Double or Simple Emulsion Process to Encapsulate Hydrophilic Oxytocin Peptide in PLA-PEG Nanoparticles
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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 (<200 nm 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 226 nm 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.
KEY WORDSemulsion process factorial experimental design oxytocin peptide polymer nanoparticles
Bovine serum albumin
Dynamic light scattering
Hanks buffer saline solution
Hydroxy ethyl cellulose
High pressure liquid chromatography
New molecular entity
External aqueous phase
Internal aqueous phase
Acknowledgments and Disclosures
The author reports no conflicts of interest in this work.
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