Preparation, in vitro and in vivo evaluation of mPEG-PLGA nanoparticles co-loaded with syringopicroside and hydroxytyrosol

Abstract

This study investigated the therapeutic efficiency of monomethoxy polyethylene glycol-poly(lactic-co-glycolic acid) (mPEG-PLGA) co-loaded with syringopicroside and hydroxytyrosol as a drug with effective targeting and loading capacity as well as persistent circulation in vivo. The nanoparticles were prepared using a nanoprecipitation method with mPEG-PLGA as nano-carrier co-loaded with syringopicroside and hydroxytyrosol (SH-NPs). The parameters like in vivo pharmacokinetics, biodistribution in vivo, fluorescence in vivo endomicroscopy, and cellular uptake of SH-NPs were investigated. Results showed that the total encapsulation efficiency was 32.38 ± 2.76 %. Total drug loading was 12.01 ± 0.42 %, particle size was 91.70 ± 2.11 nm, polydispersity index was 0.22 ± 0.01, and zeta potential was -24.5 ± 1.16 mV for the optimized SH-NPs. The nanoparticle morphology was characterized using transmission electron microscopy, which indicated that the particles of SH-NPs were in uniformity within the nanosize range and of spherical core shell morphology. Drug release followed Higuchi kinetics. Compared with syringopicroside and hydroxytyrosol mixture (SH), SH-NPs produced drug concentrations that persisted for a significantly longer time in plasma following second-order kinetics. The nanoparticles moved gradually into the cell, thereby increasing the quantity. ALT, AST, and MDA levels were significantly lower on exposure to SH-NPs than in controls. SH-NPs could inhibit the proliferation of HepG2.2.15 cells and could be taken up by HepG2.2.15 cells. The results confirmed that syringopicroside and hydroxytyrosol can be loaded simultaneously into mPEG-PLGA nanoparticles. Using mPEG-PLGA as nano-carrier, sustained release, high distribution in the liver, and protective effects against hepatic injury were observed in comparison to SH.

Paclitaxel-loaded star-shaped copolymer nanoparticles for enhanced malignant melanoma chemotherapy against multidrug resistance

“…PTX-loaded CA-PLGA-TPGS, PLGA-TPGS, and PLGA NPs had the zeta potentials of −11.5±1.8, −16.8±2.5, and −28.7±3.4 mV, respectively. With ionized carboxyl groups from polyglycolic acid and polylactic acid segments, all the NPs had negative surface charges 41. Furthermore, the zeta potentials of PTX-loaded CA-PLGA-TPGS and PLGA-TPGS NPs were decreased by TPGS segment compared with that of PLGA NPs 30…”

Preparation, Characterization, and Antioxidant Activity Evaluation of Liposomes Containing Water-Soluble Hydroxytyrosol from Olive

“…One of the strategies to overcome the rapid release of HT and increasing its pharmacological bioactivity in vivo is to encapsulate it in a suitable delivery system [ 17 ]. Recently, water in oil (W/O) emulsions, microemulsions [ 18 ] and nanoparticles [ 19 ] were shown to be effective carriers of HT, as a natural antioxidant, which retained its scavenging ability inhibiting approximately 90% of the free radical within the first 5 min of incubation. In addition, liposomes, a directed drug carrier for targeted drug-delivery systems, is a new drug formulation generally capable of encapsulating lipid-soluble substances [ 20 , 21 , 22 , 23 ].…”

Polyphenols Nanoencapsulation for Therapeutic Applications

“…This study demonstrated that nanoencapsulation significantly reduced the toxic effects of HC. Qingxia Guan et al [109] investigated the therapeutic efficiency of monomethoxy polyethylene glycol-poly (lactic co-glycolic acid) (mPEG-PLGA) nanoparticles co-loaded with syringopicroside and hydroxytyrosol prepared using a nanoprecipitation method. In particular, they analyzed the parameters of in vivo pharmacokinetics, biodistribution, fluorescence, endomicroscopy and cellular uptake.…”

“…This vector (92 nm with a narrow polydispersity and a negative zeta potential of -24.5 mV) showed an encapsulation efficiency of ~ 33% and drug loading of 12%, that allows persisting drug plasma concentrations while the nanoparticles moved gradually into the cell, thereby increasing the available quantity. The in vitro effect resulted in the liver hepatocellular carcinoma (HepG2.2.15) cells proliferation inhibition [109]. Olive leaf extract containing oleuropein and hydroxytyrosol was encapsulated in β-CD, increasing the water solubility and antioxidant capacity of the encapsulated polyphenols [110].…”

“…Magnetic bovine serum albumin (BSA) nanoparticles [105] Carbohydrate matrix Chitosan nanoparticles [106] Chitosan nanoparticles incorporated into an aqueous cream [107,108] Polyester nanoparticles mPEG-PLGA nanoparticles [109] Cyclodextrins β-CD [110] HP-β-CD [111] Micelles whey protein concentrate (WPC) and pectin complexes [112] acidic or neutral pH and slightly soluble under alkali conditions. For another CU is unstable in the gut and trace amounts of curcumin that pass through the gastrointestinal tract are rapidly degraded [118].…”