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Updated: Jan 5, 2026

Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Stereocomplexed PLA microspheres: Control over morphology, drug encapsulation and anticancer activity
M Brzeziński1, B Kost1, S Wedepohl2
1Centre of Molecular and Macromolecular Studies, Polish Academy of Sciences, Sienkiewicza 112, 90-363 Lodz, Poland.
Abstract:
Lung cancer is the leading cause of cancer death because of smoking and air pollution. Therefore, new ideas should be provided for lung cancer treatment in which the delivery of anticancer drugs to the local tumor site can be achieved. For this purpose, we propose the use of stereocomplexed spherical microspheres with sizes between 0.5 and 10 μm loaded with doxorubicin (DOX) to be administered through the nasal route. In order to gain control over the microsphere morphology, size, and drug loading capacity, we systematically studied the influence of the solvent used for preparation and the functionalization of their building blocks, namely poly-l-lactide (PLLA) and poly-d-lactide (PDLA) with blocked or unblocked l-proline moieties. We could demonstrate that DOX release is generally determined by the size of the microspheres. The antiproliferative activity of DOX released from the different microspheres was shown in vitro using the A549 lung cancer cell line as a model. Moreover, when in direct contact to the cancer cells, smaller microspheres were uptaken and could serve as a reservoir for local drug release. Our findings not only provide a novel strategy to prepare PLA microspheres with controllable morphology and release of anti-cancer drugs but also offer additional possibilities for the application of stereocomplexed particles in anticancer therapy, with suitable sizes for nasal administration.
Insights
Novel stereocomplexed microspheres offer a new approach for lung cancer treatment. These drug-loaded particles, administered nasally, show controlled release and antiproliferative activity against cancer cells.
Area of Science:
- Biomaterials Science
- Nanotechnology
- Oncology
Background:
- Lung cancer remains a leading cause of cancer mortality, necessitating innovative treatment strategies.
- Effective local delivery of anticancer drugs to tumor sites is crucial for improving therapeutic outcomes.
- Current treatments face challenges in targeted drug delivery and minimizing systemic toxicity.
Purpose of the Study:
- To develop and characterize stereocomplexed poly(lactic acid) microspheres for nasal delivery of doxorubicin (DOX) in lung cancer therapy.
- To investigate the influence of preparation methods and material functionalization on microsphere properties and drug release kinetics.
- To evaluate the in vitro antiproliferative efficacy of DOX-loaded microspheres against lung cancer cells.
Main Methods:
- Preparation of stereocomplexed poly(l-lactide) (PLLA) and poly(d-lactide) (PDLA) microspheres loaded with doxorubicin (DOX).
- Systematic study of solvent effects and l-proline functionalization on microsphere morphology, size (0.5–10 μm), and drug loading.
- In vitro assessment of DOX release profiles and antiproliferative activity using the A549 lung cancer cell line.
Main Results:
- Microsphere size was identified as a key determinant of doxorubicin (DOX) release rate.
- Smaller microspheres demonstrated enhanced uptake by A549 lung cancer cells, acting as local drug reservoirs.
- DOX released from the microspheres exhibited significant in vitro antiproliferative activity against the tested cancer cell line.
Conclusions:
- Stereocomplexed PLA microspheres provide a controllable platform for local anticancer drug delivery via the nasal route.
- The size-tunable nature of these microspheres allows for tailored drug release and enhanced cellular interaction.
- This approach presents a promising strategy for developing novel lung cancer therapies with improved localized drug delivery.
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