Tunable Release of Curcumin with an In Silico-Supported Approach from Mixtures of Highly Porous PLGA Microparticles

Abstract

In recent years, drug delivery systems have become some of the main topics within the biomedical field. In this scenario, polymeric microparticles (MPs) are often used as carriers to improve drug stability and drug pharmacokinetics in agreement with this kind of treatment. To avoid a mere and time-consuming empirical approach for the optimization of the pharmacokinetics of an MP-based formulation, here, we propose a simple predictive in silico-supported approach. As an example, in this study, we report the ability to predict and tune the release of curcumin (CUR), used as a model drug, from a designed combination of different poly(d,l-lactide-co-glycolide) (PLGA) MPs kinds. In detail, all CUR–PLGA MPs were synthesized by double emulsion technique and their chemical–physical properties were characterized by Mastersizer and scanning electron microscopy (SEM). Moreover, for all the MPs, CUR encapsulation efficiency and kinetic release were investigated through the UV–vis spectroscopy. This approach, based on the combination of in silico and experimental methods, could be a promising platform in several biomedical applications such as vaccinations, cancer-treatment, diabetes therapy and so on.

Engineered PLGA-PVP/VA based formulations to produce electro-drawn fast biodegradable microneedles for labile biomolecule delivery

“…In particular, to obtain a fast protein release kinetics, we studied 14 different emulsion formulations, analyzing consequent MN porous structure as well as the entrapment efficiency, release profiles and activity of collagenase (Table 1 ). We started from emulsions containing PLGA polymer 50: 50 (20% w/v) dissolved in 1 mL of dimethyl carbonate (DMC) and 200 µL of collagenase-488with the addition of 7.5% of ammonium bicarbonate (Table 1 , case c1), which was previously used for the fabrication of porous microparticles for drug delivery (Di Natale et al 2020 ). Needle microstructures were observed by confocal microscopy and ammonium bicarbonate showed to produce low size pores, with diameters of 1.5 ± 0.6 μm (Fig.…”

Design of biodegradable bi-compartmental microneedles for the stabilization and the controlled release of the labile molecule collagenase for skin healthcare

“…S1A and B, ESI †) according to a previously reported method used for curcumin. 13 The internal water phase, composed of 100 mL of collagenase-488 at a concentration of 0.5 mg mL À1 was homogenized with 100 mg of PLGA in 1 mL of DCM by an Ultra-Turrax s T25 basic, IKA s -WerkeDigital High-Speed Homogenizer System, at 20 000 rpm for 30 s. In the case of using a porogenic agent, an intermediary step was developed: 100 mL of a gas foaming ABC porous agent solution (7.5 mg mL À1 ) was homogenized with the first emulsion W/O at 20 000 rpm for 30 s.…”

“…A 2 mm thickness PDMS, cured at 80 1C for 30 min, was used to investigate the internal structure, as previously reported. 13…”

“…10 Release can be easily tuned by modifying the size and the microstructure of MPs by experimental or mathematical protocols. [11][12][13] The preservation of protein bioactivity reduces the administration frequency, leading to patient comfort and improvements in compliance, which are fundamental for a successful selfadministered drug delivery system. 14 To overcome the known setbacks associated with oral as well as injectable formulations, transdermal delivery certainly offers a potential alternative.…”

“…22 Unlike the previously developed protocol, 19 the polyvinylpyrrolidone (PVP) tip that is sensitive to the varying humidity and storage time 23 has been replaced with a less fragile PVP-hyaluronic acid (PVP-HA) mixture to allow strong dehydration which is useful for preserving the protein from humidity. A second main change regarding PLGA MPs is that they were synthesized by a modified double emulsion protocol 13 to tune their porosity, and thus speed up cargo release. The morphological properties of the MPs were characterized by a Mastersizer and scanning electron microscopy (SEM).…”