Jokubaite Monika, Marksa Mindaugas, Ramanauskiene Kristina
Department of Drug Chemistry, Faculty of Pharmacy, Lithuanian University of Health Sciences, Sukileliai Avenue 13, LT-50162 Kaunas, Lithuania.
Department of Analytical & Toxicological Chemistry, Faculty of Pharmacy, Lithuanian University of Health Sciences, Sukileliai Avenue 13, LT-50162 Kaunas, Lithuania.
Gels. 2024 Feb 21;10(3):161. doi: 10.3390/gels10030161.
In situ poloxamer-based gels are increasingly being explored as ocular drug delivery carriers to extend the release of active substances, thereby enhancing bioavailability. The objective of this study was to develop thermally stable in situ gels incorporating balsam poplar bud extract, propolis extract, and -coumaric acid solution and to evaluate the physicochemical parameters of these gelified eye drops. This research assessed the compatibility of poloxamer-based eye drops with active components, their physicochemical properties, stability post-sterilization and during storage, and the release profiles of the active compounds. Fifteen eye drop formulations were prepared and categorized into three groups based on active components. One of the active components was propolis extract. As an alternative to propolis, eye drops containing the plant precursor, balsam poplar bud extract, were developed. The third group's active component was -coumaric acid, a dominant phenolic acid in propolis and balsam poplar bud extracts. The study reported phenolic contents of 76.63 CAE mg/g for propolis and 83.25 CAE mg/g for balsam poplar bud aqueous extracts, with balsam poplar bud extracts showing higher SPF values (14.0) compared to propolis (12.7), while -coumaric acid solution exhibited the highest SPF values (25.5). All eye drops were transparent, with pH values meeting the requirements for ocular drops. Formulations containing 8-10% poloxamer 407 met the criteria for in situ gels. All formulations remained stable for 90 days. Conclusion: The study results indicate that the formulated gels possess suitable physicochemical properties, are resistant to applied autoclaving conditions, and exhibit an extended release of active compounds with an increase in poloxamer content.
基于泊洛沙姆的原位凝胶作为眼部药物递送载体正越来越多地被探索，以延长活性物质的释放，从而提高生物利用度。本研究的目的是开发包含香脂杨芽提取物、蜂胶提取物和对香豆酸溶液的热稳定原位凝胶，并评估这些凝胶化眼药水的物理化学参数。本研究评估了基于泊洛沙姆的眼药水与活性成分的相容性、它们的物理化学性质、灭菌后和储存期间的稳定性以及活性化合物的释放曲线。制备了15种眼药水配方，并根据活性成分分为三组。其中一种活性成分是蜂胶提取物。作为蜂胶的替代品，开发了含有植物前体香脂杨芽提取物的眼药水。第三组的活性成分是对香豆酸，它是蜂胶和香脂杨芽提取物中的主要酚酸。该研究报告称，蜂胶的酚含量为76.63 CAE mg/g，香脂杨芽水提取物的酚含量为83.25 CAE mg/g，香脂杨芽提取物的防晒系数（SPF）值（14.0）高于蜂胶（12.7），而对香豆酸溶液的SPF值最高（25.5）。所有眼药水均为透明，pH值符合眼药水的要求。含有8 - 10%泊洛沙姆407的配方符合原位凝胶的标准。所有配方在90天内保持稳定。结论：研究结果表明，所制备的凝胶具有合适的物理化学性质，能耐受高压灭菌条件，并且随着泊洛沙姆含量的增加，活性化合物呈现出延长释放的特性。
