-2
• 页码：70-79
• 全文大小：2228 K

文摘

This study evaluated the use of Pluronic F127 and Pluronic F68 as excipients for formulating in situ gelling systems for ocular drug delivery. Thermal transitions have been studied in aqueous solutions of Pluronic F127, Pluronic F68 as well as their binary mixtures using differential scanning calorimetry, rheological measurements, and dynamic light scattering. It was established that the formation of transparent gels at physiologically relevant temperatures is observed only in the case of 20 wt% of Pluronic F127. The addition of Pluronic F68 to Pluronic F127 solutions increases the gelation temperature of binary formulation to above physiological range of temperatures. The biocompatibility evaluation of these formulations using slug mucosa irritation assay and bovine corneal erosion studies revealed that these polymers and their combinations do not cause significant irritation. In vitro drug retention study on glass surfaces and freshly excised bovine cornea showed superior performance of 20 wt% Pluronic F127 compared to other formulations. In addition, in vivo studies in rabbits demonstrated better retention performance of 20 wt% Pluronic F127 compared to Pluronic F68. These results confirmed that 20 wt% Pluronic F127 offers an attractive ocular formulation that can form a transparent gel in situ under physiological conditions with minimal irritation.