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Objective: The aim of present study was to formulate chitosan microspheres loaded with ethanolic extract of Lens culinaris Medikus (L.culinaris) seeds (ME) and to explore its anticancer potential against lung cancer (A549) cell line. Methods: Central composite design was applied to prepare and optimise the chitosan microspheres. The prepared microspheres were evaluated for its physicochemical characterisation, in-vitro drug release and anti-cancer potential in-vitro. Results: L.culinaris loaded chitosan microspheres were prepared successfully with suitable particle size, entrapment efficiency and drug release. The developed ME were spherical shaped with the particle size of 2.08 µm. The drug entrapment efficiency and cumulative drug release was found 1.58±0.02% and 81.95±0.35% respectively. Differential Scanning Colorimetry studies revealed no interaction between drugs and polymers used. The cytotoxic effect of the optimised formulation revealed a significant response as compared to the ethanolic extract of L.culinaris seeds (IC50: 22.56 μg/ml vs. 63.58 μg/ml), which was comparable to that of reference drug, doxorubicin (22 µg/ml). These observations demonstrate that the optimised microspheres are effective against lung cancer(A549) cells. Conclusion: The significant cytotoxic response of the developed microspheres may be attributed due to its low particle size, high entrapment efficiency and prolonged drug release profile.

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