Synthesis And Characterization Of pH-Sensitive Polyelectrolyte Nanogels For Oral Delivery Of Bovine Serum Albumin And Insulin As Model Proteins
Loading...
Date
2018-02
Authors
Mudassir, Jahanzeb
Journal Title
Journal ISSN
Volume Title
Publisher
Universiti Sains Malaysia
Abstract
Peptide and protein are administered parentrally owing to their instability and insufficient bioavailability through oral route. Parenteral administration is associated with poor patient compliance due to pain and discomfort by multiple injections. Oral administration can be beneficial to improve patient compliance and physiologic response to peptide and protein (e.g. insulin). The aim of the present study was to synthesize pH sensitive polyelectrolyte methyl methacrylate/itaconic acid (MMA/IA) nanogels to be used as a carrier for oral delivery of model proteins (BSA and insulin). The nanogels were synthesized using monomers methyl methacrylate (MMA), itaconic acid (IA) and a crosslinker ethylene glycol dimethacrylate (EGDMA) via free radical polymerization. Several parameters were optimized during the synthesis of pH sensitive MMA/IA nanogels. The optimized parameters to synthesis the nanogels were ethanol/water 70/30 v/v, dilution volume 96/57.6 v/v, EGDMA 1.5 mol % and MMA/IA 70/30 mol %. The 1H NMR and FTIR spectra showed absence of vinyl proton peaks of MMA, IA and EGDMA, thus indicating successful synthesis of nanogels. The LC-TOF-MS showed that the molecular weight was 934.717. The XRD analysis revealed that the nanogels were in the amorphous form and had the swelling ratio of 8.08±0.64 at pH 7.4. The nanogels had the particle size of 229.10±2.09 nm, polydispersity index (PdI) of 0.111±0.03 and zeta potential of -43.1±1.81mv. The transmission electron microscope (TEM) analysis showed that the nanogels had irregular shape. The in vitro toxicity performed by MTT assays using caco-2 cell revealed that the nanogels was nontoxic at concentrations of 0.25, 0.5 and 1 mg/ml. Meanwhile, the in vivo toxicity study using Sprague Dawley rats also showed that the nanogels at a dose of 2000 mg/kg body weight was non-toxic.
Description
Keywords
Ph-sensitive polyelectrolyte nanogels for , oral delivery of bovine serum albumin