DEVELOPMENT AND EVALUATION OF PHOSPHATIDYLCHOLINE COMPLEXES OF ARBUTIN AS SKIN WHITENING AGENTAbstract
Introduction: Disorders of hyperpigmentation are difficult to treat, particularly in dark skin individuals. There is a dramatic enhancement of skin permeability of phytoconstituents due to their complexation with phospholipids. Complexation leads to better permeation through the skin, which is otherwise not possible. Research work focused on the development and evaluation of phos-phatidylcholine complexes of arbutin, having the issue of poor skin permeability as skin whitening agents. Materials and Methods: Arbutin, phosphatidylcholine, and petroleum ether have been used for the development of complexes. Authentication of arbutin has been performed by Fourier Transform Infrared study. UV–visible spectrophotometric method has been developed for estimation of arbutin followed by the development of complexes by rotary flask evaporation technique, preliminary trials for selection of dependent and independent variables, optimization of complexes by Box- Behnken reduced surface response design, evaluation of optimized batch by percentage entrapment efficiency, particle size, zeta potential, and in-vitro drug release study by Franz diffusion cell. Result and Discussion: Arbutin sample FTIR data and standard FTIR data are matched. Final polynomial equation is, % Entrapment Efficiency = + 161.924 – 25.954 * Arbutin: PC ratio – 3.8654 * Film formation temperature 0.991 * Hydration temperature +0.29737654320988 * Hydration time +17.0566 * Arbutin: PC ratio 2 + 0.03880416666667 * Film formation temperature 2 + 9.941E-003 * Hydration temperature 2 -1.499E-003 * Hydration time 2. Results show that there is ≥ 92% similarity between predictive and actual values. Developed complexes show a better in-vitro drug release profile compared to an aqueous solution of arbutin, which indicates optimized complexes improve permeability.
R. K. Patel and M. B. Jadeja *
Shree S.K. Patel College of Pharmaceutical Education and Research, Ganpat University, Mahesana, Gujarat, India.
14 November 2019
19 December 2020
17 January 2021
01 February 2021