Abstract
Oral drug delivery using NPs is a current strategy for poorly absorbed molecules. It offers significant improvement in terms of bioavailability. However, the encapsulation of proteins and peptides in polymeric NPs is a challenge. Firstly, the present study focused on the double emulsion process in order to encapsulate the OXY peptide. Then the technique was challenged by a one-step simplified process, the simple emulsion. In order to study the influence of formulation and process parameters, factorial experimental designs were carried on. The responses observed were the NP size (<200nm in order to penetrate the intestinal mucus layer), the suspension stability (ZP < |30| mV) and the OXY loading. It was thus found that the amount and the nature of surfactant, the ratio between the phases, the amount of PLA-PEG polymer and OXY, the presence of a viscosifying agent, and the duration of the sonication could significantly influence the responses. Finally, OXY-loaded NPs from both processes were obtained with NP size of 195 and 226nm and OXY loading of 4 and 3.3% for double and simple emulsions, respectively. The two processes appeared to be suitable for OXY encapsulation and comparable in term of NP size, peptide drug load and release obtained.
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