Gastroretentive Delivery System of Oil Entrapped Floating Alginate Beads for Improving Oral Bioavailability of Telmisartan

Dilli Bhai, G (2021) Gastroretentive Delivery System of Oil Entrapped Floating Alginate Beads for Improving Oral Bioavailability of Telmisartan. Masters thesis, C. L. Baid Metha College of Pharmacy, Chennai.


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The present study aims at developing and Optimizing Telmisartan loaded Oil entrapped Floating alginate beads to prolong the residence time of drug in the Gastric region and thereby improving Solubility and Bioavailability of Telmisartan. The Multiple unit Floating beads of Telmisartan were successfully developed using the hydrophilic polymer (sodium alginate) by crosslinking with calcium chloride using Emulsion Gelation technique. Sesame oil was entrapped within the beads to enhance the floating behaviour. The formulation increased the gastric retention without gastric irritation and thereby improved patient compliance. The Formulation is optimized using Response surface methodology by Central Composite Design. Telmisartan loaded oil entrapped beads were formulated with various concentrations of sodium alginate, Calcium chloride and percent of oil and their effect on responses Entrapment efficiency, In-vitro Buoyancy and Drug release at Q61. were studied. From the desirability function (1.00), the amount of sodium alginate, Calcium chloride and Sesame oil percent was optimized with values 6.672 %, 9.090% and 7.015% respectively and the results were found to fit the model. High linearity was observed between the predicted and actual values of the response variables. The results of drug release kinetics portrays that the optimized formulation is fitted with all the models and the drug release is best fitted with Higuchi (r2 < 0.9836) and Peppas model with the n value of 0.896 indicating that the drug release follows Super case II transport. The drug release mechanism follows swelling, erosion and diffusion. Alginate beads can control, improve and prolong the systemic absorption of telmisartan through their gastro-retentive properties. From the results of In-vivo studies, Anti-Hypertensive activity of this formulation is sustained and significantly improved the therapeutic efficacy of Telmisartan. Further it can be concluded that, this novel delivery system of Telmisartan loaded oil entrapped beads can be a promising tool for improving the solubility, hence the oral bioavailability and therapeutic efficacy of the drug leads to patient compliance. Further the in-vivo studies confirms the prolonged Anti-Hypertensive efficacy of the formulation in animal models.

Item Type: Thesis (Masters)
Additional Information: 261910005
Uncontrolled Keywords: Gastroretentive Delivery System, Oil Entrapped Floating Alginate Beads, Oral Bioavailability, Telmisartan.
Subjects: PHARMACY > Pharmaceutics
Depositing User: Subramani R
Date Deposited: 01 Nov 2022 02:32
Last Modified: 01 Nov 2022 02:45

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