CONTEXT: Oral administration of insulin is severely limited by very low bioavailability. Biocompatible polymeric nanocarriers have been investigated to overcome this problem. Flow focusing (FF) has revolutionized current engineering of poly(D,L-lactide-co-glycolide) (PLGA) based micromedicines. This technique has never been used to formulate insulin-loaded PLGA microparticles. OBJECTIVE: Investigation of the benefits rising from the synthesis of insulin-loaded PLGA microplatforms by FF, compared to double emulsion/solvent evaporation method. MATERIALS AND METHODS: Both synthesis methodologies were compared in terms of geometry, surface physicochemical properties and insulin vehiculization capabilities. The stability of the peptide during the formulation procedure was further analysed. RESULTS: FF permitted the preparation of insulin-loaded microcarriers with better geometry and physicochemical properties for the oral route, along with greater insulin loading capabilities and sustained insulin release kinetics. DISCUSSION AND CONCLUSION: Results have lead to the identification of the best formulation conditions for the engineering of insulin-loaded PLGA microparticles against diabetes.
CONTEXT: Oral administration of insulin is severely limited by very low bioavailability. Biocompatible polymeric nanocarriers have been investigated to overcome this problem. Flow focusing (FF) has revolutionized current engineering of poly(D,L-lactide-co-glycolide) (PLGA) based micromedicines. This technique has never been used to formulate insulin-loaded PLGA microparticles. OBJECTIVE: Investigation of the benefits rising from the synthesis of insulin-loaded PLGA microplatforms by FF, compared to double emulsion/solvent evaporation method. MATERIALS AND METHODS: Both synthesis methodologies were compared in terms of geometry, surface physicochemical properties and insulin vehiculization capabilities. The stability of the peptide during the formulation procedure was further analysed. RESULTS: FF permitted the preparation of insulin-loaded microcarriers with better geometry and physicochemical properties for the oral route, along with greater insulin loading capabilities and sustained insulin release kinetics. DISCUSSION AND CONCLUSION: Results have lead to the identification of the best formulation conditions for the engineering of insulin-loaded PLGA microparticles against diabetes.
Authors: Mariana Amaral; Ana Sofia Martins; José Catarino; Pedro Faísca; Pradeep Kumar; João F Pinto; Rui Pinto; Isabel Correia; Lia Ascensão; Ricardo A Afonso; M Manuela Gaspar; Adília J Charmier; Isabel Vitória Figueiredo; Catarina Pinto Reis Journal: Biomolecules Date: 2020-04-27
Authors: Gracia García-García; Fátima Fernández-Álvarez; Laura Cabeza; Ángel V Delgado; Consolación Melguizo; José C Prados; José L Arias Journal: Polymers (Basel) Date: 2020-11-25 Impact factor: 4.329