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Release Patterns of Liposomal Bupivacaine in Artificial Cerebrospinal Fluid
Abstract Number: F 20
Abstract Type: Original Research
Objective: Local anesthetics are encapsulated into liposomes in order to prolong their effective duration without increasing their toxicity. In this study we aimed to prepare different forms of multilamellar liposomal bupivacaine to evaluate controlled release pattern for bupivacaine in artificial cerebrospinal fluid (CSF).
Methods: Primarily, bupivacaine HCl, bupivacaine base, cholesterol, dipalmitoyl phosphatidyl choline and methanole were distilated with vacuum in rotavapor device and were kept in ultrasound bath to achive homogenic distribution to get bupivacaine base with liposomal bupivacaine base and bupivacaine HCl with liposomal bupivacaine HCl. Artificial CSF buffered solution was prepared. Bupivacaine base with liposomal bupivacaine base, bupivacaine HCl with liposomal bupivacaine HCl and bupivacaine HCl were put in franz diffusion cell. The solutions were kept in hot water bath for 24 hours. The samples were taken in the first half, 1, 3, 6, 12 and 24th hours (first experiment). Solutions of bupivacaine base with liposomal bupivacaine base and bupivacaine HCl with liposomal bupivacaine HCl were centrifuged to get liposomal bupivacaine base and liposomal bupivacaine HCl. Liposomal bupivacaine base and liposomal bupivacaine HCl were put in franz diffusion cell. The solutions were kept in hot water bath for 24 hours. The samples were taken in the first half, 1, 3, 6, 12 and 24th hours (second experiment). Fifty-four sample obtained from the first experiment and 36 samples obtained from the second experiment were analyzed with HPLC and UPLC, respectively and the chromatographies were obtained.
Results: Fifty-four sample obtained from the first experiment and 36 samples obtained from the second experiment were analyzed with HPLC and UPLC, respectively and the chromatographies were obtained. Calibration graphics were obtained for bupivacaine base and bupivacaine HCl. The release pattern of these formulations were shown in the graphic. Multilamellar liposomal bupivacaine showed slow release in artificial CSF compared to bupivacaine HCl.
Conclusion: In this study we have achieved slow releasing pattern of liposomal bupivacaine compared to non-liposomal bupivacaine in artificial CSF. With the results of this study we are encouraged to use liposomal bupivacaine in obstetric anesthesia in the future of course after successful animal studies.
Key Words: Liposome, bupivacaine, CSF