Abstract

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.

Highlights

  • The word cubosomes was termed by Larson, which reflects the cubic molecular crystallography similar to that of liposomes

  • Cubosomes are a bicontinuous cubic liquid phase that is surrounded by two separate water regions that are distinct by surfactantcontrolled bilayer

  • They can be formulated by using glycerol monooleate (GMO) as the amphiphilic lipids and Pluronic as a stabilizer which can self-form into cubosomes in water [4]

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Summary

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 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
INTRODUCTION
MATERIALS AND METHODS
Evaluation of cubosomes dispersion
Evaluation of floating gel
RESULTS AND DISCUSSION
Evaluation of telmisartan loaded cubosomes
Evaluation floating gel
Summary and conclusion
Full Text
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