Kurniawansyah Insan Sunan, Rusdiana Taofik, Sopyan Iyan, Desy Arya Insi Farisa, Wahab Habibah A, Nurzanah Dela
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang 45360, Indonesia.
Study Center of Dosage Form Development Faculty of Pharmacy, Universitas Padjadjaran, Sumedang 45360, Indonesia.
Gels. 2023 Aug 10;9(8):645. doi: 10.3390/gels9080645.
In recent years, in situ gel delivery systems have received a great deal of attention among pharmacists. The in situ gelation mechanism has several advantages over ointments, the most notable being the ability to provide regular and continuous drug delivery with no impact on visual clarity. Bioavailability, penetration, duration, and maximum medication efficacy are all improved by this mechanism. Our review systematically synthesizes and discusses comparisons between three types of in situ gelling system according to their phase change performance based on the physicochemical aspect from publications indexed in the Pubmed, ResearchGate, Scopus, Elsevier, and Google Scholar databases. An optimal temperature-sensitive in situ gelling solution must have a phase change temperature greater than ambient temperature (25 °C) to be able to be readily delivered to the eye; hence, it was fabricated at 35 °C, which is the precorneal temperature. In a pH-sensitive gelling system, a gel develops immediately when the bio-stimuli come into contact with it. An in situ gelling system with ionic strength-triggered medication can also perhaps be used in optical drug-delivery mechanisms. In studies about the release behavior of drugs from in situ gels, different models have been used such as zero-order kinetics, first-order kinetics, the Higuchi model, and the Korsmeyer-Peppas, Peppas-Sahlin and Weibull models. In conclusion, the optimum triggering approach for forming gels in situ is determined by a certain therapeutic delivery application combined with the physico-chemical qualities sought.
近年来，原位凝胶给药系统受到了药剂师的广泛关注。与软膏相比，原位凝胶化机制具有多个优点，其中最显著的是能够提供规律且持续的药物递送，同时不影响视觉清晰度。这种机制可提高生物利用度、渗透率、持续时间和最大药物疗效。我们的综述根据在PubMed、ResearchGate、Scopus、Elsevier和谷歌学术数据库中索引的出版物，从物理化学方面系统地综合并讨论了三种原位凝胶系统基于其相变性能的比较。一种最佳的温度敏感型原位凝胶溶液必须具有高于环境温度（25°C）的相变温度，以便能够轻松递送至眼部；因此，它是在角膜前温度35°C下制备的。在pH敏感型凝胶系统中，当生物刺激与之接触时会立即形成凝胶。一种具有离子强度触发药物释放功能的原位凝胶系统或许也可用于光学药物递送机制。在关于药物从原位凝胶中释放行为的研究中，使用了不同的模型，如零级动力学、一级动力学、Higuchi模型以及Korsmeyer-Peppas、Peppas-Sahlin和Weibull模型。总之，原位形成凝胶的最佳触发方法取决于特定的治疗递送应用以及所追求的物理化学性质。
