Improving Ofloxacin's Solubility and Bioavailability by Cyclodextrin Complexation: An Extensive Analysis

Abstract

One of the biggest obstacles to efficient oral drug administration is still poor aqueous solubility, especially for BCS Class II compounds like ofloxacin, where absorption is limited by dissolution rather than membrane penetration. Cyclodextrins (CDs), which are cyclic oligosaccharides with a hydrophilic exterior and a hydrophobic cavity, are frequently employed to improve formulation flexibility, stability, and apparent aqueous solubility by forming inclusion complexes with lipophilic medications. Ofloxacin–CD systems (including native β-CD and substituted derivatives like methyl-β-CD and hydroxypropyl-β-CD) are summarized in this review along with the physicochemical and spectroscopic characterization (phase-solubility, FTIR, DSC, XRD, NMR), effects on in-vitro dissolution and stability, and methods of complex preparation (kneading, co-precipitation, solvent evaporation, freeze-drying, and phase-solubility). According to representative research, β-cyclodextrin can boost the solubility of ofloxacin by multiple times, and derivative CDs typically result in higher complexation efficiency and solubility enhancement than native CDs. According to more comprehensive analyses of antibiotic–CD complexes, CD inclusion usually results in better solubility, pharmacokinetic exposure, and therapeutic efficacy for antibiotics that are poorly soluble. Limitations (drug loading, cost, and safety at high CD concentrations), formulation implications, and future directions such as CD-polymer hybrids and nanostructured CD assemblies for optimal delivery are also covered in the review. All things considered, cyclodextrin complexation shows promise as a workable and expandable method to lessen the solubility constraints of ofloxacin and enhance its biopharmaceutical efficacy.