Exenatide loaded PLGA microspheres for long-acting antidiabetic therapy: preparation, characterization, pharmacokinetics and pharmacodynamics

Abstract

We herein fabricated the exenatide-loaded microspheres by a water in oil in oil (W/O/O) method, which presented great effect on glycemic control with low initial burst release and reduced risk of gastrointestinal intolerance and hypoglycemia.

Effect of Stabilizers on Encapsulation Efficiency and Release Behavior of Exenatide-Loaded PLGA Microsphere Prepared by the W/O/W Solvent Evaporation Method

“…The CD spectra of exenatide had two specific minima at 209 and 224 nm wavelength, which indicated the presence of α-helix (Figure 8a) [25]. There was no difference between the extracted exenatide from ELPM6 and the unprocessed one, which means that the secondary structure of exenatide in ELPM6 microspheres can be maintained after the W/O/W-SE and lyophilization processes using a combination of various stabilizers [28,31]. On the other hand, for exenatide extracted from ELPM1 without protective additives in the formulation, a significant difference in the two minima at 209 and 224 nm was observed in the spectrum, implying a change in the secondary structure.…”

“…For example, adverse effects like vomiting may increase with higher rates of exenatide burst release [11]. Many groups are currently attempting to suppress exenatide burst release and the incomplete release of commercial products [12][13][14][15][16][17][18][19][20][21][22][23][24][25][26][27][28][29][30][31]. Although many investigations into exenatide formulations and dosages have been performed, there is still a lack of useful information about exenatide stability.…”

Preparation and evaluation of celecoxib nanosuspensions for bioavailability enhancement

“…The morphology of CLX coarse powder was evaluated using scanning electron microscope (SEM, S-3000N, Hitachi, Japan). 33 Prior to examination, samples were mounted onto a metal stub using a carbon double sided adhesive tape, and further sputtered with a thin layer of gold palladium. The instrument was operated at a voltage of 10 kV.…”

Component-based biocompatibility and safety evaluation of polysorbate 80

“…The cytotoxicity of each constituent isolated from polysorbate 80 was evaluated using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5diphenyltetrazolium bromide) colorimetric test by calculating the percentage of viable cells. 16,17 In brief, LO2 cells were seeded in 96-well plates at a density of 5000 cells per well in RPMI 1640 medium containing 5% FBS and allowed to grow overnight. Aer incubation with each constitute at serial concentrations (10, 25, 50, 100, 200, 300, 400 and 500 mg mL À1 ) at 37 C for 24 h, 200 mL of MTT (5 mg mL À1 ) was added to each well.…”