Abstract
PurposeThe externally given all trans retinoic acid (ATRA) for the treatment of certain solid cancers faces challenges such as stability, persistence, and effective targeted delivery into cell which necessitate the development of a suitable liposomal formulation for ATRA treatment. MethodsLipo-ATRA was developed using 1, 2- Dioleoyl-3-trimethylammonium-propane (DOTAP), cholesterol and ATRA (70:20:10) by dry thin film method and investigated for its in vitro characteristics, in vivo ATRA bioavailability and pharmacokinetic properties in normal and cancer mice using HPLC. The in vivo therapeutic efficiency of lipo-ATRA was also studied. ResultsDOTAP lipo-ATRA (91.676 ± 1.29%) of 262.776 ± 1.045 d nm size with smooth spherical surface was developed which was stable at up to 60 days with sustained ATRA release through dialysis membrane. The serum pharmacokinetics for lipo-ATRA in cancer bearing mice has shown a higher half-life-(14.8200h), Cmax (0.66 μg/ml) and a lower CL (46.6061 μg/ml/h) in vivo when compared with free ATRA group (t1/2-13.2205h, Cmax-0.29 μg/ml, CL-136.2725 μg/ml/h). A significantly higher bioavailability in blood and lung even after 24 h with a promising therapeutic efficiency was observed in lipo-ATRA group. ConclusionsThe results showed that the formulation of lipo-ATRA in DOTAP and cholesterol in the ratio of 70:20 was the suitable carrier for ATRA in treating lung cancer.
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