Self-Assembled Chitosan Nanoparticles for Percutaneous Delivery of Caffeine: Preparation, Characterization and in Vitro Release Studies

Abstract

Objective: Chitosan (CS)-tripolyphosphate (TPP)-nanoparticles (NPs) have been extensively studied during the past few decades due to their wellrecognized applicability in various fields. The present study attempts to optimise the development of these nanoparticles to enhance the percutaneous delivery of caffeine.Methods: CS-TPP-NPs were prepared via ionic cross-linking of CS and TPP and were characterized. The influence of several formulation conditions (CS: TPP mass ratio and concentration of caffeine) and process parameters (stirring speed, stirring time and ultra-sonication time) on the colloidal characteristics of CS-TPP-NPs were investigated and the resulting nanoparticles were characterized using scanning electron microscopy (SEM), transmission electron microscopy (TEM), Fourier transform infrared (FTIR) and x-ray diffraction (XRD) analyses. Physicochemical properties, including particle size, zeta potential and polydispersity index (PDI) were examined, and in vitro release studies were conducted to ascertain the release profile of caffeine from the nanoparticles. In addition, the colloidal stability of the prepared NPs was also assessed on storage.Results: Process parameters appeared to exert a significant effect on the physicochemical characteristics of the CS-TPP-NPs. The CS-TPP-NPs prepared under optimum conditions (CS concentration of 0.2 mg/ml, CS: TPP volume ratio of 25:12 ml, stirred at 700 rpm for 60 min, with 0.97 mg/ml caffeine concentration and treatment with low ultra-sonication for 30 min) had shown a mean particle size of ~143.43±1.69 nm, zeta potential of+43.13±1.10 mV, PDI of ~0.30±0.01. A drug loading capacity and encapsulation efficiency of 48.89% and 60.69%, respectively, were obtained. Cumulative release study for drug-loaded CS-NPs was significantly (p<0.001, paired t-test) higher (58.7% caffeine released) compared to control formulation (41.5% caffeine released) after 72 h. Stability studies conducted for 28 d showed that caffeine-loaded CS-NPs degraded much quicker when stored at 25 ⁰C than 4 ⁰C. It was also noted that caffeine-loaded CS-NPs in the freeze-dried form were unstable as the surface charge of nanoparticles dropped from positive zeta potential to-3.55 mV within 2 d at 4 ⁰C and at 25 ⁰C, surface charge dropped to-3.16 mV within 14 d of the experiment. Conclusion:Chitosan (CS)-tripolyphosphate (TPP)-nanoparticles (NPs) appear to be a promising strategy to achieve sustained percutaneous delivery of caffeine.

Modification of Clinoptilolite with Benzalkonium Chloride as a Carrier of Metformin Hydrochloride

“…This indicates the existence of a bond between clinoptilolite and benzalkonium chloride. This result is consistent with the research by Hassan et al [22], which showed that caffeine encapsulation in chitosan nanoparticles broadened -OH absorption peaks. CLI-BKC FTIR spectra shows that BKC absorption in Na-CLI results in a shift in absorption peak from 3448.72 cm -1 to 3456.44 cm -1 , showing an interaction between -OH group and benzalkonium chloride molecules.…”

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

“…Among the materials used for the production of nanocarriers for caffeine, chitosan (CS) has been also proposed in the literature. Despite the infinite advantages offered by such polymer, the number of studies conducted regarding the incorporation of caffeine in CS is very limited.Accordingly, the research works of Sahudin et al [ 16 ] and Suptijah et al [ 17 ] proposed chitosan as a promising carrier for caffeine. Chitosan possesses numerous benefits including its biodegradability, bioavailability, and high safety profile [ 18 , 19 ].…”

Effect of alpha-lipoic acid and caffeine-loaded chitosan nanoparticles on obesity and its complications in liver and kidney in rats

“…Caffeine and chitosan were obtained from Sigma-Adrich, Germany. The method used in the preparation of caffeine-loaded chitosan nanoparticles (CAF-CS NPs) depended on the method described by Sahudin et al ( 2018 ). In this method, nanoparticles (NPs) were prepared by inducing the gelation of chitosan (CS) solutions with the cross-link agent sodium tripolyphosphate (TPP).…”