Development of Drug-Loaded PLGA Microparticles with Different Release Patterns for Prolonged Drug Delivery

Abstract

For the prolonged delivery and sustained release rates of low molecular weight drugs, poly(lactic-co-glycolic acid) (PLGA) microparticles containing the drug SKL-2020 have been investigated. On increasing polyvinyl alcohol (PVA) concentration (from 0.2% to 5%), the size of microparticles decreased (from 48.02 µm to 10.63 µm) and more uniform size distribution was noticeable due to the powerful emulsifying ability of PVA. A higher drug loading (from 5% to 20%) caused a larger concentration gradient between 2 phases at the polymer precipitation step; this resulted in decreased encapsulation efficiency (from 34.19% to 25.67%) and a greater initial burst (from 61.71% to 70.05%). SKL-2020-loaded PLGA microparticles prepared with different fabrication conditions exhibited unique release patterns of SKL-2020. High PVA concentration and high drug loading led to an initial burst effect by rapid drug diffusion through the polymer matrix. Since PLGA microparticles enabled the slow release of SKL-2020 over 1 week in vitro and in vivo, more convenient and comfortable treatment could be facilitated with less frequent administration. It is feasible to design a release profile by mixing microparticles that were prepared with different fabrication conditions. By this method, the initial burst could be repressed properly and drug release rate could decrease.

Scaffold-based lung tumor culture on porous PLGA microparticle substrates

“…All porous MPs developed in this work were in the diameter range of 19–42 μm, which indicates that sufficient surface area will be available for A549 growth, since previously published works have shown that A549 cells have an average diameter of 6–15 μm [59, 60]. The standard deviations observed is typical of PLGA microspheres prepared using low amounts of PVA surfactant, as observed by other groups [61–63]. Ideally, a pore diameter of 20 μm or greater is desirable for growth and infiltration of mammalian cells, while smaller pores provide adequate surface area for cell attachment on the surface [64, 65].…”

PLGA-Based Composites for Various Biomedical Applications

“…Nanotechnology brings unique characteristics to the system, which, in combination with PLGA's unique features, allow for extensive biomedical applications. It is possible to encapsulate both organic and inorganic materials into PLGA, such as small-molecule drugs [2,12], vaccines [13], proteins [14,15] and metallic [16] as well as magnetic [17,18] nanoparticles (NPs). The methods of production of PLGA-based materials can be adapted to various types of drugs, making it possible to encapsulate hydrophobic and hydrophilic molecules and thus making this copolymer an ideal drug delivery system (DDS) [4].…”

Recent advances in the formulation of PLGA microparticles for controlled drug delivery

“…As a drug delivery system, MPs offer many advantages such as the use of different administration routes or the opportunity of encapsulating different molecules including proteins (Ospina-Villa et al 2019 ) and nucleic acid (McKiernan et al 2018 ). In particular, MPs can be used for the controlled release of drugs (Choi et al 2011 ; Guo et al 2015 ) that can be modulated by choosing the kind of polymer and its chemical and molecular features such as molecular weight (MW), monomer composition (Takeuchi et al 2017 ), crystallinity, glass transition temperature ( T g ), and inherent viscosity (Ansary et al 2014 ). In this scenario, a lot of biodegradable polymers can be used to formulate MPs as alginate (Strobel et al 2020 ), dextran (Shah et al 2019 ), chitosan (Batista et al 2019 ), gelatin (da Silva and Pinto et al 2019 ) and poly-(lactic- co -glycolic acid) (PLGA) (Kapoor et al 2015 ).…”