Engineering Microenvironment of Biodegradable Polyester Systems for Drug Stability and Release Control

Abstract

Polymeric systems made of poly(lactic acid) or poly(lactic-co-glycolic acid) are widely used for long-term delivery of small and large molecules. The advantages of poly(lactic acid)/poly(lactic-co-glycolic acid) systems include biodegradability, safety and a long history of use in US FDA-approved products. However, as drugs delivered by the polymeric systems and their applications become more diverse, the significance of microenvironment change of degrading systems on long-term drug stability and release kinetics has gained renewed attention. In this review, we discuss various issues experienced with acidifying microenvironment of biodegradable polymer systems and approaches to overcome the detrimental effects of polymer degradation on drug stability and release control.

Long‐Acting Microparticle Formulation of Griseofulvin for Ocular Neovascularization Therapy

“…Specifically, we included inorganic salts to modify the microenvironment of PLGA MPs and control the drug transport. [ 27 ] Three salts with different basicity and water solubility (Table S1, Supporting Information), Mg(OH) 2, Mg 3 (PO 4 ) 2 , and NaCl, were tested for their effects on the initial burst release, K lag , and MDA.…”

“…Poly(lactide-co-glycolide) (PLGA) was explored as a carrier of GRF due to commercial availability, biodegradability, safety, and the track record in commercial longacting release (LAR) products as microparticles (MPs), implants, or in situ gels. [26,27] PLGA-based LAR approaches are clinically relevant because several implants (e.g., Ozurdex, Zoladex, and Propel Durysta), microparticles (e.g., Sandostatin LAR, Lupron Depot, Nutropin Depot, sunitinib microparticles), and in situ gels (Eligard, Sublocade, Perseris, and Atridox) are used for local drug delivery. [4,[27][28][29] Here, we report on the design, production, and evaluation of GRF-loaded PLGA MPs.…”

“…[26,27] PLGA-based LAR approaches are clinically relevant because several implants (e.g., Ozurdex, Zoladex, and Propel Durysta), microparticles (e.g., Sandostatin LAR, Lupron Depot, Nutropin Depot, sunitinib microparticles), and in situ gels (Eligard, Sublocade, Perseris, and Atridox) are used for local drug delivery. [4,[27][28][29] Here, we report on the design, production, and evaluation of GRF-loaded PLGA MPs. The MPs were engineered to release the GRF for at least 1 month.…”

“…[ 26,27 ] PLGA‐based LAR approaches are clinically relevant because several implants (e.g., Ozurdex, Zoladex, and Propel Durysta), microparticles (e.g., Sandostatin LAR, Lupron Depot, Nutropin Depot, sunitinib microparticles), and in situ gels (Eligard, Sublocade, Perseris, and Atridox) are used for local drug delivery. [ 4,27–29 ]…”

Synthesis of full bio‐based, fast degradable, and high strength copolyesters: Poly(butylene succinate‐sebacicate‐salicylicate‐malicate)

“…However, their widespread use has also resulted in significant environmental pollution primarily due to their nonbiodegradability 1–3 . To address this issue, the development of biodegradable plastics with desirable mechanical properties emerges as a viable solution to replace fossil‐based materials 4–6 . Biodegradable polyester materials, as an ideal alternative to fossil‐based polymers, have aroused extensive research interest due to their excellent biodegradability, biocompatibility, and melt processing properties, offering effective solutions to combat the issue of nondegradable waste, often referred to as “white pollution.” 7,8 Many biodegradable polyesters are developed and applied in food packing films, agricultural mulch, and so forth 9–12 .…”