Chitosan Nanocarrier Entrapping Hydrophilic Drugs as Advanced Polymeric System for Dual Pharmaceutical and Cosmeceutical Application: A Comprehensive Analysis Using Box-Behnken Design

The objective of the present research is to propose chitosan as a nanocarrier for caffeine-a commonly used drug in combating cellulite. Being a hydrophilic drug, caffeine suffers from insufficient topical penetration upon application on the skin. Chitosan nanoparticles loaded with caffeine were prepared via the ionic gelation technique and optimized according to a Box-Behnken design. The effect of (A) chitosan concentration, (B) chitosan solution pH, and (C) chitosan to sodium tripolyphosphate mass ratio on (Y1) entrapment efficiency percent, (Y2) particle size, (Y3) polydispersity index, and (Y4) zeta potential were studied. Subsequently, the desired constraints on responses were applied, and validation of the optimization procedure was confirmed by the parameters exhibited by the optimal formulation. A caffeine entrapment efficiency percent of 17.25 +/- 1.48%, a particle size of 173.03 +/- 4.32 nm, a polydispersity index of 0.278 +/- 0.01, and a surface charge of 41.7 +/- 3.0 mV were attained. Microscopical evaluation using transmission electron microscope revealed a typical spherical nature of the nanoparticles arranged in a network with a further confirmation of the formation of particles in the nano range. The results proved the successful implementation of the Box-Behnken design for optimization of chitosan-based nanoparticles in the field of advanced polymeric systems for pharmaceutical and cosmeceutical applications.

Automated summary

The study aimed to propose chitosan as a nanocarrier for caffeine, optimizing the preparation of chitosan nanoparticles loaded with caffeine for enhanced topical penetration. The results demonstrated successful implementation of Box-Behnken design for chitosan-based nanoparticles, confirming the effectiveness of the optimized formulation through experimental validation.