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Biopharmaceutical characterisation of insulin and recombinant human growth hormone loaded lipid submicron particles produced by supercritical gas micro-atomisation.
Int J Pharm. 2009 Sep 08; 379(1):51-8.IJ

Abstract

Homogeneous dispersions of insulin and recombinant human growth hormone (rh-GH) in tristearin/phosphatidylcholine/PEG mixtures (1.3:1.3:0.25:0.15 w/w ratio) were processed by supercritical carbon dioxide gas micro-atomisation to produce protein-loaded lipid particles. The process yielded spherical particles, with a 197+/-94 nm mean diameter, and the insulin and rh-GH recovery in the final product was 57+/-8% and 48+/-5%, respectively. In vitro, the proteins were slowly released for about 70-80 h according to a diffusive mechanism. In vivo, the insulin and glucose profiles in plasma obtained by subcutaneous administration of a dose of particles containing 2 microg insulin to diabetic mice overlapped that obtained with 2 microg of insulin in solution. Administration of a dose of particles containing 5 microg insulin resulted in faster and longer glycaemia reduction. Oral administration of 20 and 50 microg insulin equivalent particles produced a significant hypoglycaemic effect. The glucose levels decreased since 2h after administration, reaching about 50% and 70% glucose reduction in 1-2h with the lower and higher dose, respectively. As compared to subcutaneous administration, the relative pharmacological bioavailability obtained with 20 and 50 microg equivalent insulin particles was 7.7% and 6.7%, respectively. Daily subcutaneous administration of 40 microg of rh-GH-loaded particles to hypophysectomised rats induced similar body weight increase as 40 microg rh-GH in solution. The daily oral administration of 400 microg rh-GH equivalent particles elicited a slight body weight increase, which corresponded to a relative pharmacological bioavailability of 3.4% compared to subcutaneous administration.

Authors+Show Affiliations

Department of Pharmaceutical Sciences, University of Padua, Via F. Marzolo, 5, 35131 Padua, Italy.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

19545616

Citation

Salmaso, Stefano, et al. "Biopharmaceutical Characterisation of Insulin and Recombinant Human Growth Hormone Loaded Lipid Submicron Particles Produced By Supercritical Gas Micro-atomisation." International Journal of Pharmaceutics, vol. 379, no. 1, 2009, pp. 51-8.
Salmaso S, Bersani S, Elvassore N, et al. Biopharmaceutical characterisation of insulin and recombinant human growth hormone loaded lipid submicron particles produced by supercritical gas micro-atomisation. Int J Pharm. 2009;379(1):51-8.
Salmaso, S., Bersani, S., Elvassore, N., Bertucco, A., & Caliceti, P. (2009). Biopharmaceutical characterisation of insulin and recombinant human growth hormone loaded lipid submicron particles produced by supercritical gas micro-atomisation. International Journal of Pharmaceutics, 379(1), 51-8. https://doi.org/10.1016/j.ijpharm.2009.06.014
Salmaso S, et al. Biopharmaceutical Characterisation of Insulin and Recombinant Human Growth Hormone Loaded Lipid Submicron Particles Produced By Supercritical Gas Micro-atomisation. Int J Pharm. 2009 Sep 8;379(1):51-8. PubMed PMID: 19545616.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Biopharmaceutical characterisation of insulin and recombinant human growth hormone loaded lipid submicron particles produced by supercritical gas micro-atomisation. AU - Salmaso,Stefano, AU - Bersani,Sara, AU - Elvassore,Nicola, AU - Bertucco,Alberto, AU - Caliceti,Paolo, Y1 - 2009/06/21/ PY - 2009/03/09/received PY - 2009/06/02/revised PY - 2009/06/03/accepted PY - 2009/6/24/entrez PY - 2009/6/24/pubmed PY - 2009/10/27/medline SP - 51 EP - 8 JF - International journal of pharmaceutics JO - Int J Pharm VL - 379 IS - 1 N2 - Homogeneous dispersions of insulin and recombinant human growth hormone (rh-GH) in tristearin/phosphatidylcholine/PEG mixtures (1.3:1.3:0.25:0.15 w/w ratio) were processed by supercritical carbon dioxide gas micro-atomisation to produce protein-loaded lipid particles. The process yielded spherical particles, with a 197+/-94 nm mean diameter, and the insulin and rh-GH recovery in the final product was 57+/-8% and 48+/-5%, respectively. In vitro, the proteins were slowly released for about 70-80 h according to a diffusive mechanism. In vivo, the insulin and glucose profiles in plasma obtained by subcutaneous administration of a dose of particles containing 2 microg insulin to diabetic mice overlapped that obtained with 2 microg of insulin in solution. Administration of a dose of particles containing 5 microg insulin resulted in faster and longer glycaemia reduction. Oral administration of 20 and 50 microg insulin equivalent particles produced a significant hypoglycaemic effect. The glucose levels decreased since 2h after administration, reaching about 50% and 70% glucose reduction in 1-2h with the lower and higher dose, respectively. As compared to subcutaneous administration, the relative pharmacological bioavailability obtained with 20 and 50 microg equivalent insulin particles was 7.7% and 6.7%, respectively. Daily subcutaneous administration of 40 microg of rh-GH-loaded particles to hypophysectomised rats induced similar body weight increase as 40 microg rh-GH in solution. The daily oral administration of 400 microg rh-GH equivalent particles elicited a slight body weight increase, which corresponded to a relative pharmacological bioavailability of 3.4% compared to subcutaneous administration. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/19545616/Biopharmaceutical_characterisation_of_insulin_and_recombinant_human_growth_hormone_loaded_lipid_submicron_particles_produced_by_supercritical_gas_micro_atomisation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(09)00381-0 DB - PRIME DP - Unbound Medicine ER -