Preparation and in vivo evaluation of insulin-loaded biodegradable nanoparticles prepared from diblock copolymers of PLGA and PEG

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Haggag, Yusuf ; Abdel-Wahab, Yasser ; Ojo, Opeolu ; Osman, Mohamed ; El-Gizawy, Sanaa ; El-Tanani, Mohamed ; Faheem, Ahmed ; McCarron, Paul (2015)
  • Publisher: Elsevier
  • Subject:
    mesheuropmc: technology, industry, and agriculture

The aim of this study was to design a controlled release vehicle for insulin to preserve its\ud stability and biological activity during fabrication and release. A modified, double emulsion,\ud solvent evaporation, technique using homogenisation force optimised entrapment efficiency of\ud insulin into biodegradable nanoparticles (NP) prepared from poly (dl-lactic-co-glycolic acid)\ud (PLGA) and its PEGylated diblock copolymers. Formulation parameters (type of polymer and\ud its concentration, stabiliser concentration and volume of internal aqueous phase) and\ud physicochemical characteristics (size, zeta potential, encapsulation efficiency, in vitro release\ud profiles and in vitro stability) were investigated. In vivo insulin sensitivity was tested by dietinduced\ud type II diabetic mice. Bioactivity of insulin was studied using Swiss TO mice with\ud streptozotocin-induced type I diabetic profile. Insulin-loaded NP were spherical and negatively\ud charged with an average diameter of 200–400 nm. Insulin encapsulation efficiency increased\ud significantly with increasing ratio of co-polymeric PEG. The internal aqueous phase volume\ud had a significant impact on encapsulation efficiency, initial burst release and NP size.\ud Optimised insulin NP formulated from 10% PEG-PLGA retained insulin integrity in vitro,\ud insulin sensitivity in vivo and induced a sustained hypoglycaemic effect from 3 hours to 6 days\ud in type I diabetic mice.
  • References (52)
    52 references, page 1 of 6

    Agarwal, V., Khan, M.A., 2001. Current status of the oral delivery of insulin. Pharm. Technol 10, 76-90.

    Almeida, A.J., Souto, E., 2007. Solid lipid nanoparticles as a drug delivery system for peptides and proteins. Advanced drug delivery reviews 59, 478-490.

    Bailey, C.J., Flatt, P.R., Kwasowski, P., Powell, C.J., Marks, V., 1986. Immunoreactive gastric inhibitory polypeptide and K cell hyperplasia in obese hyperglycaemic (ob/ob) mice fed high fat and high carbohydrate cafeteria diets. Acta endocrinologica 112, 224-229.

    Beletsi, A., Panagi, Z., Avgoustakis, K., 2005. Biodistribution properties of nanoparticles based on mixtures of PLGA with PLGA-PEG diblock copolymers. International journal of pharmaceutics 298, 233-241.

    Blanco-Prieto, M.J., Campanero, M.A., Besseghir, K., Heimgatner, F., Gander, B., 2004.

    Importance of single or blended polymer types for controlled in vitro release and plasma levels of a somatostatin analogue entrapped in PLA/PLGA microspheres. Journal of controlled release : official journal of the Controlled Release Society 96, 437-448.

    Blum, J.S., Saltzman, W.M., 2008. High loading efficiency and tunable release of plasmid DNA encapsulated in submicron particles fabricated from PLGA conjugated with poly-L-lysine.

    Journal of controlled release : official journal of the Controlled Release Society 129, 66-72.

    Carino, G.P., Jacob, J.S., Mathiowitz, E., 2000. Nanosphere based oral insulin delivery. Journal of controlled release : official journal of the Controlled Release Society 65, 261-269.

    Chan, J.M., Zhang, L., Yuet, K.P., Liao, G., Rhee, J.-W., Langer, R., Farokhzad, O.C., 2009. PLGAlecithin-PEG core-shell nanoparticles for controlled drug delivery. Biomaterials 30, 1627- 1634.

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