Investigations on Agglomeration and Haemocompatibility of Vitamin E TPGS Surface Modified Berberine Chloride Nanoparticles

Abstract

The objective of the present study is to investigate the influence of surface modification on systemic stability of NPs. Vitamin E TPGS (1% w/v) was used for surface modification of berberine chloride nanoparticles. Naked and surface modified NPs were incubated in different SBFs (pH 6.8 and 7.4) with or without bile salts and human plasma. NPs were observed for particle agglomeration and morphology by particle size analyzer and TEM, respectively. The haemocompatibility studies were conducted on developed NPs to evaluate their safety profile. The surface modified NPs were stable compared to naked NPs in different SBFs due to the steric stabilization property of vitamin E TPGS. Particle agglomeration was not seen when NPs were incubated in SBF (pH 6.8) with bile salts. No agglomeration was observed in NPs after their incubation in plasma but particle size of the naked NPs increased due to adhesion of plasma proteins. The TEM images confirmed the particle size results. DSC and FT-IR studies confirmed the coexistence of TPGS in surface modified NPs. The permissible haemolysis, LDH release, and platelet aggregation revealed that NPs were compatible for systemic administration. Thus, the study illustrated that the surface modification is helpful in the maintenance of stability of NPs in systemic conditions.

Genistein-Loaded Nanostructured Lipid Carriers for Intravenous Administration: A Quality by Design Based Approach

“…High-performance liquid chromatography with reverse phase was used for quantification of Gen in the prepared NLC formulation. HPLC system was consisted of waters 1525 binary HPLC pump (Waters, USA), rheodyne 7725i manual injector (Waters, USA), C18 reverse-phase (4.6 x75 mm; 3.5 µm) Symmetry® C18 column and waters 2998 photodiode array detector (Waters, USA) 14,29,30 . Acetonitrile: 2mM phosphoric acid buffer in Milli-Q water (50:50) was used as mobile phase and was run at a rate of 1.0 ml/min.…”

“…The LDH released in the supernatant was detected spectrophotometrically by microplate reader (Biorad, Germany) at 500nm. The concentration o LDH released was calculated from the following equation 29,32 :…”

Development and evaluation of vitamin E D-α-tocopheryl polyethylene glycol 1000 succinate-mixed polymeric phospholipid micelles of berberine as an anticancer nanopharmaceutical

“…4,8,17,19,39 In vitro hemolysis assay Hemolysis studies were carried out for empty mMic, along with different Brb-containing samples, according to previous report. 30 The release of hemoglobin from the erythrocytes was used for toxicity measurements of these carriers. Briefly, defibrinated rabbit blood (Thermo Fisher Scientific) was diluted ten times with PBS and centrifuged at 2,000 rpm for 15 minutes.…”

“…30 In vitro cell culture and formation of spheroids PC3, LNCaP, and Caco2 cells were grown in ATCC-formulated F-12K, RPMI-1640, and Eagle's Minimum Essential Medium culture media, respectively, containing 10%-20% FBS and penicillin (100 U/mL)/streptomycin (100 μg/mL) in a humidified environment of 37°C, 5% CO 2 . Spheroids of 400-500 μm diameter were formed from 20,000 cells in 96-well microplates, as described earlier, where Dulbecco's Modified Eagle's Medium/F12 with 1.5% agarose was usedinstead of poly (2-hydroxyethyl) methacrylate -to prevent cell adhesion, followed by microplate centrifugation for 20 minutes at 900 rpm.…”

“…[25][26][27][28][29] Such a mixed micellar system would not only improve Brb solubilization capacity, owing to increased core volume of mMics, created by the planar chromane moiety of VE, but would also provide better protection for the active isoquinolone structure of Brb (Figure 1), effectively enhancing both Brb encapsulation and stability. 30 Based on recent reports, TPGS has shown notable proapoptotic activity as well as a strong ability to overcome drug resistance by inhibiting Pgp efflux pumps. 31,32 In fact, TPGS-incorporating mMic systems have been successfully used to sensitize multidrug-resistant tumors to chemotherapy drugs, including doxorubicin, paclitaxel, gemcitabine, and vinblastine.…”