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Updated: Aug 11, 2025
Preparation and Characterization of Lipophilic Doxorubicin Pro-drug Micelles
Published on: August 2, 2016
Recent advances in long-acting drug delivery systems for anticancer drug
Catarina Pacheco1, Ana Baião2, Tao Ding3
1i3S - Instituto de Investigação e Inovação em Saúde, Universidade do Porto, Rua Alfredo Allen 208, 4200-135 Porto, Portugal; INEB - Instituto de Engenharia Biomédica, Universidade do Porto, Rua Alfredo Allen 208, 4200-135 Porto, Portugal; IUCS - Instituto Universitário de Ciências da Saúde, CESPU, Rua Central de Gandra 1317, 4585-116 Gandra, Portugal.
Abstract:
The use of systemic anticancer chemotherapy is intrinsically limited by its toxicity. Whether dealing with small molecules or biopharmaceuticals, after systemic administration, small doses fail to reach effective intratumoral concentrations, while high doses with significant tumor inhibition effects may also drive the death of healthy cells, endangering the patients. Therefore, strategies based on drug delivery systems (DDSs) for avoiding the systemic toxicity have been designed. Due to their ability to protect drugs from early elimination and control drug release, DDSs can foster tumor exposure to anticancer therapeutics by extending their circulation time or steadily releasing drugs into the tumor sites. However, approval of tailored DDSs systems for clinical use is minimal as the safety and the in vivo activity still need to be ameliorated by manipulating their physicochemical characteristics. During the last few years, several strategies have been described to improve their safety, stability, and fine-tune pharmaceuticals release kinetics. Herein, we reviewed the main DDSs, namely polymeric conjugates, nano or microparticles, hydrogels, and microneedles, explored for long-acting anticancer treatments, highlighting recently proposed modifications and their potential advantages for different anticancer therapies. Additionally, important limitations of long-acting anticancer therapies and future technology directions were also covered.
Insights
Drug delivery systems (DDSs) offer a promising strategy to enhance anticancer chemotherapy efficacy by minimizing systemic toxicity. These systems protect drugs and control their release, improving tumor drug concentrations and patient safety.
Area of Science:
- Oncology
- Nanotechnology
- Pharmaceutical Sciences
Background:
- Systemic anticancer chemotherapy is limited by toxicity, with suboptimal drug concentrations at tumor sites or severe side effects from high doses.
- Drug delivery systems (DDSs) are being developed to overcome these limitations by protecting drugs and controlling their release.
Purpose of the Study:
- To review main DDSs for long-acting anticancer treatments.
- To highlight recent modifications and their advantages.
- To discuss limitations and future directions in long-acting anticancer therapies.
Main Methods:
- Review of literature on DDSs including polymeric conjugates, nanoparticles, microparticles, hydrogels, and microneedles.
- Analysis of strategies to improve DDS safety, stability, and drug release kinetics.
- Discussion of in vivo activity and clinical translation challenges.
Main Results:
- DDSs can extend drug circulation time and provide sustained release, improving intratumoral drug concentrations.
- Various DDS strategies show potential for enhanced anticancer efficacy and reduced systemic toxicity.
- Clinical approval of tailored DDSs remains limited due to safety and in vivo activity concerns.
Conclusions:
- DDSs represent a key strategy for developing safer and more effective long-acting anticancer therapies.
- Further research into physicochemical characteristics is needed to optimize DDS performance and clinical translation.
- Future directions include innovative DDS designs and improved understanding of their in vivo behavior.
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