The objective of this study was to compare the biocompatibility for local irritation and bioavailability of Gentacol TM and Collatamp TM , after single intramuscular loading in rats. Sixty-six male Sprague-Dawley rats were divided into 4 groups; (1) any test materials were not applied into the quadriceps muscles (control group, N = 6), (2) Gentamicin was injected into the quadriceps muscles (Gentamicin group, N = 6), (3) Collatamp was applied into the quadriceps muscles (Collatamp group, N = 27), and (4) Gentacol was applied into the quadriceps muscles (Gentacol group, N = 27). The concentration of gentamicin in muscles was gradually decreased with time after loaded in the both Gentacol TM and CollatampTM loaded regions. No detectable gentamicin was observed in the plasma of Gentacol TM and Collatamp TM loaded rats. Histologically, moderate to severe inflammatory cell infiltrations including PMN, lymphoid cells and macrophages were observed with slight to moderate edematous changes of muscle fibers after intramuscular injection of gentamicin. However, these histopathological changes of gentamicin injection induced local irritations were dramatically decreases after intramuscular loading of Collatamp TM and Gentacol TM . These results suggest Gentacol TM may show favorable local bioavailability and induce only slight local irritations as comparable as Collatamp TM without systemic exposures in the condition of this experiment.