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Resveratrol loaded functionalized nanostructured lipid carriers for breast cancer targeting: Systematic development,

Neelam Poonia1, Jasjeet Kaur Narang2, Viney Lather3

  • 1Department of Pharmaceutics, Jan Nayak Ch. Devi Lal Memorial College of Pharmacy, Sirsa, 125055, Haryana, India; I. K. Gujral Punjab Technical University, Jalandhar, Punjab, India.

Colloids and Surfaces. B, Biointerfaces
|June 25, 2019
PubMed

Insights

This study developed targeted nanostructured lipid carriers (NLCs) to improve resveratrol (RSV) delivery for breast cancer. Folate-modified RSV-NLCs demonstrated enhanced cytotoxicity and improved pharmacokinetic profiles, highlighting their therapeutic potential.

Area of Science:

  • Nanotechnology
  • Pharmaceutical Sciences
  • Oncology

Background:

  • Resveratrol (RSV) exhibits anti-cancer properties but faces challenges like poor solubility and limited bioavailability.
  • Developing effective delivery systems is crucial for enhancing RSV's therapeutic efficacy in cancer treatment.

Purpose of the Study:

  • To formulate and optimize nanostructured lipid carriers (NLCs) for parenteral delivery of resveratrol (RSV).
  • To enhance RSV delivery to breast cancer cells using targeted NLCs.
  • To evaluate the in vitro and in vivo performance of optimized RSV-loaded NLCs.

Main Methods:

  • RSV-loaded NLCs (RSV-NLCs) were prepared using a modified solvent injection technique.
  • Formulation optimization was performed using a Box-Behnken design.
  • Targeting was achieved by conjugating folic acid (FA) to NLCs (RSV-FA-NLCs).
  • In vitro cytotoxicity and in vivo pharmacokinetic studies were conducted.

Main Results:

  • Optimized RSV-NLCs showed a particle size of 88.3 nm and high entrapment efficiency (88.0%).
  • Folate-modified RSV-FA-NLCs exhibited significantly higher cytotoxicity against MCF-7 breast cancer cells compared to unmodified RSV-NLCs.
  • In vivo studies revealed a nine-fold increase in AUC for RSV-FA-NLCs versus free RSV.

Conclusions:

  • Targeted NLCs effectively enhance the delivery and therapeutic potential of resveratrol.
  • Folate-targeted RSV-NLCs represent a promising strategy for improving breast cancer treatment.
  • Lipidic nanocarriers show significant potential for augmenting the efficacy of poorly soluble drugs like RSV.
Keywords:
Breast cancerNanostructured lipid carriersOptimizationResveratrolTargeting

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