Supramolecular Complexes of Phospholipids and β-Cyclodextrin with Bioactive β-Carotene: A Comparative Physico-Chemical and Functional Evaluation

Background: β-carotene, a chief component of carotenoids family exhibits multiple numbers of pharmacological activities. However, its poor aqueous solubility and low dissolution rate restricts it to become a potential drug candidate. Hence, β-carotenephospholipids complex (BPLC) and β-carotene-β-cyclodextrin complex (BCDC) were prepared with an objective of enhancing its aqueous solubility and dissolution rate. Materials and Methods: BPLC and BCDC were synthesized using solvent evaporation and kneading method respectively. BPLC and BCDC, were characterized by particle size and zeta potential analysis, complexation rate, drug loading, Fourier transform infrared spectroscopy and differential scanning calorimetry. Functional characterization of above formulations was performed by solubility and in vitro dissolution studies. Results and Conclusion: Particle size analysis result of BCDC and BPLC formulations were found to be suitable for oral route of administration. FT- IR and DSC studies supported the formation of BCDC and BPLC formulation. Solubility results displayed that BPLC (1:1) significantly enhanced the aqueous solubility upto (28-fold), compared to BCDC (1:2) (18-fold) and β-carotene. Dissolution studies showed that BPLC (1:1) considerably improved the release rate of β-carotene in PBS (pH 7.4) compared to BCDC (1:2) and β-carotene suspension. Hence, above comparison confirmed that phospholipids could be promising carrier compared to β-cyclodextrin for overall enhancement of aqueous solubility and in vitro dissolution rate of β-carotene.