24 May 2024 | Matthew S. Gatto, McNeely P. Johnson and Wided Najahi-Missaoui
Liposomal drug delivery is a promising approach in pharmaceutical sciences for targeted therapy. Liposomes, spherical vesicles with a phospholipid bilayer, are effective for delivering drugs due to their low immunogenicity, versatility, and documented efficacy. Since the approval of Doxil in 1995, liposomes have been widely used in treating various diseases, including cancer, infections, and pain. However, challenges remain in optimizing their performance.
Passive targeting mechanisms, such as the Enhanced Permeation and Retention (EPR) effect, allow liposomes to accumulate in tumor tissues due to leaky vasculature. PEGylation enhances liposomal circulation by reducing recognition by the mononuclear phagocyte system (MPS), but repeated use may lead to the accelerated blood clearance (ABC) phenomenon, reducing efficacy. Active targeting involves conjugating ligands, antibodies, peptides, or aptamers to liposomes to enhance specificity. Antibodies, peptides, folate, and aptamers have been explored for targeted delivery, though challenges remain in clinical translation.
pH-sensitive and temperature-sensitive liposomes offer site-specific drug release. pH-sensitive liposomes release drugs in acidic tumor environments, while temperature-sensitive liposomes release drugs upon heating. These strategies improve drug delivery efficiency and reduce off-target effects.
Despite progress, challenges include long-term stability, regulatory hurdles, and the need for optimized formulations. Storage issues, such as aggregation, can affect liposome integrity. Additionally, the FDA's regulatory framework needs to keep pace with advancements in targeted liposomal therapies.
In conclusion, liposomes are a versatile platform for targeted drug delivery, with ongoing research aimed at improving their efficacy, safety, and clinical application. Continued investment and innovation are essential to overcome current challenges and realize the full potential of targeted liposomal therapies.Liposomal drug delivery is a promising approach in pharmaceutical sciences for targeted therapy. Liposomes, spherical vesicles with a phospholipid bilayer, are effective for delivering drugs due to their low immunogenicity, versatility, and documented efficacy. Since the approval of Doxil in 1995, liposomes have been widely used in treating various diseases, including cancer, infections, and pain. However, challenges remain in optimizing their performance.
Passive targeting mechanisms, such as the Enhanced Permeation and Retention (EPR) effect, allow liposomes to accumulate in tumor tissues due to leaky vasculature. PEGylation enhances liposomal circulation by reducing recognition by the mononuclear phagocyte system (MPS), but repeated use may lead to the accelerated blood clearance (ABC) phenomenon, reducing efficacy. Active targeting involves conjugating ligands, antibodies, peptides, or aptamers to liposomes to enhance specificity. Antibodies, peptides, folate, and aptamers have been explored for targeted delivery, though challenges remain in clinical translation.
pH-sensitive and temperature-sensitive liposomes offer site-specific drug release. pH-sensitive liposomes release drugs in acidic tumor environments, while temperature-sensitive liposomes release drugs upon heating. These strategies improve drug delivery efficiency and reduce off-target effects.
Despite progress, challenges include long-term stability, regulatory hurdles, and the need for optimized formulations. Storage issues, such as aggregation, can affect liposome integrity. Additionally, the FDA's regulatory framework needs to keep pace with advancements in targeted liposomal therapies.
In conclusion, liposomes are a versatile platform for targeted drug delivery, with ongoing research aimed at improving their efficacy, safety, and clinical application. Continued investment and innovation are essential to overcome current challenges and realize the full potential of targeted liposomal therapies.