Abstract
Purpose: The clinical use of phytomolecules is restricted due to low oral bioavailability that may be attributed to their poor intestinal permeability owing to their complex structure, poor aqueous solubility and low biological stability. Rutin (RT), quercetin (QU), thymoquinone (TQ) are such potent and therapeutically versatile phytomolecules that await maximal utilization. Here we report a single strategy for enhanced intestinal permeation of diverse phytomolecules. Method: A simple idea with easy-to-apply method was developed that involved preparing nanoparticles of the phytomolecules RT, QU, TQ using eudragit matrix (RT-PNP, QU-PNP, TQ-PNP) and encapsulated in HPMC grade capsule shell. The PNPs were evaluated for particle characteristics, encapsulation efficiency, in vitro release kinetics, and intestinal permeability. Result: The average particle sizes of RT-PNP, QU-PNP, TQ-PNP were 446 ± 0.152, 39.6 ± 0.006 and 186 ± 0.513 nm, polydispersity indices were < 0.5 with negative zeta potential. The % release of respective phytomolecule from RT-PNP, QU-PNP, TQ-PNP was significantly higher (p<0.05) at pH 6.8 than pH 1.2. PNPs followed higuchi kinetics with non-Fickian diffusion mechanisms. The apparent intestinal permeability (Papp) of RT-PNP, QU-PNP, TQ-PNP were 14.45 ± 4.85, 12.96 ± 1.73 and 30.87 ± 8.75 µg/cm2, respectively, significantly (P <0.5) greater vs RT, QU, TQ, respectively. CLSM confirmed significantly higher (p<0.05) intestinal permeation of RT-PNP, QU-PNP, TQ-PNP vs RT, QU, TQ, respectively. Conclusion: Developed PNPs appear to be a good approach to increase the permeability of hydrophobic phytomolecules.