Long-acting parenteral formulations of hydrophilic drugs, proteins, and peptide therapeutics: mechanisms, challenges, and therapeutic benefits with a focus on technologies

Abstract

Despite being the most widely prescribed formulation, oral formulations possess several limitations such as low adherence, low bioavailability, high toxicity (in the case of anticancer drugs), and multiple-time administration requirements. All these limitations can be overcome by long-acting injectables. Improved adherence, patient compliance, and reduced relapse have been observed with long-acting formulation which has increased the demand for long-acting injectables. Drugs or peptide molecules with oral bioavailability issues can be easily delivered by long-acting systems. This review comprehensively addresses the various technologies used to develop long-acting injections with a particular focus on hydrophilic drugs and large molecules as well as the factors affecting the choice of formulation strategy. This is the first review that discusses the possible technologies that can be used for developing long-acting formulations for hydrophilic molecules along with factors which will affect the choice of the technology. Furthermore, the mechanism of drug release as well as summaries of marketed formulations will be presented. This review also discusses the challenges associated with the manufacturing and scale-up of the long-acting injectables. Graphical abstract

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