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Adv Pharm Bull. 2024;14(4): 870-882.
doi: 10.34172/apb.39294
  Abstract View: 120
  PDF Download: 14

Research Article

Developing and Applying a Single Strategy for Improved Intestinal Permeability of Diverse and Complex Phytomolecules: Nanoformulations of Rutin, Quercetin, Thymoquinone Provide Proof-of-Concept

Rajani Mathur 1* ORCID logo, Sahiba Khan 1, Ruchi Tripathi 1 ORCID logo, Saima Amin 2 ORCID logo, Saumitra Dey Choudhary 3

1 Department of Pharmacology, Delhi Institute of Pharmaceutical Sciences & Research, DPSRU, New Delhi, India
2 Pharmaceutics School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi, India
3 All India Institute of Medical Sciences, New Delhi, India
*Corresponding Author: Rajani Mathur, Email: mathurajani@gmail.com

Abstract

Purpose: The clinical use and efficacy of phytomolecules are often hampered as their complex structure, poor aqueous solubility and low biological stability restricts their intestinal permeability which results in low oral bioavailability. Rutin (RT), quercetin (QU), thymoquinone (TQ) are few of such potent and therapeutically versatile phytomolecules that await maximal utilization. To address this lacuna, an attempt was made to develop a single strategy for enhanced intestinal permeation that can be applied to 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 examined for particle characteristics, EE, in vitro release and kinetics. Phytomolecule loaded nanoparticle (PNPs) were encapsulated in HPMC grade capsule shell and evaluated for intestinal permeability by everted gut sac method.

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 (<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.


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Submitted: 21 Sep 2022
Revision: 06 Aug 2024
Accepted: 08 Sep 2024
ePublished: 15 Sep 2024
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