Microparticles vs. Macroparticles as Curcumin Delivery Vehicles: Structural Studies and Cytotoxic Effect in Human Adenocarcinoma Cell Line (LoVo)

Abstract

This study aimed to characterize the hydrogel micro- and macro-particles designed to deliver curcumin to human colon cancer cells (LoVo). Six series of vehicles based on sodium alginate (micro- and macro-particles, uncoated, coated with chitosan or gelatin) were synthesized. The uncoated microparticles were fabricated using an emulsion-based technique and the uncoated macroparticles with an extrusion technique, with both coupled with ionotropic gelation. The surface morphology of the particles was examined with scanning electron microscopy and the average size was measured. The encapsulation efficiency, moisture content, and swelling index were calculated. The release of curcumin from the particles was studied in an experiment simulating the conditions of the stomach, intestine, and colon. To evaluate the anticancer properties of such targeted drug delivery systems, the cytotoxicity of both curcumin-loaded and unloaded carriers to human colon cancer cells was assessed. The microparticles encapsulated much less of the payload than the macroparticles and released their content in a more prolonged manner. The unloaded carriers were not cytotoxic to LoVo cells, while the curcumin-loaded vehicles impaired their viability—more significantly after incubation with microparticles compared to macroparticles. Gelatin-coated or uncoated microparticles were the most promising carriers but their potential anticancer activity requires further thorough investigation.

Curcumin Loaded Nanocarriers with Varying Charges Augmented with Electroporation Designed for Colon Cancer Therapy

“…In the other study, biodegradable monomethoxy poly(ethylene glycol)poly(lactide) copolymer (MPEG-PLA) micelles were also effectively used to deliver curcumin to colon cancer cells [39]. There were also effectively used vehicles based on sodium alginate (micro-and macro-particles, uncoated, coated with chitosan or gelatin), where gelatin-based microparticles revealed the highest potential against LoVo cells [43]. The available study clearly indicates that curcumin encapsulation is promising against colon cancer [34,38,39].…”

Multilayered Curcumin-loaded Hydrogel Microcarriers With Antimicrobial Function

“…Strategies to construct properly designed microcarriers for multiple applications are guided by various factors: (i) appropriate physicochemical features: shape, size, stiffness, morphology, and surface charge; (ii) type of building blocks which should be of a biocompatible matter; (iii) appropriate chemical and colloidal stability; (iv) efficacious payload encapsulation; (v) ease of surface functionalisation [25][26][27]. Taking these outlines into account, the synthetic route of microcapsules consisted of two major steps and, thus, integrated an emulsion method [25] to obtain alginate-based microspheres loaded with CUR and the LbL technique [26] to form bilayer microcapsules coated with CHIT or PAH and antimicrobial decorated polyelectrolytes 1-4 (for details, see Table 1: PAA-C(O)O-(CH2)n-N + (CH3)3(m); n = 6, 12; m = 8, 10, 14%) as schematically described in Figure 3. Two microcapsule systems were formed, differing in the number and type of coatings.…”

“…Two microcapsule systems were formed, differing in the number and type of coatings. Based on our previous research, the CHIT and PAH polymers were selected for the first coating layer for hydrogel microsystems [25,40]. Then, hydrogels were coated with 1-4 polymers as the second layer.…”

“…An emulsion method was applied to prepare ALG-based microspheres encapsulating CUR, as previously described [25], with slight modifications. First, CUR was dispersed in a 1.5% ALG aqueous solution (1:100 w/v) containing 1% (w/v) Tween 80.…”

“…For this reason, several studies have reported the encapsulation of CUR into microparticles for potential therapeutic application [24]. Our group has recently prepared and characterised hydrogel micro-and macroparticles based on ALG, CHIT, and gelatin to deliver curcumin to colon cancer cells [25]. As a continuation of our studies on rational drug delivery [26,27], we designed, fabricated, and characterised multilayered hydrogel microcarriers, comprising the CUR-loaded core and the custom-designed LbL coatings, the latter formed by CHIT or PAH and -as the outer antimicrobial layer -alkylene quaternary ammonium salt functionalised poly(acrylic acid) (for abbreviations and structure details, see Table 1 in Section 2.1).…”