DESIGN, DEVELOPMENT AND OPTIMIZATION OF GASTRO-RETENTIVE FLOATING IN-SITU GELS LOADED WITH CARVEDILOL MICROSPHERES USING RESPONSE SURFACE METHODOLOGY

Latha Kukati; Aisha Rahman; Aymen Fatima; Vyshak R Menon; Lakshmi SVVNSM

doi:10.2478/amma-2025-0011

Latha Kukati G.Pulla Reddy College of Pharmacy, Osmania University
Aisha Rahman G.Pulla Reddy College of Pharmacy, Osmania University https://orcid.org/0009-0000-9160-4050
Aymen Fatima https://orcid.org/0009-0006-3199-3895
Vyshak R Menon https://orcid.org/0009-0004-9374-5438
Lakshmi SVVNSM https://orcid.org/0000-0002-4159-1930

DOI: https://doi.org/10.2478/amma-2025-0011

Keywords: gastro-retentive, polymers, in-situ gel, viscosity

Abstract

Aim: The goal of the present study was to develop and optimize gastro-retentive floating in-situ gel containing microspheres (OMS) by Box-Behnken design.

Methods: Gellan gum, k-carrageenan were used as gelling polymers and calcium carbonate as complexing and gas generating agent. For optimization X₁ (concentration of k-carrageenan), X₂ (concentration of calcium carbonate) and X₃ (concentration of tri sodium citrate) were considered as factors and Y₁ (viscosity), Y₂ (floating lag time), Y₃ (drug release at 8 hrs) as responses. 17 formulations obtained from the design were prepared and evaluated for physical appearance, pH, viscosity, density, in-vitro drug release, in-vitro gelation capacity and floating behaviour.

Results and discussion: The optimized formulation (OIG) obtained from the design was milky white liquid with viscosity of 355.13 cP, showed buoyancy lag time of 104 seconds and remained buoyant for >24 hrs. 27.49 % drug was released from the in-situ gel at 8 hrs indicating controlled drug release. From the stability studies which were conducted for 4 weeks, it was determined that the OIG formulation was stable.

Conclusion: This study highlights the possibility of using microspheres in the gastro-retentive floating in-situ gel.