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Controlled release and targeted drug delivery with poly(lactic-co-glycolic acid) nanoparticles: reviewing two decades of research

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Abstract

Background

Controlled release and targeted delivery of the drug payload are the two most fascinating applications of nanoparticle-based systems explored in the recent past. The advantages of achieving control over drug release kinetics include prolonged therapeutic effects, reduced dosing frequency, and fewer plasma level fluctuations and side effects, whereas targeted delivery offers enhanced drug accumulation at the site of action and reduced off-target toxicity, thereby improving the management of chronic diseases. Poly(lactic-co-glycolic acid) nanoparticles (PLGA-NPs) hold tremendous promise for such applications because of their ability to modulate drug release, pharmacokinetics, the biodistribution profiles of drugs, and the surface functionalization for targeted delivery.

Area covered

This review primarily highlights the applications of PLGA-NPs based on the controlled release of therapeutics after oral, parenteral, pulmonary, ocular, intranasal, and dermal administration and tissue engineering. The potential of PLGA-NPs for targeted delivery to various diseases, such as cancer, rheumatoid arthritis, inflammatory bowel disease, and neurological disorders, has also been extensively reviewed. This review concludes with a description of the limitations of PLGA-NPs and the hurdles associated with their clinical application.

Expert opinion

PLGA-NPs stand out among other nanoparticles because of their excellent biocompatibility and biodegradability. Although the presented data suggest that they are the major shareholders in controlled-release and targeted-delivery systems, no PLGA-NP formulation has reached clinics. Therefore, further insights into the rational design of PLGA-NPs and clinically relevant testing are required to narrow the gap between the bench and bedside realities.

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Acknowledgements

This work was supported by the Basic Science Research Program of the National Research Foundation of Korea (NRF) funded by the Ministry of Science, ICT & Future Planning (NRF-2021R1F1A1060378), and Ministry of Education (NRF-2020R1A6A1A03043708). It was also supported by the Korea Drug Development Fund funded by the Ministry of Science and ICT, Ministry of Trade, Industry, and Energy, and Ministry of Health and Welfare (HN21C1258, Republic of Korea).

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  1. College of Pharmacy, Gachon University, 191 Hambakmoe-ro, Yeonsu-gu, Incheon, 21936, Republic of Korea

    Alam Zeb, Thi-Thao-Linh Nguyen & Han-Joo Maeng

  2. Riphah Institute of Pharmaceutical Sciences, Riphah International University, Islamabad, 44000, Pakistan

    Alam Zeb & Maleeha Gul

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Zeb, A., Gul, M., Nguyen, TTL. et al. Controlled release and targeted drug delivery with poly(lactic-co-glycolic acid) nanoparticles: reviewing two decades of research. J. Pharm. Investig. 52, 683–724 (2022). https://doi.org/10.1007/s40005-022-00584-w

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