Mon, 20 Nov 2017

Design and Fabrication of Tramadol Hydrochloride Microspheres for Colon Targeted Drug Delivery System

Amitha Shetty1*, Shruti Prabhu1, Sarvesh Parsekar1, Mohd Azharuddin1, A R Shabaraya1

1. Department of Pharmaceutics, Srinivas College of Pharmacy, Valachil, Mangalore-574143, Karnataka, India.


ABSTRACT

Colon targeted drug delivery system is capable of protecting the drug in route to the colon i.e. drug gets released and absorbed once it reaches the colon. A multiparticulate system combining pH sensitive property and biodegradability has been investigated to prepare and evaluate Eudragit S-100 coated Sodium alginate microspheres for colon targeting of Tramadol Hydrochloride. Uncoated Tramadol Hydrochloride microspheres were prepared by ionotropic gelation technique using different ratios of Tramadol Hydrochloride and Sodium alginate. Coated Tramadol Hydrochloride microspheres were prepared by coacervation phase separation technique using different ratios of uncoated Tramadol Hydrochloride and Eudragit S-100/ Eudragit L-100. Uncoated and coated Tramadol Hydrochloride microspheres were evaluated for percentage yield, particle size, surface morphology, flow properties, drug content and entrapment efficiency and were found to be within the acceptable range. The uncoated microspheres sustained the release upto 8 hrs whereas coated microspheres sustained the release upto 12 hrs in a pH progression medium mimicking the condition of GIT. The drug release from MC4 formulation coated with Eudragit S-100 (1:4) showed desired rate as there was no drug release observed upto 4-5 hrs, while in colonic fluid controlled drug release was observed releasing about 69.66 % after 12 hrs. The release kinetics followed Peppas showing Super Case II transport. Stability studies suggested formulations were stable. It is concluded from the present investigation that Eudragit S-100 coated Sodium alginate microspheres are promising controlled release carriers for colon targeted delivery of Tramadol Hydrochloride.

Keywords: Colon targeted drug delivery system, Tramadol Hydrochloride, Sodium alginate, Eudragit S-100, Eudragit L-100.


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