Login Register Cart 0
Generic placeholder image

Current Drug Delivery

Editor-in-Chief

ISSN (Print): 1567-2018
ISSN (Online): 1875-5704

Back
Journal Home About Journal Editorial Board Journal Insight Current Issue Volumes/Issues
Subscribe
Research Article

Probing the Synergistic Effect of Antibacterial Drug and Oleic Acid in Lipid-based Gastroretentive Matrices by Melt Molding Method

Author(s): Amna Arshad, Ikram Ullah Khan, Moazam Ali, Fatima Arshad, Adeela Riaz, Zeeshan Ahmad Bhutta* and Ambreen Ashar

Volume 20, Issue 1, 2023

Published on: 14 June, 2022

Page: [89 - 97] Pages: 9

DOI: 10.2174/1567201819666220412112104

Price: $65

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.

Keywords: Gastroretentive, drug delivery system, clarithromycin, retention time, gelucire 48/16, Staphylococcus aureus, E.coli.

« Previous
Graphical Abstract

[1]
Pinto, J.F. Site-specific drug delivery systems within the gastro-intestinal tract: from the mouth to the colon. Int. J. Pharm., 2010, 395(1-2), 44-52.
[http://dx.doi.org/10.1016/j.ijpharm.2010.05.003] [PMID: 20546856]
[2]
Rouge, N. Drug absorption sites in the gastrointestinal tract and dosage forms for site-specific delivery. Int. J. Pharm., 1996, 117-139.
[http://dx.doi.org/10.1016/0378-5173(96)85200-8]
[3]
Kagan, L.; Hoffman, A. Selection of drug candidates for gastroretentive dosage forms: pharmacokinetics following continuous intragastric mode of administration in a rat model. Eur. J. Pharm. Biopharm., 2008, 69(1), 238-246.
[http://dx.doi.org/10.1016/j.ejpb.2007.10.019] [PMID: 18068342]
[4]
Boldhane, S.P.; Kuchekar, B.S. Development and optimization of metoprolol succinate gastroretentive drug delivery system. Acta Pharm., 2010, 60(4), 415-425.
[http://dx.doi.org/10.2478/v10007-010-0031-x] [PMID: 21169134]
[5]
Nayak, AK Gastroretentive drug delivery technologies: Current approaches and future potential. J. Pharm. Educ. Res., 2010, 1(2), 1-12.
[6]
Mandal, U.K. Senjoti, Gastro-retentive drug delivery systems and their in vivo success: A recent update. Asian J. Pharm. Sci., 2016, 11(5), 575-584.
[7]
Surana, AS An overview on various approaches to oral controlled drug delivery system via gastroretention. Int. J. Pharm. Sci. Rev. Res., 2010, 68-72.
[8]
Pawar, H.A.; Lalitha, K.G.; Ruckmani, K. Alginate beads of Captopril using galactomannan containing Senna tora gum, guar gum and locust bean gum. Int. J. Biol. Macromol., 2015, 76, 119-131.
[http://dx.doi.org/10.1016/j.ijbiomac.2015.02.026] [PMID: 25720832]
[9]
Patel, H. Matrix type drug delivery system: A review. J. Pharm. Sci., 2011, 1(3), 143-151.
[10]
Panigrahi, K.C. Gelucire: A versatile polymer for modified release drug delivery system. Future J. Pharm. Sci., 2018, 102-108.
[11]
Becker, K.; Salar-Behzadi, S.; Zimmer, A. Solvent-free melting techniques for the preparation of lipid-based solid oral formulations. Pharm. Res., 2015, 32(5), 1519-1545.
[http://dx.doi.org/10.1007/s11095-015-1661-y] [PMID: 25788447]
[12]
Dilika, F.; Bremner, P.D.; Meyer, J.J. Antibacterial activity of linoleic and oleic acids isolated from Helichrysum pedunculatum: A plant used during circumcision rites. Fitoterapia, 2000, 71(4), 450-452.
[http://dx.doi.org/10.1016/S0367-326X(00)00150-7] [PMID: 10925024]
[13]
Jannin, V. Techniques for solid and semi-solid formulations in bioavailability enhancement with lipids. Adv. Drug Deliv. Rev., 2008, 734-746.
[http://dx.doi.org/10.1016/j.addr.2007.09.006] [PMID: 18045728]
[14]
Fratini, F.; Cilia, G.; Turchi, B.; Felicioli, A. Beeswax: A minireview of its antimicrobial activity and its application in medicine. Asian Pac. J. Trop. Med., 2016, 9(9), 839-843.
[http://dx.doi.org/10.1016/j.apjtm.2016.07.003] [PMID: 27633295]
[15]
Bogdanov, S. Beeswax: Quality issues today. Bee World, 2004, 85, 46-50.
[http://dx.doi.org/10.1080/0005772X.2004.11099623]
[16]
Ahmed Abdelbary, A.; Elsayed, I.; Hassen Elshafeey, A. Design and development of novel lipid based gastroretentive delivery system: Response surface analysis, in vivo imaging and pharmacokinetic study. Drug Deliv., 2015, 22(1), 37-49.
[http://dx.doi.org/10.3109/10717544.2013.868960] [PMID: 24350634]
[17]
Gao, P.; Nie, X.; Zou, M.; Shi, Y.; Cheng, G. Recent advances in materials for extended-release antibiotic delivery system. J. Antibiot. (Tokyo), 2011, 64(9), 625-634.
[http://dx.doi.org/10.1038/ja.2011.58] [PMID: 21811264]
[18]
Malladi, M. Formulation development and evaluation of a novel bidependent clarithromycin gastroretentive drug delivery system using Box-Behnken design. J. Drug Deliv. Sci. Technol., 2016, 134-145.
[http://dx.doi.org/10.1016/j.jddst.2016.06.003]
[19]
Balanč, B.; Kalušević, A.; Drvenica, I.; Coelho, M.T.; Djordjević, V.; Alves, V.D.; Sousa, I.; Moldão-Martins, M.; Rakić, V.; Nedović, V.; Bugarski, B. Calcium–alginate–inulin microbeads as carriers for aqueous Carqueja extract. J. Food Sci., 2016, 81(1), E65-E75.
[http://dx.doi.org/10.1111/1750-3841.13167] [PMID: 26613390]
[20]
Tozuka, Y.; Ito, A.; Seki, H.; Oguchi, T.; Yamamoto, K. Characterization and quantitation of clarithromycin polymorphs by powder X-ray diffractometry and solid-state NMR spectroscopy. Chem. Pharm. Bull. (Tokyo), 2002, 50(8), 1128-1130.
[http://dx.doi.org/10.1248/cpb.50.1128] [PMID: 12192153]
[21]
Chen, C.H. (2011). An innate bactericidal oleic acid effective against skin infection of methicillin-resistant Staphylococcus aureus: a therapy concordant with evolutionary medicine. J. Microbiol. Biotechnol., 2011, 21(4), 391-399.
[22]
Dash, S.; Murthy, P.N.; Nath, L.; Chowdhury, P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol. Pharm., 2010, 67(3), 217-223.
[PMID: 20524422]

Rights & Permissions Print Cite
Article Metrics
3
© 2024 Bentham Science Publishers | Privacy Policy