@article {10.3844/ajmsp.2011.1.8, article_type = {journal}, title = {Antibacterial Activity of β-Cyclodextrin and 2-Hydroxypropyl-β-Cyclodextrin Trimethoprim Complexes}, author = {Sun, Hsien-Kuo and Seshadri, Madhumathi and Lingard, Scott and Monaghan, Wayne and Faoagali, Joan and Chan, Enoch and McDonald, Helen and Houston, Todd and King, Michelle and Peak, Ian and Wilson, Jennifer C. and Haywood, Alison and Spencer, Briohny and Dunn, Perrea and Grant, Gary Dean}, volume = {2}, year = {2011}, month = {Oct}, pages = {1-8}, doi = {10.3844/ajmsp.2011.1.8}, url = {https://thescipub.com/abstract/ajmsp.2011.1.8}, abstract = {Problem statement: Cyclodextrin complexation has previously been shown to improve the solubility and dissolution properties of trimethoprim; however, no report provides an account of the effect cyclodextrin complexation has on the antibacterial activity of this agent. Approach: β-cyclodextrin and 2-hydroxypropyl β-cyclodextrin inclusion complexes of trimethoprim were prepared and confirmed by differential scanning calorimetry and proton nuclear magnetic resonance. The in-vitro antibacterial activity, in terms of minimum inhibitory concentrations, of cyclodextrin-drug complexes were compared to uncomplexed free trimethoprim by a broth-microdilution method against several sensitive and resistant Gram-positive and Gram-negative bacteria. The effect of complexation on the apparent permeability coefficients was also determined using a Caco-2 permeability assay to account for potential alterations in bioavailability that could influence in-vivo antibacterial activity. Results: Inclusion complexation of trimethoprim with both unsubstituted and hydroxylated versions of β-cyclodextrin produced a reduction in the MIC80 required to inhibit the growth of S. aureus ATCC 29213, S. pneumoniae ATCC 4961, S. epidermidis ATCC 14990 and E. coli ATCC 25922 (p>0.05). The effect was limited to bacteria normally susceptible to trimethoprim. Neither complex negatively affected the antibacterial activity of trimethoprim. Hydroxypropyl-β-cyclodextrin and β-cyclodextrin inclusion complexes significantly (p}, journal = {Current Research in Microbiology}, publisher = {Science Publications} }