Impact of Cross-linking and Drying Method on Drug Delivery Performance of Casein–Pectin Microparticles

Abstract

Abstract. Pectin is a heteropolysaccharide which has been investigated for the development of colonspecific drug delivery systems. Polymers have been associated with pectin to reduce its aqueous solubility and improve the performance of drug delivery systems. Pectin-casein interaction is widely known in food research, but it has not been fully considered by pharmaceutical scientists. Thus, this study investigated the potential of casein-pectin microparticles as a drug delivery system and clarified the impact of cross-linking and drying methods on the in vitro release of indomethacin (IND) or acetaminophen (PCT) from microparticles. Microparticles were prepared by coacervation and dried by spray or spouted bed methods. Drug recovery, in vitro drug release, size, morphology, and the thermal and diffractometric properties of dried microparticles were determined. Spray-dried non-cross-linked microparticles were able to prolong IND release, and pectin was still degraded by pectinolytic enzymes. On the other hand, glutaraldehyde cross-linking prevented the enzymatic breakdown of pectin without improving IND release. Spouted bed drying reduced IND recovery from all microparticles when compared with spray drying, thus the successful spouted bed drying of microparticles depends on the chemical characteristics of both the drug and the polymer. Release data from PCT microparticles suggested that the microparticle formulation should be improved to bring about a more efficient delivery of water-soluble drugs. In conclusion, casein-pectin microparticles show great potential as a drug delivery system because casein reduces the water solubility of pectin. The drying method and cross-linking process had significant effects on the in vitro performance of these microparticles.

Skimmed milk powder and pectin decorated solid lipid nanoparticle containing soluble curcumin used for the treatment of colorectal cancer

“…Likewise, the intensity and peak location of amine groups at 672–910 cm −1 area triggered by the twisting vibration were altered in the coating, demonstrating the presence of N–H groups. The strength of carboxylate groups (1,385 cm −1 ) in CP‐SD‐SLNs reduced because the carboxylate groups contributed to the coating process (Marreto, Ramos, Silva, Freitas, & de Freitas, ).…”

“…Free CMN exhibited −OH stretch vibration at 3,324.68 cm −1 and 3,015.16 cm −1 owning the presence of two hydroxyl groups, and the peaks exhibited at 1,742.37, 1,629.55, 1,597.73, and 1,507.1 cm −1 for the existence of carbonyl groups in its structure (Firman, Lisa, Raffaella, & Neil, 2017 Likewise, the intensity and peak location of amine groups at 672-910 cm −1 area triggered by the twisting vibration were altered in the coating, demonstrating the presence of N-H groups. The strength of carboxylate groups (1,385 cm −1 ) in CP-SD-SLNs reduced because the carboxylate groups contributed to the coating process (Marreto, Ramos, Silva, Freitas, & de Freitas, 2013).…”

Ultrasonic atomization and polyelectrolyte complexation to produce gastroresistant shell–core microparticles

“…19 Furthermore, similar principles were proposed by Luo et al 20 and successfully used in formulation of casein/pectin nanocomplexes as potential oral delivery vehicles. Nandy et al 7 used a combination of the release retardant ethyl cellulose and Eudragit RS 100 mixed with Eudragit S100 to produce microparticles by a quasi-emulsion solvent diffusion technique.…”

“…Furthermore pH‐sensitive Eudragits, that is, Eudragit L or Eudragit S, were used to encapsulate indomethacin by applying an emulsion–solvent evaporation method . The need to combine different polymers to encapsulate indomethacin was evident in Marreto et al ., that used pectin cross‐linked with casein, to reduce its aqueous solubility in order to achieve a better encapsulation efficiency, as polymer in microparticles prepared by coacervation and then dried by spray or spouted bed methods . Furthermore, similar principles were proposed by Luo et al .…”

Biological Activity and Pharmacological Application of Pectic Polysaccharides: A Review

“…It is reported that pectin-based polymers were discovered as having a novel potential to create highly technological materials with enhanced characteristics. Casein–pectin as a multiple-unit drug delivery system was designed for the colonic drug delivery of two model drugs with different solubilities: acetaminophen (PCT) and indomethacin (IND) [130]. The effect of chemical cross-linking and the drying method (spouted or spray-drying) on in vitro drug release, microcapsule digestibility, and structural integrity was investigated.…”