Abstract
The aim of this study was to prepare and evaluate alpha-mangostin-loaded polymeric nanoparticle gel (alpha-MNG-PLGA) formulation to enhance alpha-mangostin delivery in an epidermal carcinoma. The poly (D, L-lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) were developed using the emulsion-diffusion-evaporation technique with a 3-level 3-factor Box-Behnken design. The NPs were characterized and evaluated for particle size distribution, zeta potential (mV), drug release, and skin permeation. The formulated PLGA NPs were converted into a preformed carbopol gel base and were further evaluated for texture analysis, the cytotoxic effect of PLGA NPs against B16-F10 melanoma cells, and in vitro radical scavenging activity. The nanoscale particles were spherical, consistent, and average in size (168.06 & PLUSMN; 17.02 nm), with an entrapment efficiency (EE) of 84.26 & PLUSMN; 8.23% and a zeta potential of -25.3 & PLUSMN; 7.1 mV. Their drug release percentages in phosphate-buffered solution (PBS) at pH 7.4 and pH 6.5 were 87.07 & PLUSMN; 6.95% and 89.50 & PLUSMN; 9.50%, respectively. The release of alpha-MNG from NPs in vitro demonstrated that the biphasic release system, namely, immediate release in the initial phase, was accompanied by sustained drug release. The texture study of the developed alpha-MNG-PLGA NPs gel revealed its characteristics, including viscosity, hardness, consistency, and cohesiveness. The drug flux from alpha-MNG-PLGA NPs gel and alpha-MNG gel was 79.32 & PLUSMN; 7.91 and 16.88 & PLUSMN; 7.18 mu g/cm(2)/h in 24 h, respectively. The confocal study showed that alpha-MNG-PLGA NPs penetrated up to 230.02 mu m deep into the skin layer compared to 15.21 mu m by dye solution. MTT assay and radical scavenging potential indicated that alpha-MNG-PLGA NPs gel had a significant cytotoxic effect and antioxidant effect compared to alpha-MNG gel (p < 0.05). Thus, using the developed alpha-MNG-PLGA in treating skin cancer could be a promising approach.