Long acting injectable formulations: the state of the arts and challenges of poly(lactic-co-glycolic acid) microsphere, hydrogel, organogel and liquid crystal
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Long-acting injectable formulations (LAIFs) have received substantial attention recently due to their advantages over conventional formulations, including easy administration, continuous and controlled release of drug over months, and the ability to maintain drug concentrations within the therapeutic range. The constant advances in biotechnology produce complex active pharmaceuticals that might be difficult to administer by conventional means. In particular, peptides, proteins, and antibodies are hard to administer orally given their physicochemical instability in the gastrointestinal tract and short half lives in blood. Therefore, LAIFs are a good candidate delivery system for such drugs. LAIFs reduce the frequency of application and improve patient compliance. For instance, LAIF-based antipsychotics can be more effective in patients with bipolar disorder and schizoaffective disorder.
This review provides an overview of the various drug delivery technologies using LAIFs. Poly (lactic-co-glycolic acid) microspheres, hydrogels, organogels, and liquid crystals were chosen as representative LAIFs, and their preparation methods, advantages, limitations, challenges, and prospects are discussed.
LAIFs are an attractive delivery system for bio-macromolecules that might participate in the new drug paradigm in the future. While each LAIF-based delivery technology has its own unique advantages, there are still some limitations that need to be overcome, and studies are being performed to understand and address these limitations.
KeywordsPoly (lactic-co-glycolic acid) Microsphere Hydrogel Organogel Liquid crystal Long acting injection
This work was supported by the Basic Science Research Program of the National Research Foundation of Korea (NRF) funded by the Ministry of Education (NRF-2018R1D1A1B07045240).
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Conflict of interest
The authors report no conflicts of interest in this work.
Statement of human and animal rights
This article does not contain any studies with human or animal subjects performed by any of the authors.
- Engstrom S (1990) Drug delivery from cubic and other lipid–water phases. Lipid Technol 2:42–45Google Scholar
- Garg T, Bilandi A, Kapoor B, Kumar S, Joshi R (2011) Organogels: advanced and novel drug delivery system. Int Res J Pharm 2(12):15–21Google Scholar
- Kazazi-Hyseni F, Landin M, Lathuile A, Veldhuis GJ, Rahimian S, Hennink WE, Kok RJ, van Nostrum CF (2014) Computer modeling assisted design of monodisperse PLGA microspheres with controlled porosity affords zero order release of an encapsulated macromolecule for 3 months. Pharm Res 31:2844–2856CrossRefPubMedGoogle Scholar
- Makino K, Nakajima T, Shikamura M, Ito F, Ando S, Kochi C, Inagawa H, Soma G, Terada H (2004) Efficient intracellular delivery of rifampicin to alveolar macrophages using rifampicin-loaded PLGA microspheres: effects of molecular weight and composition of PLGA on release of rifampicin. Colloids Surf B Biointerfaces 36:35–42CrossRefPubMedGoogle Scholar
- Mank R, Rafler G, Nerlich B (1991) Parenterale depotarzneiformen auf der Basis von biologisch abbaubaren Polymeren. Phamazie 46:9–17Google Scholar
- Petersen H, Ahlheimer M (2007) Sustained release formulation comprising octreotide and two or more polylactide-co-glycolide polymers. International Publication WO 2007/071395Google Scholar
- Sahoo S, Kumar N, Bhattacharya C, Sagiri SS, Jain K, Pal K, Ray SS, Nayak B (2012) Organogels: Properties and applications in drug delivery. Des Monomers Polym 14(2):95–108Google Scholar