Biodegradable Nanoparticles-Loaded PLGA Microcapsule for the Enhanced Encapsulation Efficiency and Controlled Release of Hydrophilic Drug

Abstract

Recently, nano- and micro-particulate systems have been widely utilized to deliver pharmaceutical compounds to achieve enhanced therapeutic effects and reduced side effects. Poly (DL-lactide-co-glycolide) (PLGA), as one of the biodegradable polyesters, has been widely used to fabricate particulate systems because of advantages including controlled and sustained release, biodegradability, and biocompatibility. However, PLGA is known for low encapsulation efficiency (%) and insufficient controlled release of water-soluble drugs. It would result in fluctuation in the plasma levels and unexpected side effects of drugs. Therefore, the purpose of this work was to develop microcapsules loaded with alginate-coated chitosan that can increase the encapsulation efficiency of the hydrophilic drug while exhibiting a controlled and sustained release profile with reduced initial burst release. The encapsulation of nanoparticles in PLGA microcapsules was done by the emulsion solvent evaporation method. The encapsulation of nanoparticles in PLGA microcapsules was confirmed by scanning electron microscopy and confocal microscopy. The release profile of hydrophilic drugs can further be altered by the chitosan coating. The chitosan coating onto alginate exhibited a less initial burst release and sustained release of the hydrophilic drug. In addition, the encapsulation of alginate nanoparticles and alginate nanoparticles coated with chitosan in PLGA microcapsules was shown to enhance the encapsulation efficiency of a hydrophilic drug. Based on the results, this delivery system could be a promising platform for the high encapsulation efficiency and sustained release with reduced initial burst release of the hydrophilic drug.

CD44/Folate Dual Targeting Receptor Reductive Response PLGA-Based Micelles for Cancer Therapy

“…Compared with them, the contact angle of PLGA was 98°, which was a hydrophobic substance ( Taubner et al, 2020 ). Therefore, PLGA copolymers with more lactic acid components have low hydrophilicity ( Wang et al, 2005 ), ( Ryu et al, 2021 ). The ratio of PLGA lactic acid to glycolic acid used in this experiment was 75:25, which was confirmed to be hydrophobic by measurement.…”

Physical, Chemical, and Biological Properties of Chitosan-Coated Alginate Microparticles Loaded with Porcine Interleukin-1β: A Potential Protein Adjuvant Delivery System

“…Our electrosprayed alginate MPs were also coated with 1% ( w / v ) chitosan, which facilitated electrostatic interactions that may meet the requirements for prolonging pIL-1β release. Additionally, a chitosan coating on alginate has been shown to facilitate more sustained release of a hydrophilic drug with a lesser initial burst release [ 25 ]. In our present study, the pIL-1β, which is hydrophilic, that had been encapsulated in chitosan-coated alginate MPs was released in a relatively slow, sustained manner, with a reduced initial burst of release.…”

“…Nevertheless, the potential for prolonged drug release from sodium alginate particles is still limited owing to sodium alginate’s solubility, which leads to rapid particle dissolution in vivo [ 24 ]. However, a copolymer such as chitosan can be used to coat alginate MPs to reduce the initial “burst” release of an encapsulated drug or antigen [ 25 ]. Chitosan is a naturally occurring cationic polymer that is derived by deacetylating chitin in alkaline solution [ 26 ].…”

PLGA-Based Nanoparticles for Neuroprotective Drug Delivery in Neurodegenerative Diseases

“…Depending on the process used, amphiphilic, hydrophobic, or hydrophilic drugs can be either loaded inside the NP core, trapped among the polymer chains, or adsorbed on the NP surface (leading to burst release and potential off target effects). Even though a low encapsulation efficiency characterizes PLGA NPs, in particular for hydrophilic drugs, there is room for improvement by playing with the molecular weight (i.e., the higher the molecular weight, the larger the NPs) or the poly( d , l -lactic acid) (PLA)/poly ( d , l -glycolyc acid) (PGA) ratio [ 24 ]. The latter parameter is directly related to the crystallinity degree and the melting point of PLGA copolymers, and drives the capacity of polymers to undergo hydrolysis.…”