Evaluation of sucrose esters as alternative surfactants in microencapsulation of proteins by the solvent evaporation method

Abstract

KEYWORDS: proteins, microencapsulation, solvent evaporation, sucrose ester, surfactants Sucrose esters (SE) are surfactants with potential pharmaceutical applications because of their low toxicity, biocompatibility, and excellent biodegradability. The objective of the study was to investigate SE as alternative surfactants in stabilizing emulsions for the preparation of protein-loaded microparticles. To achieve this goal, using bovine serum albumin as model protein and 75/25 poly(d,l-lactide-co-glycolide) as polymer carrier, we have investigated the influence of the following formulation variables on particle characteristics: (1) SE concentration from 0.01% to 1% (wt/vol), (2) hydrophile-lipophile balance (HLB) value of SE from 6 to 15, and (3) the nature of emulsion stabilizer. The formulations were characterized using ATR-FTIR spectroscopy, bicinchoninic acid protein assay, optical microscopy and SDS-PAGE. Results showed that at 0.05% (wt/vol) surfactant concentration, SE with HLB of 6 to 15 provided discrete and spherical microparticles with the highest encapsulation efficiency compared with controls polyvinyl alcohol (PVA) and poloxamer 188. These results may be explained by the difference in critical micelle concentration, diffusion, and partition coefficient among the tested surfactants. HLB values were consistent with SE spectral data. The protein molecular weight was preserved after the encapsulation process. The effective SE concentration was far less (20-to 200-fold) than that is usually required for PVA in microencapsulation of proteins. However, the encapsulation efficiency was relatively lower (~13.5%). These preliminary results suggest that it may be desirable to optimize such formulations in vitro and in vivo for SE to be eventually used as alternative surfactants in the development of microparticulate systems for parenteral delivery of protein and gene medicines.

Nanoparticles of Polyethylene Sebacate: A New Biodegradable Polymer

“…This is explained by the low CMC value of lutrol F 68 (0.1%) (22) and Tween 80 (0.0013%) (23). In general, at the same concentration, mean size of nanoparticles was in the order of PVA > lutrol F 68 > Tween 80.…”

Microencapsulation Efficacy of d-Limonene by Spray Drying Using Various Combinations of Wall Materials and Emulsifiers

“…Microemulsions based on nonionic emulsifiers have been extensively investigated for their formulation, phase behavior, structural point of view, and also for the oxidation stability of the oil (Azuma et al, 2009;Tual et al, 2006;Takaishi et al, 2006). Youan et al (2003) reported an increasing interest in using SE in the microencapsulation process for stabilizing emulsions. Kwak et al (2001) reported that polyglycerol monostearate could be used as an effective coating material to microencapsulate lactase using an airless paint sprayer.…”

New pH-Sensitive Glycopolymers for Colon-Specific Drug Delivery

“…The objective of the study was to investigate SE as alternative surfactants in stabilizing emulsions for the preparation of protein-loaded microparticles (Youan, Hussain, and Nguyen 2003). Design and synthesis of new biodegradable and biocompatible polymeric hydrogel systems based on suger-containing monomers was the primary objective in our study.…”