Development, optimization, and evaluation of PEGylated brucine-loaded PLGA nanoparticles

Abstract

The application of nanotechnology to drug delivery systems for cancer therapy has progressively received great attention. The most heavily investigated approach is the development of nanoparticles (NPs) utilizing biodegradable and biocompatible polymers such as poly (lactic-co-glycolic acid) (PLGA). These NPs could be further improved by surface modification utilizing a hydrophilic biodegradable polymer such as polyethylene glycol (PEG) to achieve passive targeting. Modified NPs can deliver drugs such as brucine (BRU), which has shown its potential in cancer therapy. The objective of the current investigation was to develop and evaluate the passive targeting of long-circulating PLGA NPs loaded with BRU. NPs were characterized in terms of drug-excipient compatibility studies, including FTIR and DSC; physicochemical evaluations including particle size, zeta potential, morphological evaluation, entrapment efficiency and percentage yield; total serum protein adsorbed onto NP surfaces; and in vitro release of the loaded drug. Factorial design was employed to attain optimal PLGA-loaded NPs. Finally, the in vivo anti-tumor activity of BRU-loaded PLGA NPs was evaluated in tumor-bearing mice. The NPs obtained had smooth surfaces with particle sizes ranged from 94 ± 3.05 to 253 ± 8.7 nm with slightly positive surface charge ranged from 1.09 ± 0.15 to 3.71 ± 0.44 mV. Entrapment of BRU ranged between 37.5 ± 1.8% and 77 ± 1.3% with yields not less than 70.8%. Total protein adsorbed was less than 25.5 mg total protein/1 mg NP. In vitro drug release was less than 99.1% at 168 h. Finally, significant reductions in tumor growth rate and mortality rate were observed for PEG PLGA NP formulations compared to both BRU solution and naked NPs.

Curcumin Niosomes Prepared from Proniosomal Gels: In Vitro Skin Permeability, Kinetic and In Vivo Studies

“…Then, 0.1 mL of the niosomal preparations were diluted to 4 mL before measurements of particle size. It is important that no drug particles were suspended during measurements [ 20 ].…”

“…The niosomal or emulsion droplet size was determined using Malvern Zetasizer (Malvern Instruments, Malvern, UK) at 25 • C. Then, 0.1 mL of the niosomal preparations were diluted to 4 mL before measurements of particle size. It is important that no drug particles were suspended during measurements [20].…”

Quality by Design for Development, Optimization and Characterization of Brucine Ethosomal Gel for Skin Cancer Delivery

“…Vesicular size and PDI for all BRU loaded ethosome were examined measuring their dynamic light scattering at 25 °C and a scattering angle of 90° [ 46 ]. Zeta potential determination was assessed for the optimized BRU ethosomal gel in which the formulation surface charge was measured through the electrophoretic mobility using Zetasizer apparatus (Malvern Instruments Ltd., Worcestershire, UK) [ 47 ].…”

“…[46]. Zeta potential determination was assessed for the optimized BRU ethosomal gel in which the formulation surface charge was measured through the electrophoretic mobility using Zetasizer apparatus (Malvern Instruments Ltd., Worcestershire, UK) [47].…”

Targeting Antibacterial Effect and Promoting of Skin Wound Healing After Infected with Methicillin-Resistant Staphylococcus aureus for the Novel Polyvinyl Alcohol Nanoparticles

“…Nanoparticles were prepared by solvent evaporation from an oil-water emulsion, as described previously. 21 Briefly, 100 mg of PLGA (50:50, Sigma-Aldrich, USA) was dissolved in 4 mL of dichloromethane (Chongqing Chuandong Chemical Co., Ltd, Chongqing, China) and poured into 20 mL of a 1% (W/W) poly(vinyl alcohol) (PVA, Sigma-Aldrich, USA) and 0.2% sodium polyphosphate (Bella Biology, China) in distilled water. Next, 5 mg of BZK was added to the solution to generate BZK-imbedded PLGA nanoparticles.…”