Encapsulation of metronidazole in polycaprolactone microspheres
Non-aqueous oil-in-oil solvent evaporation technique is used for the preparation of polycaprolactone microspheres loaded with the antibiotic metronidazole by introducing different masses for the drug. The prepared microspheres are characterized by calculating drug encapsulation and drug loading percentages, measuring the corresponding particle size, performing FT-IR polymer-drug compatibility study and in vitro drug release. Moderate drug encapsulation values with a maximum of 34% are observed due to the low molecular weight of the drug. Microspheres had a particle size ranging between 130 and 280 µm with a spherical profile and porous structure. FT-IR study showed no interactions between the drug and the polymer. Drug release studies showed fast release rates for all the formulations with the slowest release for the highest drug loading.
Keywords: polycaprolactone, metronidazole, targeted drug delivery, solvent evaporation.
2- Erdemli O, Ozen S, Keksin D, Usanmaz A, Batu ED, Atilla B, Tezcaner A, In vitro evaluation of effects of sustained anti-TNF release from MPEG-PCL-MPEG and PCL microspheres on human rheumatoid arthritis synoviocytes, Journal of Biomaterials Applications, 2014; 29(4):524-542.
3- Mohammad S, Pectin-based biodegradable hydrogels with potential biomedical applications as drug delivery systems, Journal of Biomaterials and Nanobiotechnology, 2011; 2(1):36-40.
4- Yammine P, Maarawi T, Moussa D, Abdel-Massih R, Kassab R, Effects of different surfactants on Indomethacin microspheres formulations, Journal of Advances in Chemistry, 2015; 11(4):3453-3462.
5- Ferreira SI, Bettencourt AF, Gonçalves MD, Kasper S, Bétrisey B, Kikhney J, Moter A, Trampuz A, Almeida AJ, Activity of Daptomycin- and Vancomycin-loaded poly-epsilon-caprolactone microparticles against mature staphylococcal biofilms, International Journal of Nanomedicine, 2015; 10(1):451-4366.
6- Dash TK, Konkimalla VB, Poly-є-caprolactone based formulations for drug delivery and tissue engineering: a review, Journal of Controlled Release, 2012; 158(1):15-33.
7- Choughury PK, Murthy PN, Tripathy NK, Panigraphy R, Behera S, Investigation of drug polymer compatibility: formulation and characterization of metronidazole microspheres for colonic delivery, Pharmaceutical Sciences, 2012; 3(5):1-20.
8- Emara L, Abdo A, El-Ashmawy A, Mursi N, Preparation and evaluation of metronidazole sustained release floating tablets, International Journal of Pharmacy and Pharmaceutical Sciences, 2014; 6(9):198-204.
9- Dash TK, Konkimalla VB, Polycaprolactone based formulations for drug delivery and tissue engineering: a review, Journal of Controlled Release, 2012; 158(1):15-33.
10- Miladi K, Ibraheem D, Iqbal M, Sfar S, Fessi H, Elaissari A, Particles from preformed polymers as carriers for drug delivery, Excli Journal 2014; 13:28-57.
11- Kassab R, Moussa D, Yammine P, Polycaprolactone as drug carrier for an antifungal agent, Journal of Drug Delivery and Therapeutics, 2018; 8(1):81-85.
12- Mondal D, Griffith M, Venkatraman S, Polycaprolactone-based biomaterials for tissue engineering and drug delivery: current scenario and challenges, International Journal of Polymeric Materials and Polymeric Biomaterials, 2016; 65(5):255-265.
13- Shi R, Xue J, He M, Chen D, Zhang L, Tian W, Structure, physical properties, biocompatibility and in vitro-vivo degradation behavior of anti-infective polycaprolactone-based electrospun membranes for guided tissue/bone regeneration, Polymer Degradation and Stability, 2014; 109:293-306.
14- Lokhande AB, Mishra S, Kulkarni RD, Naik JB, Influence of different viscosity grade ethylcellulose polymers on encapsulation and in vitro release study of drug loaded nanoparticles, Journal of Pharmacy Research, 2013; 7(5):414-420.
15- Yuce M, Canefe K, Indomethacin-loaded microspheres: preparation, characterization and in-vitro evaluation regarding ethylcellulose matrix material, Turkish Journal of pharmaceutical sciences, 2008; 5(3):129-142.
16- Maji R, Ray S, Ras B, Nayak AK, Ethylcellulose microparticles containing metformin HCl by emulsification-solvent evaporation technique: effect of formulation variables, ISRN Polymer Science, 2012, article ID 801827.
17- Jelvehgari M, Valizadi H, Rezapour M, Nokhodchi A, Control of Encapsulation Efficiency in Polymeric Microparticle System of Tolmetin, Pharmaceutical Development and Technology, 2010; 15(1):71-79.
18- Kassab R, Yammine P, Moussa D, Safi N, A comparative study of Doxycycline and Tetracycline polymeric microspheres, International Journal of Pharmaceutical Sciences and Research, 2014; 5(6):2452-2457.
19- Cetin M, Atila A, Sahin S, Vural I, Preparation and characterization of metformin hydrochloride loaded-Eudragit RSPO and Eudragit RSPO/PLGA nanoparticles, Pharmaceutical Development and Technology, 2013; 18(3):570–576.
20- Zupancic S, Potrc T, Baumgartner S, Kocbek P, Kristl J, Formulation and evaluation of chitosan/polyethylene oxide nanofibers loaded with metronidazole for local infections, European Journal of Pharmaceutical Sciences, 2016; 95:152-160.
21- Natarajan V, Krithica N, Madhan B, Sehgal PK, Formulation and evaluation of Quercitin polycaprolactone microspheres for the treatment of rheumatoid arthritis, Journal of Pharmaceutical Sciences, 2011; 100(1):195-205.
22- Kassab R, Yammine P, Moussa D, Safi N, Microspheres containing Doxycycline: properties and in vitro study, International Journal of Drug Delivery, 2013; 5(3):264-269.
23- Yoon Y, Kinam P, Control of Encapsulation Efficiency and Initial Burst in Polymeric Microparticle Systems, Archives of Pharmacal Research, 2004; 27(1):1-12.
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