Abstract

  The objective of this work was to prepare and investigate in vitro ciprofloxacin (CPX)-loaded solid lipid microparticles (SLM) against some selected micro-organisms for improved activity. Lipid matrix consisting of Softisan^®-154 and Phospholipon^® 90H was used to prepare SLMs loaded with CPX. The thermal properties of polymers and the SLMs were determined by a differential scanning calorimetry (DSC), particles size and the pH change of CPX-loaded SLMs were evaluated. The encapsulation efficiency (EE), loading capacity (LC) and in vitro release of CPX from the SLMs were evaluated. The antimicrobial activities of the SLM against selected organisms were determined. Characterizations showed that lipid matrix generated imperfect microstructure that accommodated CPX in a concentration-dependent manner. The EE and LC% were 89.2 and 33%, respectively. Maximum CPX release of > 80% was obtained in batch A3. The antimicrobial activity of the formulation against the tested organisms was comparably higher in batch C (49.10 ± 2.10) against S. aureus and (33.10 ± 0.21 mm) against S. typhii as compared to the reference sample. This result suggests the capability of the SLMs to modify the release of the drug and improve its activities against the microorganisms.

Keywords:Antimicrobial Activity; Ciprofloxacin; Hybrid; Lipid-Matrix

References

1. Alipour M and Suntres ZE. “Liposomal antibiotic formulations for targeting the lungs in the treatment of Pseudomonas aeruginosa”. Therapeutic Delivery 5 (2014): 409-427.
2. Friedrich I., et al. “Drug release and permeation studies of nanosuspensions based on solidified reverse micellar solutions (SRMS)”. International Journal of Pharmaceutics 305 (2005): 167.
3. Attama AA and Mu¨ller-Goymann CC. “A critical study of physically structured lipid matrices composed of a homolipid from Capra hircus and theobroma oil”. International Journal of Pharmaceutics 322 (2006): 67-78. 
4. Franklin CK., et al. “Surface-modified mucoadhesive microgels as a controlled release system for miconazole nitrate to improve localized treatment of vulvovaginal candidiasis”. European Journal of Pharmaceutical Sciences 111 (2018): 358-375. 
5. Umeyor CE., et al. “Preparation of novel solid lipid microparticles loaded with gentamicin and its evaluation in vitro and in vivo”. Journal of Microencapsulation 29 (2014): 296-307. 
6. Attama AA., et al. “Formulation and in vitro evaluation of a PEGylated microscopic lipospheres delivery system for ceftriaxone sodium”. Drug Delivery 16 (2009): 448-457. 
7. Turel I., et al. “Compounds of antibacterial agent ciprofloxacin and magnesium - Crystal structures and molecular modeling calculations”. European Journal of Inorganic Chemistry (2008): 3718-3727. 
8. Aristilde L and Sposito G. “Binding of ciprofloxacin by humic substances: a molecular dynamics study”. Environmental Toxicology and Chemistry 29 (2010): 90-98. 
9. Severino P., et al. “Polymorphism, crystallinity and hydrophilic-lipophilic balance of stearic acid and stearic acid-capric/caprylic triglyceride matrices for production of stable nanoparticles”. Colloids Surf B Biointerfaces 86 (2011): 125-130.
10. Xia J., et al. “Nosocomial infection and its molecular mechanisms of antibiotic resistance”. BioScience Trends 10 (2016): 14-21. 
11. Zhang ZR., et al. “In vivo biodistribution, anti-inflammatory, and hepatoprotective effects of liver targeting dexamethasone acetate loaded nanostructured lipid carrier system”. International Journal of Nanomedicine 5 (2010): 487-497. 
12. Mbah CC. “Formulation and evaluation of ethosomes for the delivery of four bioactive agents. PhD Thesis”. Department of Pharmaceutics University of Nigeria, Nsukka, Nigeria (2013). 
13. O'driscoll CM and Griffin BT. “Biopharmaceutical challenges associated with drugs with low aqueous solubility—the potential impact of lipid-based formulations”. Advanced Drug Delivery Reviews 60 (2008): 617-624. 
14. Shah NV., et al. “Nanostructured lipid carriers for oral bioavailability enhancement of raloxifene: design and in vivo study”. Journal of Advanced Research 7 (2016): 423-434. 
15. Mumuni AM and Charles OE. “Phospholipon 90H (P90H)-based PEGylated microscopic lipospheres delivery system for gentamicin: an antibiotic evaluation”. Asian Pacific Journal of Tropical Biomedicine (2012): 889-894. 
16. Kenechukwu FC., et al. “Solid lipid microdispersions (SLMs) based on PEGylated solidified reverse micellar solutions (SRMS): A novel carrier system for gentamicin”. Drug Delivery 22 (2015): 710-722. 
17. Clinical and Laboratory Standards Institute (CLSI). Reference methods for broth dilution antifungal susceptibility testing of yeast. In: Approved Standard M27-A3, 3^rd edition. Clinical and Laboratory Standards Institute (2008). 
18. Nnamani PO., et al. “SRMS142-based solid lipid microparticles: Application in oral delivery of glibenclamide to diabetic rats”. European Journal of Pharmaceutics and Biopharmaceutics 76 (2012): 68-74. 
19. Chukwuma OA., et al. “Formulation, characterization and anti-malarial activity of homolipid-based artemether microparticles”. International Journal of Pharmaceutics 478 (2015): 202-222. 
20. Severino P., et al. “Development and characterization of a cationic lipid nanocarriers as non-viral vector for gene therapy”. European Journal of Pharmaceutical Sciences 66C (2014): 78-82.
21. Sadeek SA., et al. “Spectroscopic, structure and antimicrobial activity of new Y(III) and Zr(IV) ciprofloxacin”. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy 78 (2011): 854-867. 
22. Nabanita K., et al. “Development and evaluation of a cedrol-loaded nanostructured lipid carrier system for in vitro and in vivo susceptibilities of wild and drug resistant Leishmania donovani amastigotes”. European Journal of Pharmaceutical Sciences 104 (2017): 196-211. 
23. Govindarajan VK., et al. “Ciprofloxacin loaded genipin cross-linked chitosan/heparin nanoparticles for drug delivery application”. Materials Letters 180 (2016): 119-122.

Citation

Citation: Momoh A Mumuni., et al. “Antimicrobial Activity of Ciprofloxacin-Loaded Softisan-154 Lipid Microparticles: Physicochemical Evaluation and In Vitro Activity". Acta Scientific Pharmaceutical Sciences 4.5 (2020): 30-35.