Long-Acting Injectable Drug Delivery Systems
Summary
Long-acting injectable formulations are designed to maintain therapeutic drug concentrations over extended periods—from weeks to months—following a single administration. By forming a depot at the injection site, these systems minimise peak-to-trough fluctuations and reduce dosing frequency, thereby improving patient adherence and clinical outcomes. Diverse materials, including biodegradable polymers, lipids and drug crystals, serve as matrices or vehicles that modulate release through mechanisms such as diffusion, degradation or enzymatic conversion of prodrugs. Key design parameters encompass particle size, surface characteristics, solubility, depot rheology and biocompatibility. Technological advances in nanotechnology, solvent-based crystallisation and self-assembling prodrug strategies have expanded the repertoire of injectable platforms, enabling tailored release profiles and enhanced stability. Applications span psychiatry (antipsychotics), infectious diseases (antivirals, antibiotics) and hormonal therapies, with growing interest in oncology and vaccine delivery. Manufacturing innovations—such as continuous processing and microfluidic control—facilitate scalable production with consistent quality. In parallel, mechanistic modelling and simulation inform formulation optimisation and accelerate regulatory assessment. Together, these developments underscore the global significance of long-acting injectables as a means to improve therapeutic efficacy, safety and patient quality of life.
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Long-Acting Injectable Drug Delivery Systems publication trend
The graph below shows the total number of articles in long-acting injectable drug delivery systems across all publications each year (not limited to Nature Index journals).
Technical terms
Depot: A localised reservoir of drug at the injection site that gradually releases active compound over time.
Prodrug: A pharmacologically inactive molecule that is metabolised into its active form in the body.
Nanosuspension: A colloidal dispersion of drug nanoparticles stabilised in a liquid medium to enhance solubility and control release.
Antisolvent crystallisation: A bottom-up technique in which a non-solvent is added to a solvent containing dissolved drug to precipitate fine crystals.
Esterase: An enzyme that cleaves ester bonds, often responsible for converting prodrugs into their active forms.
References
- Novel pH‐Responsive Structural Rearrangement of Myristic Acid‐Conjugated Quetiapine Nanosuspension for Enhanced Long‐Acting Delivery Performance. Advanced Science (2024).
- Role of Modeling and Simulation in Preclinical and Clinical Long-Acting Injectable Drug Development. The AAPS Journal (2023).
- Continuous Microfluidic Antisolvent Crystallization as a Bottom-Up Solution for the Development of Long-Acting Injectable Formulations. Pharmaceutics (2024).
- Tricaprylin‐based drug crystalline suspension for intramuscular long‐acting delivery of entecavir with alleviated local inflammation. Bioengineering & Translational Medicine (2024).
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