Advancements in Betulinic Acid-Loaded Nanoformulations for Enhanced Anti-Tumor Therapy

Int J Nanomedicine. 2024 Dec 29:19:14075-14103. doi: 10.2147/IJN.S493489. eCollection 2024.

Abstract

Betulinic acid (BA) is a natural compound obtained from plant extracts and is known for its diverse pharmacological effects, including anti-tumor, antibacterial, anti-inflammatory, antiviral, and anti-atherosclerotic properties. Its potential in anti-tumor therapy has garnered considerable attention, particularly for the treatment of breast, lung, and liver cancers. However, the clinical utility of BA is greatly hindered by its poor water solubility, low bioavailability, and off-target toxicity. To address these issues, researchers have developed various BA-loaded nanoformulations, such as nanoparticles, liposomes, micelles, and nanofibers, aiming to improve its solubility and bioavailability, prolong plasma half-life, and enhance targeting ability, thereby augmenting its anti-cancer efficacy. In preparing this review, we conducted extensive searches in well-known databases, including PubMed, Web of Science, and ScienceDirect, using keywords like "betulinic acid", "nanoparticles", "drug delivery", "tumor", and "cancer", covering the literature from 2014 to 2024. The review provides a comprehensive overview of recent advancements in the application of BA-loaded nano-delivery systems for anti-tumor therapy and offers insights into their future development prospects.

Keywords: anti-tumor; betulinic acid; bioavailability; nanoformulations; targeting.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacokinetics
  • Betulinic Acid*
  • Biological Availability
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods
  • Humans
  • Liposomes / chemistry
  • Micelles
  • Nanoparticles* / chemistry
  • Neoplasms* / drug therapy
  • Pentacyclic Triterpenes*
  • Solubility
  • Triterpenes* / administration & dosage
  • Triterpenes* / chemistry
  • Triterpenes* / pharmacokinetics
  • Triterpenes* / pharmacology

Substances

  • Betulinic Acid
  • Pentacyclic Triterpenes
  • Triterpenes
  • Antineoplastic Agents
  • Liposomes
  • Drug Carriers
  • Micelles

Grants and funding

This work was supported by the Luzhou Municipal People’s Government-Southwest Medical University Science and Technology Strategic Cooperation Project [grant number 2023LZXNYDJ004] and the National Natural Science Foundation of China [grant number 82104083].