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The molecular targeted drug ATRA demands a suitable carrier that delivers to the cancer site due to its poor bioavailability and drug resistance. ATRA, being a lipid with carboxylic acid, has been nano-formulated as a cationic lipo-ATRA with DOTAP:cholesterol:ATRA (5:4:1) and its pH-responsive release, intracellular drug accumulation, and anticancer effect on human lung cancer (A549) cell line analysed. The analysis of the physicochemical characteristics of the developed lipo-ATRA (0.8 mu mol) revealed that the size of 231 +/- 2.35 d.nm had a zeta potential of 6.4 +/- 1.19 and an encapsulation efficiency of 93.7 +/- 3.6%. The ATRA release from lipo-ATRA in vitro was significantly (p