Author(s): Youan BB
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Abstract The aim of this work was to encapsulate superoxide dismutase (SOD) into biodegradable microparticles by spray-drying technique. The nature of the organic solvent to dissolve the polymer, the method of incorporation of the drug in the organic phase (with or without a surfactant, namely sucrose ester of HLB = 6), the surfactant/polymer ratio, and the nature of the biodegradable polyesters were investigated as formulation variables. The polyesters investigated as matrix were poly(epsilon-caprolactone) (PCL), poly(d, l, lactide-co-glycolide) (PLG-RG756), and poly(d, l-lactide) (PLA-R207) of respective molecular weight 78.2 kDa, 84.8 kDa, and 199.8 kDa. At surfactant/polymer ratio of 1/10, the SOD-retained enzymatic activities were higher (> 95\%) for PLG-RG756 and PLA-R207 but relatively lower for the PCL (approximately 85\%) probably due to the PCL relatively higher hydrophobicity. The obtained microparticles exhibited average volume mean diameter of 4-10 microm, the smaller for PCL and the larger for PLG-RG756 polymeric matrix. The in vitro release profile showed that SOD was completely (100\%) released from PLA-R207 in 48 hr and from PLG-RG756 and PCL within 72 hr. These results showed that spray-drying with incorporation of surfactant such as sucrose ester may efficiently encapsulate SOD into biodegradable microparticles. Such formulations may improve the bioavailability of SOD and similar biopharmaceuticals.
This article was published in Drug Deliv
and referenced in Journal of Nanomedicine & Nanotechnology