Flurbiprofen-encapsulated microsphere laden into heat-triggered situ gel for ocular delivery

Year 2024, Volume: 54 Issue: 2, 108 - 121, 26.08.2024

Heybet Kerem Polat , Sedat Ünal

https://doi.org/10.26650/IstanbulJPharm.2024.1269717

Abstract

Background and Aims: This investigation aimed to enhance flurbiprofen’s (FB) pre-corneal residence period and ocular availability in the postoperative management of ocular inflammation.

Methods: The microsphere (MS) material was poly (lactic-co-glycolic acid) PLGA, and FB-laden microspheres were prepared using a single emulsification/solvent evaporation process, loaded onto thermosensitive in situ gels, and then characterised.

Results: The size of the microparticles was measured as 19.3±2.1 μm. Entrapment efficiency, zeta potential, and in vitro release; it was observed that the microspheres were released for six days. The optimum gelling capacity was obtained using 15% Poloxamer 407, 8% Poloxamer 188, and 1% HEC (viscosity 80-125 cp). Poloxamer 407 concentration was reduced, resulting in increased gelation temperature and duration. It was determined that the gelling temperature of the selected formulation was 35±0.1 °C, the pH was 6.9±0.02, and the viscosity at the gelling temperature was 11042±247 cP. The addition of hydroxyethyl cellulose increased the mucoadhesive strength. - in vitro release of FB from FB-PLGA MS followed the Korsmeyer-Peppas model , –, and the in situ gel preparation was found to be compatible with the Peppas-Sahlin model. In addition, MTT analysis of the ARPE-19 cell line revealed that the in situ gel formulation was biocompatible.

Conclusion: Flurbiprofen release was sustained, ocular availability was improved, and residence time was increased when flurbiprofen-loaded microspheres were incorporated into in situ gel bases.

Keywords

Flurbiprofen, Poloxamer Gel, Ocular Gel, PLGA Microsphere, Release Kinetics

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