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Bioavailability Enhancement: Drug Solubility Enhancement01:16

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Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
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Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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Drug Delivery: Overview01:16

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Manufacture and Drug Delivery Applications of Silk Nanoparticles
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Potential Enhancement of Topical Drug Delivery Using Grapefruit-derived Nanoparticles Modified Using TAT Peptide.

Risa Kanai1, Tomohiro Seki1, Tomona Yukimura1

  • 1Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado, Saitama, 350-0295, Japan.

Pharmaceutical Research
|January 21, 2026
PubMed
Summary

Surface modification of grapefruit-derived nanoparticles (GNPs) with stearylated Tat-peptide (STR-Tat) enhanced skin penetration. This method improves the delivery of nucleic acids via plant-derived nanoparticles (PdNPs) without significant cell toxicity.

Keywords:
Cell penetration peptidePlant-derived nanoparticlesSkin penetrationSurface modificationTat-peptide

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Area of Science:

  • Biomaterials Science
  • Nanotechnology
  • Dermal Drug Delivery

Background:

  • Plant-derived nanoparticles (PdNPs) show promise for nucleic acid delivery, particularly for transdermal applications.
  • Enhancing the skin penetration of PdNPs is crucial for effective transdermal delivery.
  • Cell penetration peptides (CPPs), such as the Tat-peptide, can facilitate cellular uptake and skin penetration.

Purpose of the Study:

  • To evaluate the feasibility of enhancing skin penetration of grapefruit-derived nanoparticles (GNPs) using surface modification with stearylated Tat-peptide (STR-Tat).
  • To assess the impact of STR-Tat modification on GNP properties, cellular uptake, and skin penetration.
  • To determine the potential of STR-Tat modified GNPs for transdermal nucleic acid delivery.

Main Methods:

  • GNP surface modification with synthesized STR-Tat via simple mixing.
  • Measurement of particle size and zeta potential of modified GNPs (STR-Tat-GNPs).
  • In vivo skin penetration studies on mouse models, alongside in vitro cellular uptake and toxicity assays.

Main Results:

  • STR-Tat-GNPs exhibited a positive zeta potential, contrasting with the negative zeta potential of unmodified GNPs.
  • Enhanced cellular uptake was observed for STR-Tat-GNPs with minimal cytotoxicity.
  • In vivo studies showed significant penetration of DiI-labeled STR-Tat-GNPs into hair follicles and deeper dermal layers.

Conclusions:

  • Simple STR-Tat surface modification effectively enhances the skin penetration of GNPs.
  • This approach improves the delivery of lipophilic substances via GNPs without inducing significant cellular toxicity.
  • STR-Tat modified GNPs represent a promising strategy for developing plant-derived nanoparticles with high skin penetration ability for nucleic acid delivery.