Title:Probing the Synergistic Effect of Antibacterial Drug and Oleic Acid in
Lipid-based Gastroretentive Matrices by Melt Molding Method
Volume: 20
Issue: 1
Author(s): Amna Arshad, Ikram Ullah Khan, Moazam Ali, Fatima Arshad, Adeela Riaz, Zeeshan Ahmad Bhutta*Ambreen Ashar
Affiliation:
- Laboratory of Biochemistry and Immunology,
College of Veterinary Medicine, Chungbuk National University, Cheongju, Chungbuk, 28644, Republic of Korea
Keywords:
Gastroretentive, drug delivery system, clarithromycin, retention time, gelucire 48/16, Staphylococcus aureus, E.coli.
Abstract:
Introduction: Clarithromycin (antibiotic), due to its narrow absorption window in the gastrointestinal
tract, was taken as a model drug.
Materials and Methods: Focusing on the efficient drug delivery system, floating tablets that remain
buoyant over gastric fluid for 24 hrs were produced by adopting the melt mold method using beeswax,
gelucire, and oleic acid. To modulate the release pattern, a different concentration of 48/16 of beeswax
and gelucire was used.
Results: To evaluate and characterize the final product, several tests, including the percentage recovery,
in-vitro release studies, clarithromycin loading, scanning electron microscopy, differential scanning
calorimeter, X-ray powder diffractometry, fourier transform infrared spectroscopy, weight variation,
hardness, and friability, were carried out. Regarding the results, the encapsulation efficiency of the
floating tablets was 39.5% to 59%, having weight variation with and without gelucire as 48/16
0.09525±0.0032g, and 0.09527±0.00286g to 0.0957±0.00321g, respectively. Clarithromycin release
was controlled by using hydrophobic beeswax and hydrophilic gelucire 48/16. X-ray powder diffractometry,
differential scanning calorimeter, and fourier transform infrared spectroscopy confirmed the
absence of drug-polymer interaction, and exhibited amorphous and crystalline form of the drug after
encapsulation. Drug release kinetics was determined by applying different models, such as zero-order,
first-order model, Higuchi, and Korsemeyer-Pappas model. All formulations followed the Korsmeyer-
Peppas model at 1.2 pH.
Conclusion: Gastroretentive drug delivery systems were produced by using melt molding technique. In
vitro dissolution represents the sustained release of the drug from the formulation.
