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Bioavailability Enhancement of Herbal Drugs through Phytosomal and Nanoformulation Technologies

Nishita R. Mehta*

Department of Pharmaceutics and Herbal Drug Delivery, BITS Pilani, Hyderabad Campus, India

*Corresponding Author:
Nishita R. Mehta
Department of Pharmaceutics and Herbal Drug Delivery, BITS Pilani, Hyderabad Campus, India
E-mail: nishita.mehta@bitspilani.ac.in

Received: 05-Mar-2025, Manuscript No. jprpc-25-169379; Editor assigned: 7-Mar-2025, Pre-QC No. jprpc-25-169379 (PQ); Reviewed: 18-Mar-2025, QC No jprpc-25-169379; Revised: 25-Mar- 2025, Manuscript No. jprpc-25-169379 (R); Published: 30-Mar-2025, DOI: 10.4172/2347-1234.13.010

Citation: Nishita R. Mehta, Bioavailability Enhancement of Herbal Drugs through Phytosomal and Nanoformulation Technologies. J Pharmacogn Phytochem. 2025.13.010.

Copyright: © 2025 Nishita R. Mehta, this is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Visit for more related articles at Research & Reviews: Journal of Pharmacognosy and Phytochemistry

Abstract

Despite the promising pharmacological activity of herbal drugs, many suffer from poor oral bioavailability due to low solubility, permeability, and stability. Modern drug delivery technologies such as phytosomes, liposomes, nanoemulsions, and solid lipid nanoparticles are being employed to enhance the absorption and therapeutic efficacy of herbal compounds. This article reviews advanced formulation strategies used to improve the pharmacokinetic profiles of key phytoconstituents.

INTRODUCTION

Herbal medicines offer a wide range of therapeutic benefits, but poor bioavailability of active constituents remains a major barrier to clinical translation. Phytoconstituents like curcumin, quercetin, and silymarin have low aqueous solubility and are rapidly metabolized. Nanoformulation techniques provide novel ways to overcome these limitations by enhancing solubility, protecting against enzymatic degradation, and improving permeability across biological membranes.

Barriers to Herbal Drug Bioavailability

  • Poor Aqueous Solubility: Limits absorption in the GI tract (e.g., curcumin, baicalin).
  • First-Pass Metabolism: Rapid hepatic metabolism reduces systemic availability.
  • P-Glycoprotein Efflux: Many phytochemicals are substrates for efflux transporters.
  • Enzymatic Instability: Degradation by intestinal or hepatic enzymes.

Phytosomal Technology

Definition:
Phytosomes are complexes of phytoconstituents with phospholipids (usually phosphatidylcholine), which improve solubility and membrane permeability.

Applications:

Phytoconstituent

Herbal Source

Benefit via Phytosome

Silybin

Silybum marianum

↑ Liver bioavailability

Curcumin

Curcuma longa

↑ Anti-inflammatory activity

Quercetin

Allium cepa, Camellia sinensis

↑ Cardiovascular protection

Ginkgo flavones

Ginkgo biloba

↑ CNS penetration

Mechanism: Phytosomes interact with lipid bilayers, enhancing passive diffusion across enterocytes.

Nanoparticle-Based Herbal Formulations

  1. Solid Lipid Nanoparticles (SLNs)
    • Encapsulate lipophilic actives
    • Controlled release and improved stability
  2. Nanoemulsions
    • Droplet size <200 nm; improves solubilization of essential oils and actives
    • Example: Thymoquinone-loaded nanoemulsion for anti-inflammatory activity
  3. Polymeric Nanoparticles
    • Use of biopolymers (e.g., chitosan, PLGA)
    • Improved mucoadhesion and intestinal residence time
  4. Nanocrystals
    • Pure drug particles stabilized with surfactants
    • Increases dissolution rate and bioavailability

Case Studies

  • Curcumin Phytosome (Meriva®): 29x higher absorption vs. unformulated curcumin; clinically validated in arthritis and metabolic syndrome.
  • Silybin-Phosphatidylcholine Complex: Demonstrated hepatoprotection in alcoholic liver disease models.
  • Quercetin-loaded SLNs: Enhanced antioxidant activity and brain targeting in neurodegenerative models.

Evaluation Parameters

  • Particle Size and PDI: Affects absorption and tissue distribution.
  • Zeta Potential: Predicts stability of nanoparticles.
  • Entrapment Efficiency: Indicates drug loading efficiency.
  • In Vitro Release: Provides sustained release profiles.
  • Pharmacokinetics (PK): Assessed via AUC, Cmax, t½ in animal models or human trials.

Advantages of Nanoformulations

  • Improved bioavailability and dose reduction
  • Enhanced patient compliance due to reduced dosing frequency
  • Better targeting to specific tissues or organs
  • Protection from degradation in the GI tract
  • Potential for parenteral and transdermal applications

Regulatory and Commercial Considerations

  • GRAS Excipients: Must use safe, biocompatible materials
  • Scale-up Challenges: Reproducibility and cost are hurdles
  • Patent Landscape: Many phytosomal and nano-herbal technologies are patented
  • Marketed Products:
    • Meriva® (Curcumin)
    • Siliphos® (Silymarin)
    • Quercevita® (Quercetin)

CONCLUSION

Advanced formulation techniques such as phytosomes and nanoparticles offer a promising future for overcoming the bioavailability barriers associated with herbal medicines. By combining traditional phytotherapy with modern delivery systems, these strategies enhance therapeutic efficacy, improve safety, and support the global integration of herbal drugs into mainstream healthcare.

References

  1. Bombardelli E, et al. Phytosome: New cosmetic delivery system. Fitoterapia. 1991;62(5):387â??401.
  2. Yadav S, et al. Nanoformulations of herbal drugs: Recent advances. J Pharm Investig. 2020;50(5):487â??508.
  3. Maiti K, et al. Enhanced therapeutic benefit of quercetinâ??phospholipid complex. AAPS PharmSciTech. 2007;8(2):E1â??E7.
  4. Sharma A, et al. Lipid-based nanocarriers for enhancing bioavailability of herbal drugs. J Control Release. 2015;193:64â??76.
  5. Bhattacharya S. Phytosomes: Emerging strategy for delivery of herbal bioactives. Iran J Pharm Res. 2019;18(1):1â??15.