Acta Chemica Malaysia (ACMY) 6(1) (2022) 20-25 Quick Response Code Access this article online Website: www.actachemicamalaysia.com DOI: 10.26480/acmy.01.2022.20.25 Cite the Article: Abayomi Bamisaye, Catherine Oluyemisi Eromosele, Enock Olugbenga Dare, Sivakumar Manickam, Oluseyi Adeboye Akinloye, Mopelola A. Idowu, Ige A. Raphael (2022). Generation, Characterization and Pharmacokinetic Study of Ofloxacin-loaded Castor Oil Based Nanoemulsion. Acta Chemica Malaysia, 6(1): 20-25. ISSN: 2576-6724 (Print) ISSN: 2576-6732 (Online) CODEN: ACMCCG REVIEW ARTICLE Acta Chemica Malaysia (ACMY) DOI: http://doi.org/10.26480/acmy.01.2022.20.25 GENERATION, CHARACTERIZATION AND PHARMACOKINETIC STUDY OF OFLOXACIN-LOADED CASTOR OIL BASED NANOEMULSION Abayomi Bamisaye a,b* , Catherine Oluyemisi Eromosele a , Enock Olugbenga Dare a , Sivakumar Manickam c , Oluseyi Adeboye Akinloye d , Mopelola A. Idowu a , Ige A. Raphael e a Department of Chemistry, College of Physical Sciences, Federal university of Agriculture, Abeokuta, Nigeria b Department of Chemistry, Faculty of Basic Medical and Applied Science, Lead City University, Ibadan, Nigeria c Faculty of Science and Engineering, University of Nottingham Malaysia, 43500 Semenyih, Selangor, Malaysia d Department of Biochemistry, College of Biological Sciences, Federal university of Agriculture, Abeokuta, Nigeria e Department Pure and Applied Chemistry, Kebbi State University of Science and Technology, Aliero, Nigeria * Corresponding Author E-mail: abayomibamisaye@gmail.com This is an open access journal distributed under the Creative Commons Attribution License CC BY 4.0, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. ARTICLE DETAILS ABSTRACT Article History: Received 31 December 2021 Accepted 04 February 2022 Available online 11 February 2022 The challenges associated with effective drug delivery necessitates the development and adoption of modern approach. This research aims to improve the bio-potency of ofloxacin (OF) against drug resistant strains of microorganism using nanoemulsion. The emulsification was achieved by mechano-chemical process. The morphological characterization of emulsion was carried out using Cryogenic-TEM (Cryo-TEM). The electro- kinetic properties and emulsion size was done using Zetasizer and Photon Correlation Photo-spectrometer (PCS). Drug-emulsion interaction study using FTIR. The antimicrobial studies of Ofloxacin (OF), non-drug loaded emulsion (COAB), drug-loaded emulsion (COAB+OF) was carried out on P. aeruginosa and pharmacokinetics were established using HPLC. Cryo-TEM micrograph showed spherical morphology with mean particle size of 166.8 and 177.5 nm for COAB and COAB+OF respectively. While PCS and Zetasizer recorded a mean value of 0.156 and -26.1 mV for COAB and 0.341, and -2.72 mV for COAB+OF respectively. This shows that the colloids are nano-sized, charged and metastable. FTIR results shows O-H absorption at 3570 – 3200 cm -1 , likewise CH3 and CH2 at 3050-2895 cm -1 for OF, COAB and COAB+OF respectively. This suggests encapsulation and wholeness with no drug-excipient interactions. The antimicrobial study shows COAB+OF to me more bio-potent that OF with zone of inhibition value of 12.8±0.3 mm compared to 8.0±0.2 mm in OF at 62.50 mg/ml. HPLC showed a maximum OF concentration (Cmax) of 2.27 µg/mL at 150 min which is the drug release maxima. This study showed that encapsulating ofloxacin in castor oil based nanoemulsion system improves its bio-potency. KEYWORDS Emulsification, Nanoemulsion, Morphology, Encapsulation, Pharmacokinetics 1. INTRODUCTION Nanoemulsion are thermodynamically bi-phasic liquid system which is a dispersion of liquid in liquid; oil-in water (O/W) or water-in–oil (W/O), with a dispersed phase in nanometer range (Bolla et al., 2020; Bamisaye et al., 2018; Tamilvanan and Benita, 2004). The different liquid phases are combined in a definite ratio to form a homogenous (in nature) liquid with the help of an emulsifying agent. They form spontaneously and present no discernible change in size distribution, charge, shape and spatial arrangement of its dispersed phase (Pandey et al., 2020; Jaiswal et al., 2015; Chime et al., 2014). The above mentioned features as well as the metastability, ease of preparation (spontaneous emulsification), high solubilization rate of drug molecules and excellent surface characteristics (size, charge and shape) of emulsion promotes the solubility, encapsulation, effective drug targeting and release, with an improved bioavailability of drugs and bio-active agent trapped in the organic phase of the emulsion system (Lee and McClements, 2010). This accorded it a wide application in the field of medicine and pharmacy as potential vehicle for delivery of biomolecules. Nanoemulsion has shown to be one of the frequently preferred types of ophthalmic, oral and transdermal drug delivery system as a result of its excellent characteristic which includes advanced rate of bioavailability and improved shelf life with high solubility and permeability across the reticuloendothelial cell barriers (Choradiya and Patil, 2021; Halnor et al., 2018). Many poor soluble or hydrophobic drugs are now soluble when transformed into nanoemulsion (Sonneville- Aubrun, 2004, Inayat and Mallikarjuna, 2012). Furthermore, some strains of disease causing microorganism have shown to have developed resistance to certain antibiotics. Pseudomonas aeruginosa is not exonerated because it is considered as one of the major causes of certain infections in the urinary tracts, burns, and wounds as well as hospital acquired pneumonia. This is due to its immunity to a vast array of antibiotics (Stryjewski and Sexton, 2003; Bryan et al., 2016). It is one of the major pathogens that contributes to high rate of morbidity and mortality in immunocompromised individuals (Goosens, 2003). More so, ofloxacin, a synthetic drug belongs to the second generation fluoroquinolones. It possesses a broad spectrum of activities against both