FORMULATION AND IN VITRO EVALUATION OF GASTRO RETENTIVE IN-SITU FLOATING GELS OF TELMISARTAN CUBOSOMES
Keywords:Cubosomes, Floating gel, Gastro-retentive
Objective: Telmisartan is a BCS class II antihypertensive drug used with poor solubility. The present work aim to formulate and evaluate a sustained release formulation of Telmisartan in form of cubosomes and gastro-retentive in situ floating gels of cubosomes.
Methods: The method used was a top-down approach employing GMO(glyceryl monooleate) as a lipid phase and Pluronic F127 as a stabilizer and distilled water as aqueous phase and the resultant cubosomes dispersion is subjected to various evaluation parameters. Floating gels are prepared similarly to that of dispersion by using various gelling agents. The formulated gels are subjected to various evaluations such as pH, In vitro drug release, and kinetic release.
Results: The compatibility studies by using infrared spectroscopy showed no interaction between the drug and excipients. Cubosomes formulation TELF8 (Telmisartan cubosomes formulation) containing 40% of GMO showed a maximum drug release of 82.75% within 20 h. This formulation exhibits an average particle size of 156.8 nm and a zeta potential of-30.06 mV. The concentration from the above optimized cubosome formulation is used for the preparation of floating gel using the various concentration of gelling agents(TELFNXGC)(Telmisartan gel formulation) and the sustained release was observed up to 20 h with a maximum drug release of about 91.58% and in vitro release kinetics exhibited sustained release follows First-order kinetics.
Conclusion: Cubosomes formulated with GMO can be used as gastro retentive sustained drug delivery vehicle and when form as a floating gel greater sustained release will be achieved.
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