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Development of lipoprotein-drug conjugates for targeted drug delivery

Manish S Bhatia1, Sujata P Choudhari1, Rakesh P Dhavale1

  • 1Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of Pharmacy, Kolhapur, India.

Journal of Biomolecular Structure & Dynamics
|August 14, 2020
PubMed

Insights

Researchers developed a targeted drug delivery system using synthesized lipoproteins for cancer chemotherapy. This novel approach enhances drug uptake and significantly inhibits cancer cell growth, offering a promising alternative to conventional methods.

Area of Science:

  • Biomedical Engineering
  • Nanotechnology
  • Pharmacology

Background:

  • Conventional chemotherapy faces limitations due to systemic toxicity and poor drug localization.
  • Targeted drug delivery systems aim to improve therapeutic efficacy and reduce side effects.
  • Lipoproteins offer a potential platform for localized and protected drug interaction with diseased tissues.

Purpose of the Study:

  • To develop an anticancer targeted drug delivery system using synthesized lipoproteins.
  • To integrate a quality by design (QbD) approach for optimizing lipoprotein-based drug delivery.
  • To evaluate the efficacy of synthesized lipoproteins in enhancing cellular drug uptake and cytotoxicity against cancer cells.

Main Methods:

  • Lipoprotein structures were designed and optimized using a quality by design approach.
  • Synthesized lipoproteins were characterized for physicochemical properties.
  • Drug-lipoprotein physical composites (tablets) and chemical conjugates were prepared and evaluated.
  • Cellular drug uptake and cytotoxicity studies were performed on HaCaT cancer cells.

Main Results:

  • Synthesized lipoproteins exhibited good swelling capacity but poor flowability.
  • Spectroscopic analysis confirmed the successful synthesis of drug-lipoprotein conjugates.
  • Tablets demonstrated sustained drug release for up to 12 hours.
  • Synthesized conjugates significantly improved cellular drug uptake (up to 86.1%) and cancer cell inhibition (87.39%).

Conclusions:

  • Synthesized lipoproteins show potential as a drug delivery vehicle for anticancer formulations.
  • The developed targeted delivery system effectively enhances drug efficacy against HaCaT cancer cells.
  • This approach offers a promising strategy to overcome limitations of conventional chemotherapy.
Keywords:
Lipoproteindrug-lipoprotein conjugateimmortalized human HaCaT keratinocytetargeted drug delivery

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