The barrier and defense mechanisms in the eye are a major challenge in developing drugs for glaucoma. Therefore, for better bioavailability of drugs, we need novel drug delivery systems to enable continuous ocular drug delivery. In-situ gel systems are systems in which a liquid formulation is converted into a thin layer of gel after being mounted in the eye. Due to its good adhesion properties, the goal of drug retention can be achieved.
In recent years, the development of in-situ gels has received considerable attention as an ocular delivery system for glaucoma drugs. Ace Therapeutics offers in-situ gel system development services for glaucoma drug delivery, including the formulation of various responsive polymers, control of gel formation, drug release rates and a range of other studies.
In-Situ Gel System
The in-situ gel is in the form of a solution before administration, but when exposed to the eye, the irritant is activated and the solution is converted into a gel. This transformation process is called phase change and is shown in the diagram below. The essence of such systems is to enhance therapeutic efficacy through drug release and contact time caused by sol-gel conversion and mucosal adhesion behavior.
Fig. 1 The transformation of solution to gel in an in-situ gel system. (Yadav K S, et al., 2019)
This phase change process is usually obtained using gels prepared from various types of polymers. These polymers are large molecules that undergo physicochemical changes in the environment, resulting in structural changes in the polymer. Common stimulus responses include physical, chemical or biological changes such as temperature, pressure, pH, ionic strength, electric field, magnetic field, etc. Thermally responsive, pH-responsive and ion-responsive in-situ eye gel systems are the most widely explored in-situ gel systems. They each have good gelling ability and can be combined to form multi-stimulus-responsive formulations to provide even better performance.
Services for In-Situ Gel System Development for Glaucoma
Our service aims to develop and optimize in-situ gel systems for the treatment of glaucoma and can provide one-stop development services for formulation, characterization, optimization and in vivo evaluation of in-situ gels.
Table 1. Our specific services for in-situ gel system development for glaucoma.
| Specific Items | Our Services |
|---|---|
| Formulation development | Gels are formulated using commonly used or high-performance polymer molecules including carbopols, polycarbophils, chitosan, gellan gum, alginate, alginate, pectin, etc. We are committed to developing excellent formulations that are non-toxic, histocompatible, non-immunogenic, and long-lasting and slow-release. |
| Characterization | We can provide formulation characterization services including appearance, pH, gel capacity, viscosity, spreadability, particle size, potential, drug packaging efficiency, SEM, TEM, in vitro drug release studies, in vivo pharmacodynamic studies, and other specific analytical testing elements. |
| Optimization | We can use the designed expert software to optimize the system formulation and select the best batch based on your needs. Design factors, derive equations, and predict optimization effects. Generate optimized formulations by setting minimum and maximum limits for each factor and response, and further characterize optimized batches. |
| Evaluation | We perform in vivo animal studies using animal models to observe the therapeutic effect of the new formulation after administration, mainly to assess the effect on glaucoma IOP reduction in relation to time. |
Development Advantages
- Advanced topical preparations
- Reproducibility
- Sustainable drug release
- Reliable safety performance
You can use this formulation for long-term topical administration to improve the effectiveness of glaucoma medications. The long precorneal residence time and ability to tolerate drug release of the in-situ gel system are utilized to achieve ease of administration and reduced frequency of drug delivery.
To maximize the potential of this approach to ocular drug delivery, you can contact us for further study and evaluation of the drug delivery system.
References
- Yadav K S, et al. Glaucoma: Current treatment and impact of advanced drug delivery systems. Life Sciences, 2019.
- Londhe V Y and Sharma S. Formulation, characterization, optimization and in-vivo evaluation of methazolamide liposomal in-situ gel for treating glaucoma. Journal of Drug Delivery Science and Technology, 2021.