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Published on: August 22, 2017
Levofloxacin Hemihydrate-Adorned Floating Drug Delivery System to Ameliorate H. Pylori Infection: Formulation
Sheikh Muhammad Mishkat Ullah1, Sheikh Abdur Rashid1, Nauman Rahim Khan2
1Gomal Center of Pharmaceutical Sciences, Faculty of Pharmacy, Gomal University, Dera Ismail Khan, 29050, KPK, Pakistan.
Objective:
This study focused on developing and characterizing Levofloxacin hemihydrate floating bioadhesive tablets for the treatment of Helicobacter pylori (H. pylori) infection.
Significance:
This study demonstrates a promising gastroretentive and bioadhesive drug delivery system that enhances the effectiveness of levofloxacin in the stomach for targeted H. pylori infection treatment.
Methods:
Floating bio-adhesive tablets were prepared by direct compression using sodium bicarbonate (NaHCO3) as a gas-generating agent and HPMC K4M/chitosan and carbopol 940P/sodium alginate as release retardants and bio-adhesives. Pre-formulation flow properties were evaluated. Tablets were characterized by physicochemical parameters, bioadhesion on goat stomach mucosa, and FTIR, which confirmed drug-excipient compatibility.
Results:
The optimized formulation (FT7) showed a buoyancy lag time of 62.59 ± 6.83 second, a total floating time of more than 12h, a swelling index of 81.89%, and a bioadhesion strength of 28.19 ± 5.12g. The formulation remained physically stable after three months of storage at 40 °C and 75% RH. Drug release followed a non-Fickian diffusion mechanism (n = 0.514) and best fit the Korsmeyer-Peppas model (R2 = 0.989). In vitro and in vivo mucoadhesion studies demonstrated good retention of the tablet in the rabbit stomach for over 12 h. In-vivo barium sulfate X-ray imaging further confirmed that the tablet remained floating in the stomach 12 hours after oral administration.
Conclusion:
A matrix-floating bio-adhesive tablet containing levofloxacin hemihydrate was successfully developed to effectively eliminate H. pylori infection.
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