Abstract
Background: A novel, biologically degradable emulsifier, Lutensol XL 80 was applied in the encapsulation procedure of human serum albumin (HSA) model protein by poly(lactic-co-glycolic acid) (PLGA) to eliminate some drawbacks of common surfactants. Methods: The microcomposites were prepared by the double emulsion solvent-evaporation method. Results: The mean size of the composites was optimally 1.1 μm, while their entrapment efficiency was maximum 54% which was increased by the combination of Lutensol XL 80 with poloxamer 188 surfactant to 77%. 30.5% of the model drug was released during the 5-day study. The release was found to be slower using the combination of the two surfactants probably because of the changed structure of the particles. Conclusions: The main advantage of the drug delivery particles, formulated by the novel surfactant, was their excellent redispersibility after centrifugation. The combination of Lutensol XL 80 with poloxamer 188 in an appropriate ratio also prevented the agglomeration after centrifugation.
Highlights
The modern biotechnological methods have promoted the synthesis of numerous protein therapeutic agents in industrial scale
Lutensol XL 80 was not studied before for this purpose, the results of other emulsifiers were considered for the design of the experiments
The human serum albumin (HSA) loading of the particles was aimed to be smaller than 10% w/w with respect to the poly(lactic-co-glycolic acid) (PLGA) concentration, as we found that with Polyvinyl alcohol (PVA) emulsifier, the entrapment could be maximized (>90%) by applying 5–10% w/v initial protein concentration [4]
Summary
The modern biotechnological methods have promoted the synthesis of numerous protein therapeutic agents in industrial scale. Pharmaceutical Frontiers order to develop more effective therapeutic agents. Both the protection of protein drugs against enzymatic digestion and their controlled release can be achieved by encapsulation into composite nano- or microparticles [1]. Poly(lactic-co-glycolic acid) (PLGA) is one of the most promising FDA-approved encapsulating compounds because of its good biodegradability, biocompatibility and low toxicity [2]. As more and more new protein drugs are being invented, there is an increasing demand to find suitable methods and preparation conditions for the formation of composites, whose properties (e.g., particle size distribution, encapsulation efficiency, release profile) fulfil the strict requirements of drug formulation. A novel, biologically degradable emulsifier, Lutensol XL 80 was applied in the encapsulation procedure of human serum albumin (HSA) model protein by poly(lactic-co-glycolic acid) (PLGA) to eliminate some drawbacks of common surfactants
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