Rheological properties and release profile of aloperine vaginal thermosensitive in situ gel
OBJECTIVE To examine the rheological characteristics of a thermosensitive in situ gel containing aloperine for vaginal application and to forecast its in vivo release pattern.METHODS The thermosensitive gel was fabricated using poloxamer 407 and poloxamer 188 through a cold dissolution process.The gelation temperature and duration of the aloperine thermosensitive gel were determined using the inverted tube method.Rheological parameters were measured with a rheometer,and the in vitro drug release performance was assessed using a membraneless dissolution model.The local retention in the vagina was studied using fluorescence imaging.RESULTS The gel at room temperature appeared as a light yellow,homogeneous,transparent fluid with low viscosity.It transformed into a gel-like pseudoplastic fluid with increased viscosity at approximately 33 ℃ and formed a gel at 37 ℃ after being diluted with a simulated vaginal fluid.The in vitro release kinetics of aloperine from the thermosensitive gel aligned with the Higuchi equation.Through imaging and 1R783 fluorescence quantitative analysis,the aloperine thermosensitive gel could remain in the mouse vagina for at least 48 h,with almost no fluorescence signal observable in its solution after 24 h.CONCLUSION Aloperine thermosensitive gel,with its appropriate gelation temperature and excellent rheological properties,has the potential to extend the drug retention time in the vagina and delay drug release,thereby meeting the requirements for local vaginal medication.
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